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pubmed23n0001_1400	Inhibition of drug-induced anorexia in rats by methysergide.	Iproniazid was found to reduce food consumption in fasting rats. Combined treatment of iproniazid with tryptophan resulted in a significantly greater anorexic action whilst tryptophan alone had no effect on food consumption. Iproniazid treatment was associated with a significant increase in brain 5-hydroxytryptamine (5-HT) concentration but in association with tryptophan higher brain 5-HT concentrations were recorded. The anorexic action of the iproniazid-tryptophan combination was antagonized in a dose-dependent fashion by methysergide. Equivalent levels of anorexia induced by fenfluramine and mazindol were similarly antagonized by methysergide in a dose-related manner. The results suggest a common role of 5-HT in the inhibition of eating behaviour in fasting rats when anorexia is induced by iproniazid, fenfluramine or mazindol, sensitive to a specific 5-HT antagonist.	Inhibition of drug-induced anorexia in rats by methysergide. Iproniazid was found to reduce food consumption in fasting rats. Combined treatment of iproniazid with tryptophan resulted in a significantly greater anorexic action whilst tryptophan alone had no effect on food consumption. Iproniazid treatment was associated with a significant increase in brain 5-hydroxytryptamine (5-HT) concentration but in association with tryptophan higher brain 5-HT concentrations were recorded. The anorexic action of the iproniazid-tryptophan combination was antagonized in a dose-dependent fashion by methysergide. Equivalent levels of anorexia induced by fenfluramine and mazindol were similarly antagonized by methysergide in a dose-related manner. The results suggest a common role of 5-HT in the inhibition of eating behaviour in fasting rats when anorexia is induced by iproniazid, fenfluramine or mazindol, sensitive to a specific 5-HT antagonist.	2,658
pubmed23n0001_1401	Cerebral monoamine metabolism in guinea-pigs with ascorbic acid deficiency.	Guinea-pigs kept on a diet deficient in vitamin C showed, after 3 weeks, a marked decrease of ascorbic acid in brain and blood leucocytes as well as of the activity of alkaline phosphatase in blood plasma. Pair-fed animals did not exhibit these changes. The alpha-methyl-p-tyrosine (alpha MpT)-induced diminution of noradrenaline in the hypothalamus and the rest of the brain was attenuated in pair-fed animals, but restored in guinea-pigs deficient in ascorbic acid. The cerebral noradrenaline content (without administration of alpha MpT) showed a decrease in both pair-fed and ascorbic acid deficient animals. The noradrenaline of the heart exhibited a similar tendency. The alpha MpT-induced dopamine decrease in the striatum of ascorbic acid deficient animals was attenuated and the dopamine content (without alpha MpT administration) decreased. Pair-fed animals showed a similar tendency. The striatal concentration of homovanillic acid (HVA) was diminished in both pair-fed and ascorbic acid deficient guinea-pigs. The cerebral content of 5-hydroxyindoleacetic acid showed a decrease in pair-fed as well as in ascorbic acid deficient animals. It is concluded that ascorbic acid deficiency enhances the turnover of brain noradrenaline, whereas under-nutrition without ascorbic acid deficiency (pair-feeding) diminishes the turnover of cerebral noradrenaline, 5-hydroxytryptamine and striatal dopamine.	Cerebral monoamine metabolism in guinea-pigs with ascorbic acid deficiency. Guinea-pigs kept on a diet deficient in vitamin C showed, after 3 weeks, a marked decrease of ascorbic acid in brain and blood leucocytes as well as of the activity of alkaline phosphatase in blood plasma. Pair-fed animals did not exhibit these changes. The alpha-methyl-p-tyrosine (alpha MpT)-induced diminution of noradrenaline in the hypothalamus and the rest of the brain was attenuated in pair-fed animals, but restored in guinea-pigs deficient in ascorbic acid. The cerebral noradrenaline content (without administration of alpha MpT) showed a decrease in both pair-fed and ascorbic acid deficient animals. The noradrenaline of the heart exhibited a similar tendency. The alpha MpT-induced dopamine decrease in the striatum of ascorbic acid deficient animals was attenuated and the dopamine content (without alpha MpT administration) decreased. Pair-fed animals showed a similar tendency. The striatal concentration of homovanillic acid (HVA) was diminished in both pair-fed and ascorbic acid deficient guinea-pigs. The cerebral content of 5-hydroxyindoleacetic acid showed a decrease in pair-fed as well as in ascorbic acid deficient animals. It is concluded that ascorbic acid deficiency enhances the turnover of brain noradrenaline, whereas under-nutrition without ascorbic acid deficiency (pair-feeding) diminishes the turnover of cerebral noradrenaline, 5-hydroxytryptamine and striatal dopamine.	2,659
pubmed23n0001_1402	The effect of an aldosterone antagonist on the protective action of carbenoxolone on the gastric mucosal barrier.	The effect of an aldosterone antagonist on the protective action of carbenoxolone sodium on the gastric mucosal barrier has been studied in three dogs with Heidenhain pouches. The net fluxes of hydrogen ion and sodium ion were measured before, during, and after contact with a 10 mM bile acid solution at pH 2, in pouches which had not been treated with drugs, in pouches treated with carbenoxolone sodium and in pouches treated with both carbenoxolone sodium and the aldosterone antagonist, spironolactone. Hydrogen ion back diffusion from, and sodium ion gain by the untreated pouch was increased by 10 mM bile acid solution. Addition to the pouches of either carbenoxolone sodium alone or carbenoxolone sodium and spironolactone reduced the hydrogen ion back diffusion after exposure to the bile acid solution. The spironolactone did not change the protective effect of carbenoxolone on the gastric mucosal barrier. Carbenoxolone did not change the increased sodium ion diffusion caused by bile.	The effect of an aldosterone antagonist on the protective action of carbenoxolone on the gastric mucosal barrier. The effect of an aldosterone antagonist on the protective action of carbenoxolone sodium on the gastric mucosal barrier has been studied in three dogs with Heidenhain pouches. The net fluxes of hydrogen ion and sodium ion were measured before, during, and after contact with a 10 mM bile acid solution at pH 2, in pouches which had not been treated with drugs, in pouches treated with carbenoxolone sodium and in pouches treated with both carbenoxolone sodium and the aldosterone antagonist, spironolactone. Hydrogen ion back diffusion from, and sodium ion gain by the untreated pouch was increased by 10 mM bile acid solution. Addition to the pouches of either carbenoxolone sodium alone or carbenoxolone sodium and spironolactone reduced the hydrogen ion back diffusion after exposure to the bile acid solution. The spironolactone did not change the protective effect of carbenoxolone on the gastric mucosal barrier. Carbenoxolone did not change the increased sodium ion diffusion caused by bile.	2,660
pubmed23n0001_1403	The quantification of kanamycin ototoxicity in the rat using conditioned tone discrimination.	Twelve male Lister hooded rats were conditioned to discriminate an 8 kHz tone (56.5 +/- 0.5 dB re 0.0002 dyne cm-2) and were subsequently injected subcutaneously with kanamycin (400 mg kg-1 day-1) for 28 days; during this time and for five weeks after dosage was stopped, the nature and extent of the resultant hearing deficits were studied. The animals' Preyer reflex thresholds were determined at intervals during the study. Only one rat was unaffected by the kanamycin dosage. The onset of hearing impairment (reduced discrimination performance), which was gradual in some rats and sudden in others, generally occurred during the fourth week of kanamycin dosage although the earliest onset was towards the end of the second week. In most animals the hearing impairment progressed after kanamycin was stopped and in one rat there was a latency between the end of drug dosage and onset of hearing impairment. Hearing impairment was irreversible in five rats. One rat, whose impairment was slight, recovered normal hearing. Some rats showed a reduced discrimination performance at a time when their Preyer reflex threshold showed no elevation suggesting that kanamycin, at least initially, caused a threshold elevation rather than reduced sensitivity to intense sounds.	The quantification of kanamycin ototoxicity in the rat using conditioned tone discrimination. Twelve male Lister hooded rats were conditioned to discriminate an 8 kHz tone (56.5 +/- 0.5 dB re 0.0002 dyne cm-2) and were subsequently injected subcutaneously with kanamycin (400 mg kg-1 day-1) for 28 days; during this time and for five weeks after dosage was stopped, the nature and extent of the resultant hearing deficits were studied. The animals' Preyer reflex thresholds were determined at intervals during the study. Only one rat was unaffected by the kanamycin dosage. The onset of hearing impairment (reduced discrimination performance), which was gradual in some rats and sudden in others, generally occurred during the fourth week of kanamycin dosage although the earliest onset was towards the end of the second week. In most animals the hearing impairment progressed after kanamycin was stopped and in one rat there was a latency between the end of drug dosage and onset of hearing impairment. Hearing impairment was irreversible in five rats. One rat, whose impairment was slight, recovered normal hearing. Some rats showed a reduced discrimination performance at a time when their Preyer reflex threshold showed no elevation suggesting that kanamycin, at least initially, caused a threshold elevation rather than reduced sensitivity to intense sounds.	2,661
pubmed23n0001_1404	The bioavailability in man of ICRF-159 a new oral antineoplastic agent.	The bioavailability of the antineoplastic agent, ICRF-159, has been examined in 12 patients receiving the drug in single and subdivided dose schedules in an attempt to account for the differences in toxicity found with the different schedules clinically. Recovery of radioactivity in the urine after single large doses (13.3-19.4 g) was 8.5 +/- 3.0% of the administered dose. After doses of 3.8-5.55 g recovery was 22.7 +/- 10.5% and after the same dose subdivided into 3 equal aliquots it was 52 +/- 8.7%. Unrecovered radioactivity was largely accounted for in the faeces. Plasma radioactivity levels in 2 patients after high and low dose were equivalent. Toxicity of the drug paralleled urinary recovery of radioactivity. It is concluded that schedule dependence of toxicity of ICRF-159 is at least partly due to bioavailability factors.	The bioavailability in man of ICRF-159 a new oral antineoplastic agent. The bioavailability of the antineoplastic agent, ICRF-159, has been examined in 12 patients receiving the drug in single and subdivided dose schedules in an attempt to account for the differences in toxicity found with the different schedules clinically. Recovery of radioactivity in the urine after single large doses (13.3-19.4 g) was 8.5 +/- 3.0% of the administered dose. After doses of 3.8-5.55 g recovery was 22.7 +/- 10.5% and after the same dose subdivided into 3 equal aliquots it was 52 +/- 8.7%. Unrecovered radioactivity was largely accounted for in the faeces. Plasma radioactivity levels in 2 patients after high and low dose were equivalent. Toxicity of the drug paralleled urinary recovery of radioactivity. It is concluded that schedule dependence of toxicity of ICRF-159 is at least partly due to bioavailability factors.	2,662
pubmed23n0001_1405	Cornea preparation for in vitro bio-pharmaceutical evaluation of ophthalmic dosage forms.	A system has been developed for a specific biopharmaceutical purpose: testing for ophthalmic preparations, the influence of formulation on drug transport through the cornea. The apparatus is a lucite cell, divided in two compartments by a clamped rabbit cornea. Physiological conditions are ensured by a supply of oxygenated perfusion medium. They are monitored by electrical conductivity and corneal thickness measurements. Reliability of the system was tested in a set of experiments.	Cornea preparation for in vitro bio-pharmaceutical evaluation of ophthalmic dosage forms. A system has been developed for a specific biopharmaceutical purpose: testing for ophthalmic preparations, the influence of formulation on drug transport through the cornea. The apparatus is a lucite cell, divided in two compartments by a clamped rabbit cornea. Physiological conditions are ensured by a supply of oxygenated perfusion medium. They are monitored by electrical conductivity and corneal thickness measurements. Reliability of the system was tested in a set of experiments.	2,663
pubmed23n0001_1406	A study of the human metabolism of secbutobarbitone.	The urinary excretion of secbutobarbitone (I) and its metabolites has been studied quantitatively using combined gas chromatography-mass spectrometry. After a single oral dose was given to healthy male volunteers, unchanged drug (5-9%), 2'-hydroxysecbutobarbitone (II, 1.7-3.2%), 2'-oxosecbutobarbitone (III, less than 1%), and the carboxylic acid (IV, 24-34%) were found. The kinetics of the excretion process were studied.	A study of the human metabolism of secbutobarbitone. The urinary excretion of secbutobarbitone (I) and its metabolites has been studied quantitatively using combined gas chromatography-mass spectrometry. After a single oral dose was given to healthy male volunteers, unchanged drug (5-9%), 2'-hydroxysecbutobarbitone (II, 1.7-3.2%), 2'-oxosecbutobarbitone (III, less than 1%), and the carboxylic acid (IV, 24-34%) were found. The kinetics of the excretion process were studied.	2,664
pubmed23n0001_1407	The identification and analysis of the metabolic products of mephentermine.	Phentermine (Ib), N-hydroxymephentermine (Ic) and N-hydroxyphentermine (Id) were identified as metabolic products after in vitro incubation of mephentermine (Ia) with rabbit liver microsomal fractions. Compounds Ia, Ib and Ic were also identified as excretion products in the urine of a human subject given a single dose of mephentermine (Ia) sulphate. Derivatization with acetic anhydride, trifluoroacetic anhydride and the trimethylsilyl donor reagent N,O-bis-(trimethylsilyl)-trifluoroacetamide (BSTFA) or hexamethyldisilazane (HMDS) were used for qualitative identification of the metabolic products Ib-Id by g.l.c.-mass spectrometry and for quantitative determination of Ia-Id after extraction from rabbit hepatic homogenates. The synthesis of N-hydroxymephentermine (Ic) and the properties of the metabolic products are reported.	The identification and analysis of the metabolic products of mephentermine. Phentermine (Ib), N-hydroxymephentermine (Ic) and N-hydroxyphentermine (Id) were identified as metabolic products after in vitro incubation of mephentermine (Ia) with rabbit liver microsomal fractions. Compounds Ia, Ib and Ic were also identified as excretion products in the urine of a human subject given a single dose of mephentermine (Ia) sulphate. Derivatization with acetic anhydride, trifluoroacetic anhydride and the trimethylsilyl donor reagent N,O-bis-(trimethylsilyl)-trifluoroacetamide (BSTFA) or hexamethyldisilazane (HMDS) were used for qualitative identification of the metabolic products Ib-Id by g.l.c.-mass spectrometry and for quantitative determination of Ia-Id after extraction from rabbit hepatic homogenates. The synthesis of N-hydroxymephentermine (Ic) and the properties of the metabolic products are reported.	2,665
pubmed23n0001_1408	A rapid g.l.c. procedure for the determination of codeine and norcodeine in biological fluids based on micro-phase extraction techniques.	Therapeutic serum concentrations of codeine can be virtually completely extracted and obtained sufficiently concentrated for g.c. measurement without distillation, by acid extraction of the drug from the initial crude organic extracts of alkalinized serum followed by a micro-phase back extraction step. The procedure has simplicity, rapidity and eliminates concentration by distillation and background interference. The method can be readily adapted for the seperate measurements of codeine and norcodeine and it can also be used for similar analysis of other body fluids.	A rapid g.l.c. procedure for the determination of codeine and norcodeine in biological fluids based on micro-phase extraction techniques. Therapeutic serum concentrations of codeine can be virtually completely extracted and obtained sufficiently concentrated for g.c. measurement without distillation, by acid extraction of the drug from the initial crude organic extracts of alkalinized serum followed by a micro-phase back extraction step. The procedure has simplicity, rapidity and eliminates concentration by distillation and background interference. The method can be readily adapted for the seperate measurements of codeine and norcodeine and it can also be used for similar analysis of other body fluids.	2,666
pubmed23n0001_1409	Plasma sodium concentration and sodium excretion in the anaesthetized dog.	1. The effect of acute alterations of plasma sodium concentration (PNa) on renal sodium excretion (UNaV) was investigated by three types of experiments on anaesthetized dogs: (a) A local increase in PNa at one kidney was produced by infusion of hypertonic saline directly into its artery while systemic levels of PNa were stabilized by haemodialysis. (b) Systemic levels of PNa were lowered by exchange transfusion of blood for an equal volume of salt-free dextran-in-dextrose solution. The results were contrasted with those observed after similar exchanges, but using dextran-in-saline solution. (c) The level of PNa was altered by varying the sodium concentration of a saline solution infused at a fixed rate either intravenously or into one renal artery. 2. All three types of experiment suggest a dependence of UNaV on PNa Analysis demonstrated that this relationship was not due to contemporary changes in: packed cell volume; plasma solids concentration; plasma potassium concentration; blood pressure or plasma hydrogen ion concentration. The distribution of these variables did not change with PNa except for plasma hydrogen ion concentration. Moreover, the relationship persisted when data were selected to exclude clearance periods in which the value for any variable had shifted past the group mean obtained before PNa was altered. 3. The fall in UNaV at low levels of PNa could be attributed to a fall in glomerular filtration rate (GFR), but the progressive rise in UNaV seen as PNa exceeded 150 m-mole 1(-1) occurred despite a fall in GFR and no apparent change in the mean filtered load of sodium. These results suggest that the increased sodium excretion accompanying raised levels of PNa is due to reduced tubular re-absorption of sodium.	Plasma sodium concentration and sodium excretion in the anaesthetized dog. 1. The effect of acute alterations of plasma sodium concentration (PNa) on renal sodium excretion (UNaV) was investigated by three types of experiments on anaesthetized dogs: (a) A local increase in PNa at one kidney was produced by infusion of hypertonic saline directly into its artery while systemic levels of PNa were stabilized by haemodialysis. (b) Systemic levels of PNa were lowered by exchange transfusion of blood for an equal volume of salt-free dextran-in-dextrose solution. The results were contrasted with those observed after similar exchanges, but using dextran-in-saline solution. (c) The level of PNa was altered by varying the sodium concentration of a saline solution infused at a fixed rate either intravenously or into one renal artery. 2. All three types of experiment suggest a dependence of UNaV on PNa Analysis demonstrated that this relationship was not due to contemporary changes in: packed cell volume; plasma solids concentration; plasma potassium concentration; blood pressure or plasma hydrogen ion concentration. The distribution of these variables did not change with PNa except for plasma hydrogen ion concentration. Moreover, the relationship persisted when data were selected to exclude clearance periods in which the value for any variable had shifted past the group mean obtained before PNa was altered. 3. The fall in UNaV at low levels of PNa could be attributed to a fall in glomerular filtration rate (GFR), but the progressive rise in UNaV seen as PNa exceeded 150 m-mole 1(-1) occurred despite a fall in GFR and no apparent change in the mean filtered load of sodium. These results suggest that the increased sodium excretion accompanying raised levels of PNa is due to reduced tubular re-absorption of sodium.	2,771
pubmed23n0001_1410	Synthesis of angiotensin II antagonists containing N- and O-methylated and other amino acid residues.	[1-N-Methylisoasparagine,8-isoleucine]- (I), [1-sarcosine,4-N-methyltyrosine,8-isoleucine]- (II), [1-sarcosine,5-N-methylisoleucine,8-isoleucine]- (III), [1-sarcosine,8-N-methylisoleucine]- (IV), [1-sarcosine8k-N-methylisoleucine,8-N-methylisoleucine]- (V), [1-sarcosine,8-O-methylthreonine]- (VI), [1-sarcosine,8-methionine]- (VII), and [1-sarcosine,8-serine]angiotensin II (VIII), synthesized by Merrifield's solid-phase procedure, possess respectively 0.8, 0.3, 0.5, 1.0, 0.0, 0.5, 3.7, and 0.7% pressor activity of angiotensin II (vagotomized, ganglion-blocked rats). They caused an initial rise in blood pressure (30 min of infusion, 250 ng/kg/min in vagotomized, ganglion-blocked rats) of 16.57, 9.80, 22.80, 32.00, 7.00, 15.06, 32.50, and 11.42 mmHg and showed secretory activity (isolated cat adrenal medulla) of 1.0, 0.1, 0.01, 0.1, less than 0.01, 0.1, less than 0.01, and 0.05% of angiotensin II. On isolated organs pA2 values (rabbit aortic strips) of 8.74, 7.44, 7.64, 7.85, 7.89, 8.76, 8.63, and 8.08, and pA2 values (cat adrenal medulla of 8.16, 9.16, 9.31, 8.00, 8.00, 7.00, 9.16, and 9.33 were obtained. Dose ratios (ratio of ED20 of angiotensin II during infusion of the antagonist and before infusion of the antagonist) in vagotomized, ganglion-blocked rats, infused at 250 ng/kg/min, were 33.43, 2.14, 3.26, 2.99, 0.62, 62.52, incalculable, and 11.15, respectively. The results obtained suggest that (a) analogs I and VI are potent antagonists of the pressor response of angiotensin II in normal rat, VI being the most potent antagonist thus far synthesized; (b) replacement of position 4 (Tyr) with MeTyr or position 5 and/or 8 (Ile) with Melle in [1-sarcosine,8-isoleucine]angiotensin II reduced the antagonist activity of this peptide (rabbit aortic strips and rats), indicating that steric hindrance imposed due to N-methylation in positions 4, 5, or 8 was not favorable in eliminating the initial pressor activity or prolonging the duration of action of [Sar1, Ile8]angiotensin II without reducing its antagonistic properties; (c) except II, none of the analogs showed any enhanced duration of action, suggesting that N-methylation in positions 5 or 8 did not afford protection against proteolytic enzymes; and (d) perfusion studies in cat adrenals indicated that all of these analogs are only very weak secretagogues. With the exception of [Sar1,Thr(ObetaMe)8]angiotensin II, which gave lower antagonistic properties, all other analogs had either similar antagonistic properties or were better antagonists in adrenal medulla than in smooth muscle.	Synthesis of angiotensin II antagonists containing N- and O-methylated and other amino acid residues. [1-N-Methylisoasparagine,8-isoleucine]- (I), [1-sarcosine,4-N-methyltyrosine,8-isoleucine]- (II), [1-sarcosine,5-N-methylisoleucine,8-isoleucine]- (III), [1-sarcosine,8-N-methylisoleucine]- (IV), [1-sarcosine8k-N-methylisoleucine,8-N-methylisoleucine]- (V), [1-sarcosine,8-O-methylthreonine]- (VI), [1-sarcosine,8-methionine]- (VII), and [1-sarcosine,8-serine]angiotensin II (VIII), synthesized by Merrifield's solid-phase procedure, possess respectively 0.8, 0.3, 0.5, 1.0, 0.0, 0.5, 3.7, and 0.7% pressor activity of angiotensin II (vagotomized, ganglion-blocked rats). They caused an initial rise in blood pressure (30 min of infusion, 250 ng/kg/min in vagotomized, ganglion-blocked rats) of 16.57, 9.80, 22.80, 32.00, 7.00, 15.06, 32.50, and 11.42 mmHg and showed secretory activity (isolated cat adrenal medulla) of 1.0, 0.1, 0.01, 0.1, less than 0.01, 0.1, less than 0.01, and 0.05% of angiotensin II. On isolated organs pA2 values (rabbit aortic strips) of 8.74, 7.44, 7.64, 7.85, 7.89, 8.76, 8.63, and 8.08, and pA2 values (cat adrenal medulla of 8.16, 9.16, 9.31, 8.00, 8.00, 7.00, 9.16, and 9.33 were obtained. Dose ratios (ratio of ED20 of angiotensin II during infusion of the antagonist and before infusion of the antagonist) in vagotomized, ganglion-blocked rats, infused at 250 ng/kg/min, were 33.43, 2.14, 3.26, 2.99, 0.62, 62.52, incalculable, and 11.15, respectively. The results obtained suggest that (a) analogs I and VI are potent antagonists of the pressor response of angiotensin II in normal rat, VI being the most potent antagonist thus far synthesized; (b) replacement of position 4 (Tyr) with MeTyr or position 5 and/or 8 (Ile) with Melle in [1-sarcosine,8-isoleucine]angiotensin II reduced the antagonist activity of this peptide (rabbit aortic strips and rats), indicating that steric hindrance imposed due to N-methylation in positions 4, 5, or 8 was not favorable in eliminating the initial pressor activity or prolonging the duration of action of [Sar1, Ile8]angiotensin II without reducing its antagonistic properties; (c) except II, none of the analogs showed any enhanced duration of action, suggesting that N-methylation in positions 5 or 8 did not afford protection against proteolytic enzymes; and (d) perfusion studies in cat adrenals indicated that all of these analogs are only very weak secretagogues. With the exception of [Sar1,Thr(ObetaMe)8]angiotensin II, which gave lower antagonistic properties, all other analogs had either similar antagonistic properties or were better antagonists in adrenal medulla than in smooth muscle.	2,777
pubmed23n0001_1411	Synthesis and enzymic activity of some novel xanthine oxidase inhibitors. 3-Substituted 5,7-dihydroxypyrazolo(1,5-alpha)pyrimidines.	A series of 3-substituted 5,7-dihydroxypyrazolo[1,5-alpha]pyrimidines containing various aromatic [phenyl- (3e), 3-pyridyl- (3f), p-bromophenyl- (3g), p-chlorophenyl- (3h), p-acetamidophenyl- (3i), p-tolyl- (3j), m-tolyl- (3k), 3,4-methylenedioxyphenyl- (3m), or naphthyl- (3n)] or nonaromatic [hydrogen- (3a), nitro- (3b), bromo- (3c), or chloro- (3d)] substituents in the 3 position was synthesized and tested as inhibitors of xanthine oxidase. The compounds (3a-m) were synthesized by condensation of the appropriate 3-amino-4-substituted pyrazole with diethyl malonate in alcoholic sodium methoxide and neutralization of the resulting enol sodium salts. As inhibitors of xanthine oxidase, 3e-n greater than 3a,c,d congruent to allopurinol greater than 3b. The 3-aryl-substituted compounds 3e-n were 30-160 times better xanthine oxidase inhibitors than allopurinol using hypoxanthine as substrate and 10-80 times better using xanthine as substrate, as evidenced by a comparison of Ki values. The inhibition by all compounds (3a-n) was totally reversible and of the noncompetitive or mixed type. A study of the pH dependence of xanthine oxidase inhibition by 3a,e,g and allopurinol indicated that the 3-aryl substituents facilitated binding to the enzyme. These and the above results show that the compounds reported here inhibit xanthine oxidase by a mechanism which is significantly different from that of allopurinol.	Synthesis and enzymic activity of some novel xanthine oxidase inhibitors. 3-Substituted 5,7-dihydroxypyrazolo(1,5-alpha)pyrimidines. A series of 3-substituted 5,7-dihydroxypyrazolo[1,5-alpha]pyrimidines containing various aromatic [phenyl- (3e), 3-pyridyl- (3f), p-bromophenyl- (3g), p-chlorophenyl- (3h), p-acetamidophenyl- (3i), p-tolyl- (3j), m-tolyl- (3k), 3,4-methylenedioxyphenyl- (3m), or naphthyl- (3n)] or nonaromatic [hydrogen- (3a), nitro- (3b), bromo- (3c), or chloro- (3d)] substituents in the 3 position was synthesized and tested as inhibitors of xanthine oxidase. The compounds (3a-m) were synthesized by condensation of the appropriate 3-amino-4-substituted pyrazole with diethyl malonate in alcoholic sodium methoxide and neutralization of the resulting enol sodium salts. As inhibitors of xanthine oxidase, 3e-n greater than 3a,c,d congruent to allopurinol greater than 3b. The 3-aryl-substituted compounds 3e-n were 30-160 times better xanthine oxidase inhibitors than allopurinol using hypoxanthine as substrate and 10-80 times better using xanthine as substrate, as evidenced by a comparison of Ki values. The inhibition by all compounds (3a-n) was totally reversible and of the noncompetitive or mixed type. A study of the pH dependence of xanthine oxidase inhibition by 3a,e,g and allopurinol indicated that the 3-aryl substituents facilitated binding to the enzyme. These and the above results show that the compounds reported here inhibit xanthine oxidase by a mechanism which is significantly different from that of allopurinol.	2,778
pubmed23n0001_1412	Immobilized glucuronosyltransferase for the synthesis of conjugates.	Partially purified rabbit liver UDPglucuronosyltransferase is immobilized on agarose by the cyanogen bromide activation method. Both soluble and matrix-bound enzyme preparations display very similar Km and pH optimum. The storage stability of the immobilized enzyme at 4 degrees is 5-10 times improved over the soluble preparations. The agarose-bound UDPglucuronosyltransferase is successfully used in the synthesis of p-nitrophenyl glucuronide in an overall yield of 50-70%. The matrix-bound enzyme is reusable over an extended period of time and offers an easy and convenient synthetic tool for various drug glucuronides.	Immobilized glucuronosyltransferase for the synthesis of conjugates. Partially purified rabbit liver UDPglucuronosyltransferase is immobilized on agarose by the cyanogen bromide activation method. Both soluble and matrix-bound enzyme preparations display very similar Km and pH optimum. The storage stability of the immobilized enzyme at 4 degrees is 5-10 times improved over the soluble preparations. The agarose-bound UDPglucuronosyltransferase is successfully used in the synthesis of p-nitrophenyl glucuronide in an overall yield of 50-70%. The matrix-bound enzyme is reusable over an extended period of time and offers an easy and convenient synthetic tool for various drug glucuronides.	2,779
pubmed23n0001_1413	The limits of informed consent.	The patient, a 59-year-old man, was referred to a psychiatric hospital with what appeared initially to be the signs and symptoms of mental disorder. In hospital a lesion of the brain was diagnosed and surgery was proposed to relieve the condition. The patient, however, during this and subsequent admissions to hospital, refused operation. His refusal to consent was regarded as valid as he seemed to have good insight into his condition. Finally, under section 26 of the Mental Health Act, he was treated surgically. Unfortunately the patient died six weeks later of intracranial haemorrhage. Three comments are made on this case - two by psychiatrists, Dr K Davison and Dr Ashley Robin, the other by a professor of Christian ethics, Professor F C Blackie. Both psychiatrists argue that when a patient's mind is affected by mental or organic illness to the degree that 'he cannot bring a rational and conscious mind' to the question of his treatment then the doctor, in consultation with the relatives, making clear to them the likely course of events if an operation is not performed, must take whatever is the proper course of action, in this case surgery. In this view, such an operation performed immediately the diagnosis was confirmed might not have been so complicated. Professor Blackie, commending 'the attempt to regard the patient as a responsible human being' with a 'moral right to be consulted on all aspects of treatment', questions in this patient the limits to which the appeal to reason was carried. He concludes that 'in this situation the advice and consent of the family must weigh more heavily than the statements of the patient'.	The limits of informed consent. The patient, a 59-year-old man, was referred to a psychiatric hospital with what appeared initially to be the signs and symptoms of mental disorder. In hospital a lesion of the brain was diagnosed and surgery was proposed to relieve the condition. The patient, however, during this and subsequent admissions to hospital, refused operation. His refusal to consent was regarded as valid as he seemed to have good insight into his condition. Finally, under section 26 of the Mental Health Act, he was treated surgically. Unfortunately the patient died six weeks later of intracranial haemorrhage. Three comments are made on this case - two by psychiatrists, Dr K Davison and Dr Ashley Robin, the other by a professor of Christian ethics, Professor F C Blackie. Both psychiatrists argue that when a patient's mind is affected by mental or organic illness to the degree that 'he cannot bring a rational and conscious mind' to the question of his treatment then the doctor, in consultation with the relatives, making clear to them the likely course of events if an operation is not performed, must take whatever is the proper course of action, in this case surgery. In this view, such an operation performed immediately the diagnosis was confirmed might not have been so complicated. Professor Blackie, commending 'the attempt to regard the patient as a responsible human being' with a 'moral right to be consulted on all aspects of treatment', questions in this patient the limits to which the appeal to reason was carried. He concludes that 'in this situation the advice and consent of the family must weigh more heavily than the statements of the patient'.	2,780
pubmed23n0001_1414	Calcium-potassium-stimulated net potassium efflux from human erythrocyte ghosts.	In the presence of 8 mM external Ca++, the K+ permeability of human red cell ghosts increases provided K+ is also present in the medium. This increase does not represent K+/K+ exchange but a stimulation of net K+ efflux. The stimulation is half-maximal at 0.7 +/- 0.15 mM (n=5). At concentrations above 4.0 mM, external K+ inhibits net K+ efflux. Similar stimulatory and inhibitory effects of external K were also observed in intact cells after exposure to Pb++ or to Ca++ in the presence of fluoride, iodoacetate plus adenosine, or propranolol, suggesting that a common K+ -activated K+ -specific transfer system may be involved under all of these various circumstances. Internal K+ also stimulates net K+ efflux from ghosts, but it is uncertain whether internal K+ is an absolute requirement for the K+ permeability increase. In contrast to external Na+ which slightly stimulates K+ efflux, internal Na+ inhibits. The inhibition by internal Na+ is abolished by sufficiently high concentrations of external K+, showing that K+ binding to the outer membrane surface and Na+ binding to the internal surface are mutually interdependent. In red cell ghosts the Ca++ -K+ -stimulated net K+ efflux increases with increasing pH until a plateau is reached between pH 7.2 and 8.0. In fluoride-poisoned intact cells, the Ca++-K+ stimulated flux passes through a maximum around pH 6.8. Neither internal nor external Mg++ interferes with the combined effects of Ca++ and K+. Similarly, external EDTA has no influence at concentrations which are far lower than the Ca++ concentration required to produce a maximal response. In contrast, low concentrations of internal EDTA prevent the permeability change.	Calcium-potassium-stimulated net potassium efflux from human erythrocyte ghosts. In the presence of 8 mM external Ca++, the K+ permeability of human red cell ghosts increases provided K+ is also present in the medium. This increase does not represent K+/K+ exchange but a stimulation of net K+ efflux. The stimulation is half-maximal at 0.7 +/- 0.15 mM (n=5). At concentrations above 4.0 mM, external K+ inhibits net K+ efflux. Similar stimulatory and inhibitory effects of external K were also observed in intact cells after exposure to Pb++ or to Ca++ in the presence of fluoride, iodoacetate plus adenosine, or propranolol, suggesting that a common K+ -activated K+ -specific transfer system may be involved under all of these various circumstances. Internal K+ also stimulates net K+ efflux from ghosts, but it is uncertain whether internal K+ is an absolute requirement for the K+ permeability increase. In contrast to external Na+ which slightly stimulates K+ efflux, internal Na+ inhibits. The inhibition by internal Na+ is abolished by sufficiently high concentrations of external K+, showing that K+ binding to the outer membrane surface and Na+ binding to the internal surface are mutually interdependent. In red cell ghosts the Ca++ -K+ -stimulated net K+ efflux increases with increasing pH until a plateau is reached between pH 7.2 and 8.0. In fluoride-poisoned intact cells, the Ca++-K+ stimulated flux passes through a maximum around pH 6.8. Neither internal nor external Mg++ interferes with the combined effects of Ca++ and K+. Similarly, external EDTA has no influence at concentrations which are far lower than the Ca++ concentration required to produce a maximal response. In contrast, low concentrations of internal EDTA prevent the permeability change.	2,781
pubmed23n0001_1415	Analog circuit of the Acetabularia membrane.	The high membrane potential of Acetabularia (Em=-170mV) is due to an electrogenic pump in parallel with the passive diffusion system (Ed=-80mV) which could be studied separately in the cold, when the pump is blocked. Electrical measurements under normal conditions show that the pump pathway consists of its electromotive force Ep with two elements P1 and P2 in series; P2 is shunted by a large capacitance (Cp=3mF cm-2). The nonlinear current-voltage relationship of P1 (light- and temperature-sensitive) could be determined separately; it reflects the properties of a carrier-mediated electrogenic pump. The value of Ep(-190 mV) indicates a stoichiometry of 2:1 between electrogenically transported charges and ATP. The electrical energy normally stored in Cp, compares well with the metabolic energy, stored in the ATP pool. The nonlinear current-voltage relationship of P2 (attributed to phosphorylating reactions) is also sensitive to light and temperature and is responsible for the region of negative conductance of the overall current-voltage relationship. The power of the pump (1 muW cm-2) amounts to some percent of the total energy turnover. The high Cl- fluxes (1 nmol cm-2 sec-1) and the electrical properties of the plasmalemma are not as closely related as assumed previously. For kinetic reasons, a direct and specific Cl- pathway between the vacuole and outside is postulated to exist.	Analog circuit of the Acetabularia membrane. The high membrane potential of Acetabularia (Em=-170mV) is due to an electrogenic pump in parallel with the passive diffusion system (Ed=-80mV) which could be studied separately in the cold, when the pump is blocked. Electrical measurements under normal conditions show that the pump pathway consists of its electromotive force Ep with two elements P1 and P2 in series; P2 is shunted by a large capacitance (Cp=3mF cm-2). The nonlinear current-voltage relationship of P1 (light- and temperature-sensitive) could be determined separately; it reflects the properties of a carrier-mediated electrogenic pump. The value of Ep(-190 mV) indicates a stoichiometry of 2:1 between electrogenically transported charges and ATP. The electrical energy normally stored in Cp, compares well with the metabolic energy, stored in the ATP pool. The nonlinear current-voltage relationship of P2 (attributed to phosphorylating reactions) is also sensitive to light and temperature and is responsible for the region of negative conductance of the overall current-voltage relationship. The power of the pump (1 muW cm-2) amounts to some percent of the total energy turnover. The high Cl- fluxes (1 nmol cm-2 sec-1) and the electrical properties of the plasmalemma are not as closely related as assumed previously. For kinetic reasons, a direct and specific Cl- pathway between the vacuole and outside is postulated to exist.	2,782
pubmed23n0001_1416	Nigericin-induced charge transfer across membranes.	The electric properties of the bilayer lecithin membranes have been studied in the presence of the antibiotic nigericin. When the antibiotic concentration is about 10(-7) ohm-1 cm-2. The potassium ion concentration gradient gives rise to a transmembrane potential of the order of 40 mV per 10-fold concentration gradient with the side of the higher potassium concentration negative. The transmembrane potential produced by the hydrogen ion concentration gradient is a function of the potassium ion concentration which is equal on both sides of the membrane. For low potassium ion concentrations the hydrogen potential has the expected polarity with the solution having higher concentration of protons negative. For potassium ion concentrations exceeding 0.03 M the hydrogen potential has the reverse polarity. This unexpected result cannot be accounted for in terms of the available simple hypotheses about the charge transport mechanism for nigericin in BLM. In order to account for the experimental results obtained, a theoretical approach has been developed based on the assumption that charge is transported across the membrane by nigericin dimers. The theoretical predicitons are in satisfactory agreement with the experimental results. The model also yields some predictions which may be verified in future experiments.	Nigericin-induced charge transfer across membranes. The electric properties of the bilayer lecithin membranes have been studied in the presence of the antibiotic nigericin. When the antibiotic concentration is about 10(-7) ohm-1 cm-2. The potassium ion concentration gradient gives rise to a transmembrane potential of the order of 40 mV per 10-fold concentration gradient with the side of the higher potassium concentration negative. The transmembrane potential produced by the hydrogen ion concentration gradient is a function of the potassium ion concentration which is equal on both sides of the membrane. For low potassium ion concentrations the hydrogen potential has the expected polarity with the solution having higher concentration of protons negative. For potassium ion concentrations exceeding 0.03 M the hydrogen potential has the reverse polarity. This unexpected result cannot be accounted for in terms of the available simple hypotheses about the charge transport mechanism for nigericin in BLM. In order to account for the experimental results obtained, a theoretical approach has been developed based on the assumption that charge is transported across the membrane by nigericin dimers. The theoretical predicitons are in satisfactory agreement with the experimental results. The model also yields some predictions which may be verified in future experiments.	2,783
pubmed23n0001_1417	Reactions of aminomalononitrile with electrophiles.	Aminomalononitrile (HCN trimer) reacts with electrophiles such as aldehydes and acrylonitrile under very mild conditions of temperature and pH to produce intermediates which, after acid hydrolysis, yield amino acids. The following amino acids have been identified and quantitated: glycine, D, L-erythro- and D, L-threo-beta - hydroxyaspartic acids, D, L glutamic acid, and D, L-threonine and allo-threonine. The mechanism of their formation and the possible significance of these reactions in prebiotic syntheses are discussed.	Reactions of aminomalononitrile with electrophiles. Aminomalononitrile (HCN trimer) reacts with electrophiles such as aldehydes and acrylonitrile under very mild conditions of temperature and pH to produce intermediates which, after acid hydrolysis, yield amino acids. The following amino acids have been identified and quantitated: glycine, D, L-erythro- and D, L-threo-beta - hydroxyaspartic acids, D, L glutamic acid, and D, L-threonine and allo-threonine. The mechanism of their formation and the possible significance of these reactions in prebiotic syntheses are discussed.	2,786
pubmed23n0001_1418	[Diagnosis and therapy of primary defects of immunity (author's transl)].	Immunological responses are divided into those mediated by humoral antibody (B-Cells) and those by cells (T-Cells). Both depend upon the activity of small lymphocytes which become thymus or bursa analogue dependent during embryonic development. Primary immundeficiencies are therefor defects of lymphocytes attributed in most cases to gene defects. Early diagnosis is the necessary prerequisit for possible treatment. Tests for assessing the cellular immune status are: skin testes and in vitro tests. Clinical syndroms are: lymphocytopenia, hypoplasia, deficiency of lymphocytes in lymphatic tissues normal cortical germinal centres. Recurrent infections with viruses, candida or pneumocystis carinii are common. Tests for assesing the humoral immune status are: measurement of immunglobulin levels in serum, isohaemagglutinins, tests for antibody formation following active immunization, in vitro tests. Clinical syndroms are: no germinal centres in lymphnodes, no plasma cells. Recurrent bacterial infections. Treatment of B-cell deficiencies: immunglobulin replacement therapy. Treatment of T-cell deficiencies by grafting of thymus transplants. Combined immune deficiencies are treated with bone marrow transplants from matched donors. For bone marrow transplantation germfree state seems to be the ideal situation to protect the patient against infection before the therapeutic maneuver and for prevention of graft versus host reaction in the posttransplantation period.	[Diagnosis and therapy of primary defects of immunity (author's transl)]. Immunological responses are divided into those mediated by humoral antibody (B-Cells) and those by cells (T-Cells). Both depend upon the activity of small lymphocytes which become thymus or bursa analogue dependent during embryonic development. Primary immundeficiencies are therefor defects of lymphocytes attributed in most cases to gene defects. Early diagnosis is the necessary prerequisit for possible treatment. Tests for assessing the cellular immune status are: skin testes and in vitro tests. Clinical syndroms are: lymphocytopenia, hypoplasia, deficiency of lymphocytes in lymphatic tissues normal cortical germinal centres. Recurrent infections with viruses, candida or pneumocystis carinii are common. Tests for assesing the humoral immune status are: measurement of immunglobulin levels in serum, isohaemagglutinins, tests for antibody formation following active immunization, in vitro tests. Clinical syndroms are: no germinal centres in lymphnodes, no plasma cells. Recurrent bacterial infections. Treatment of B-cell deficiencies: immunglobulin replacement therapy. Treatment of T-cell deficiencies by grafting of thymus transplants. Combined immune deficiencies are treated with bone marrow transplants from matched donors. For bone marrow transplantation germfree state seems to be the ideal situation to protect the patient against infection before the therapeutic maneuver and for prevention of graft versus host reaction in the posttransplantation period.	2,800
pubmed23n0001_1419	[Effect of the chronic action of small doses of ionizing radiation of the excretion of gaseous metabolic products in albino rats].	White rats were kept in sealed chambers for 3 months and were exposed to chronic gamma-irradiation (100 mur/day). The effect of the exposure on the excretion of some metabolites--ammonia, acetone, carbon monoxide, phenol and organic substances measured by their oxidability--was studied. Under the influence of low doses of gamma-irradiation the excretion of acetone and organic substances decreased, whereas that of carbon monoxide, phenol and ammonia increased. Possible mechanisms responsible for these changes are discussed.	[Effect of the chronic action of small doses of ionizing radiation of the excretion of gaseous metabolic products in albino rats]. White rats were kept in sealed chambers for 3 months and were exposed to chronic gamma-irradiation (100 mur/day). The effect of the exposure on the excretion of some metabolites--ammonia, acetone, carbon monoxide, phenol and organic substances measured by their oxidability--was studied. Under the influence of low doses of gamma-irradiation the excretion of acetone and organic substances decreased, whereas that of carbon monoxide, phenol and ammonia increased. Possible mechanisms responsible for these changes are discussed.	2,802
pubmed23n0001_1420	[Effect of hyperoxia and hypokinesia on the formation and excretion of gaseous metabolic products in rats].	It has been shown experimentally that a 30-day exposure of white rats to hypokinesia and moderate hyperoxia decreases elimination of ammonia and increases the formation and release into an enclosed atmosphere of carbon monoxide, aldehydes and ketones. The level of metabolism of prophyrin and nitrogen containing compounds as well as of fats and carbohydrates is higher during a combined effect of hypokinesia and moderate hyperoxia than during their separate influences.	[Effect of hyperoxia and hypokinesia on the formation and excretion of gaseous metabolic products in rats]. It has been shown experimentally that a 30-day exposure of white rats to hypokinesia and moderate hyperoxia decreases elimination of ammonia and increases the formation and release into an enclosed atmosphere of carbon monoxide, aldehydes and ketones. The level of metabolism of prophyrin and nitrogen containing compounds as well as of fats and carbohydrates is higher during a combined effect of hypokinesia and moderate hyperoxia than during their separate influences.	2,803
pubmed23n0001_1421	[Sorption method of water regeneration for cosmonaut personal hygiene].	The paper describes sanitary-hygienic and technological investigations aimed at development of the sorption method of water reclamation for personal hygiene needs of cosmonauts from wash water. Catamine-AB was used as a detergent with bactericidal properties. Manned experiments helped to identify the conditions that provided an adequate cleaning of skin and simultaneous sterilization of wash water. The technology of wash water purification was developed, proper sorbents were selected and recommended values of their use were established.	[Sorption method of water regeneration for cosmonaut personal hygiene]. The paper describes sanitary-hygienic and technological investigations aimed at development of the sorption method of water reclamation for personal hygiene needs of cosmonauts from wash water. Catamine-AB was used as a detergent with bactericidal properties. Manned experiments helped to identify the conditions that provided an adequate cleaning of skin and simultaneous sterilization of wash water. The technology of wash water purification was developed, proper sorbents were selected and recommended values of their use were established.	2,804
pubmed23n0001_1422	Plasma glucose in miniature swine infused with ethanol and fructose.	Hypoglycemia resulting from intragastric infusion of ethanol in miniature swine was counteracted by simultaneous infusion of fructose. The magnitude and time of peak plasma ethanol concentrations were functions of the quantity of ethanol or ethanol and fructose.	Plasma glucose in miniature swine infused with ethanol and fructose. Hypoglycemia resulting from intragastric infusion of ethanol in miniature swine was counteracted by simultaneous infusion of fructose. The magnitude and time of peak plasma ethanol concentrations were functions of the quantity of ethanol or ethanol and fructose.	2,808
pubmed23n0001_1423	[Effect of a magnetic field on Escherichia coli].	The decontaminating effect of the pulsing magnetic field on the E. coli infected reclaimed water was studied on two installations. The magnetic field intensity was 500 and 1000-1500 ersted and the microbial load was 1, 10 and 100 thous. microbial units per 1 ml. It was found that the magnetic treatment of water had a noticeable bactericidal effect. This indicated that the method can be used for decontamination of reclaimed water.	[Effect of a magnetic field on Escherichia coli]. The decontaminating effect of the pulsing magnetic field on the E. coli infected reclaimed water was studied on two installations. The magnetic field intensity was 500 and 1000-1500 ersted and the microbial load was 1, 10 and 100 thous. microbial units per 1 ml. It was found that the magnetic treatment of water had a noticeable bactericidal effect. This indicated that the method can be used for decontamination of reclaimed water.	2,806
pubmed23n0001_1424	Dietary caffeine and alcohol consumption by rats.	The alcohol consumption of malnourished rats increased slowly but substantially during a 4-week period in which caffeine was added to their marginally adequate diet. Consumption fell to precaffeine levels as soon as caffeine was withdrawn.	Dietary caffeine and alcohol consumption by rats. The alcohol consumption of malnourished rats increased slowly but substantially during a 4-week period in which caffeine was added to their marginally adequate diet. Consumption fell to precaffeine levels as soon as caffeine was withdrawn.	2,809
pubmed23n0001_1425	Effect of taurine on ethanol-induced sleeping time in mice.	The CNS-depressant effect of ethanol was markedly reduced in mice by simultaneous intraperitoneal injection of taurine.	Effect of taurine on ethanol-induced sleeping time in mice. The CNS-depressant effect of ethanol was markedly reduced in mice by simultaneous intraperitoneal injection of taurine.	2,810
pubmed23n0001_1426	[Urine conservation by surface-active agents].	The antibacterial activity of surface-active substances -- catamine-AB, catapine B-300, GIPH-200 and Tego-51 was measured on the E. coli and Staphylococcus aureus cultures and anthracoid spores. The purpose of the measurements was to explore the use of the substances as urine conserving agents. Catamine-AB showed the highest antibacterial activity. Anthracoid spores exhibited the highest resistance to the substances; staphylococci were less resistant than E. coli. Investigations of the effectiveness of urine conservation demonstrated that catamine-AB at a concentration of 0.1% killed all Staph. aureus and E. coli. Therefore, it can be recommended as a urine conserving agent.	[Urine conservation by surface-active agents]. The antibacterial activity of surface-active substances -- catamine-AB, catapine B-300, GIPH-200 and Tego-51 was measured on the E. coli and Staphylococcus aureus cultures and anthracoid spores. The purpose of the measurements was to explore the use of the substances as urine conserving agents. Catamine-AB showed the highest antibacterial activity. Anthracoid spores exhibited the highest resistance to the substances; staphylococci were less resistant than E. coli. Investigations of the effectiveness of urine conservation demonstrated that catamine-AB at a concentration of 0.1% killed all Staph. aureus and E. coli. Therefore, it can be recommended as a urine conserving agent.	2,807
pubmed23n0001_1427	Blood alcohol level discrimination by nonalcoholics. The role of internal and external cues.	Men were trained to estimate their blood alcohol levels, after drinks of different strengths, by means of internal or external cues or both. All groups improved in estimation accuracy but the type of training made no difference.	Blood alcohol level discrimination by nonalcoholics. The role of internal and external cues. Men were trained to estimate their blood alcohol levels, after drinks of different strengths, by means of internal or external cues or both. All groups improved in estimation accuracy but the type of training made no difference.	2,811
pubmed23n0001_1428	Alcohol and backward masking of visual information.	Alcohol increased the time necessary to transfer information from the initial sensory information storage system into the short-term memory system.	Alcohol and backward masking of visual information. Alcohol increased the time necessary to transfer information from the initial sensory information storage system into the short-term memory system.	2,812
pubmed23n0001_1429	Recovery of verbal short-term memory in alcoholics.	When given a short-term memory distractor test on the day after admission to the hospital in an intoxicated state, the performance of older alcoholic patients was significantly worse than that of younger alcoholics and on a par with that of alcoholic Korsakoff patients. One month later, however, the older patients' performance was comparable to that of the other alcoholics.	Recovery of verbal short-term memory in alcoholics. When given a short-term memory distractor test on the day after admission to the hospital in an intoxicated state, the performance of older alcoholic patients was significantly worse than that of younger alcoholics and on a par with that of alcoholic Korsakoff patients. One month later, however, the older patients' performance was comparable to that of the other alcoholics.	2,813
pubmed23n0001_1430	Group therapy and changes in the self-concept of alcoholics.	One group of alcoholics received closed-group encounter therapy, and another, open elective group therapy. The closed-group encounter therapy was superior in elevating self-concept.	Group therapy and changes in the self-concept of alcoholics. One group of alcoholics received closed-group encounter therapy, and another, open elective group therapy. The closed-group encounter therapy was superior in elevating self-concept.	2,814
pubmed23n0001_1431	Alcoholism, hopelessness and suicidal behavior.	A study of alcoholic and nonalcoholic suicide attempters indicated that hopelessness was the key determinant of suicidal intent in both groups.	Alcoholism, hopelessness and suicidal behavior. A study of alcoholic and nonalcoholic suicide attempters indicated that hopelessness was the key determinant of suicidal intent in both groups.	2,815
pubmed23n0001_1432	An application of anomy theory to the study of alcoholism.	In a study of 442 alcoholics, a positive relationship between the development of anomy and the development of alcoholism was found.	An application of anomy theory to the study of alcoholism. In a study of 442 alcoholics, a positive relationship between the development of anomy and the development of alcoholism was found.	2,816
pubmed23n0001_1433	Drinking behavior in laboratory and barroom settings.	Barroom patrons consumed their drinks in significantly less time and with fewer sips than subjects observed in a laboratory. The former most often drank beer while the latter preferred mixed drinks.	Drinking behavior in laboratory and barroom settings. Barroom patrons consumed their drinks in significantly less time and with fewer sips than subjects observed in a laboratory. The former most often drank beer while the latter preferred mixed drinks.	2,817
pubmed23n0001_1434	Effect of role empathy on human figures drawn by women alcoholics.	Drawings by women alcoholics of the self, a murderer, the murderer's victim and victim's parent revealed conscious and unconscious identification with the depicted roles.	Effect of role empathy on human figures drawn by women alcoholics. Drawings by women alcoholics of the self, a murderer, the murderer's victim and victim's parent revealed conscious and unconscious identification with the depicted roles.	2,818
pubmed23n0001_1435	The Cornell Medical Index as an adjunct to paraprofessional evaluation of alcohol addiction.	The Cornell Medical Index may prove a significant aid to paraprofessional personnel in recognizing alcoholics in need of medical attention.	The Cornell Medical Index as an adjunct to paraprofessional evaluation of alcohol addiction. The Cornell Medical Index may prove a significant aid to paraprofessional personnel in recognizing alcoholics in need of medical attention.	2,819
pubmed23n0001_1436	Surgical management of severe aortic coarctation and interrupted aortic arch in neonates.	Forty-four infants, 2 to 90 days of age, with severe obstructive lesions of the aortic arch, underwent emergency surgical correction between Jan. 1, 1966, and April 1, 1975. The typical clinical presentation was severe congestive heart failure and acidemia. Resection of an aortic coarctation with end-to-end anastomosis was performed in 31 patients. Eight (26 per cent) died after the operation. Since 1969, the mortality rate has been reduced to 14 per cent (3 of 22 patients) even though the incidence of major associated cardiac lesions has remained essentially constant (56 per cent from 1966 through 1969, 64 per cent from 1970 through March, 1975). This suggests that the higher survival rate has resulted from improved surgical techniques and postoperative care. The mortality rate in the infants operated upon during the second and third months of life was twice as high as that in those operated upon before the age of 1 month. Eight patients with Type A interrupted aortic arch were operated upon and 5 survived. Five patients with Type B aortic arch were operated upon and 3 survived.	Surgical management of severe aortic coarctation and interrupted aortic arch in neonates. Forty-four infants, 2 to 90 days of age, with severe obstructive lesions of the aortic arch, underwent emergency surgical correction between Jan. 1, 1966, and April 1, 1975. The typical clinical presentation was severe congestive heart failure and acidemia. Resection of an aortic coarctation with end-to-end anastomosis was performed in 31 patients. Eight (26 per cent) died after the operation. Since 1969, the mortality rate has been reduced to 14 per cent (3 of 22 patients) even though the incidence of major associated cardiac lesions has remained essentially constant (56 per cent from 1966 through 1969, 64 per cent from 1970 through March, 1975). This suggests that the higher survival rate has resulted from improved surgical techniques and postoperative care. The mortality rate in the infants operated upon during the second and third months of life was twice as high as that in those operated upon before the age of 1 month. Eight patients with Type A interrupted aortic arch were operated upon and 5 survived. Five patients with Type B aortic arch were operated upon and 3 survived.	2,820
pubmed23n0001_1437	Pharmacological analysis of the adrenergic control of the cerebral circulation.	The adrenergic control of the cerebral circulation was subjected to pharmacological analysis. The status of the cerebral circulation was assessed using radioisotope, electromagnetic and resistographic methods. EEG, ECG and arterial pressure were recorded. The acid-base equilibrium and oxygen tension were measured in the arterial blood and cerebrospinal fluid. The experiments showed that the sympathetic innervation plays an important role in controlling cerebral circulation and in the development of cerebrovascular disorders. This was indicated by the constriction of intracranial arteries induced by noradrenaline, stimulation of sympathetic nerves, reflex sympathetic activations and the effect of potassium chloride on the centrol nervous system. The pharmacological study demonstrated that constriction of the intracranial vessels is brought about by an activation of the sympatho-adrenal system which is mediated via alpha-adrenoreceptors of cerebral blood vessels.	Pharmacological analysis of the adrenergic control of the cerebral circulation. The adrenergic control of the cerebral circulation was subjected to pharmacological analysis. The status of the cerebral circulation was assessed using radioisotope, electromagnetic and resistographic methods. EEG, ECG and arterial pressure were recorded. The acid-base equilibrium and oxygen tension were measured in the arterial blood and cerebrospinal fluid. The experiments showed that the sympathetic innervation plays an important role in controlling cerebral circulation and in the development of cerebrovascular disorders. This was indicated by the constriction of intracranial arteries induced by noradrenaline, stimulation of sympathetic nerves, reflex sympathetic activations and the effect of potassium chloride on the centrol nervous system. The pharmacological study demonstrated that constriction of the intracranial vessels is brought about by an activation of the sympatho-adrenal system which is mediated via alpha-adrenoreceptors of cerebral blood vessels.	2,821
pubmed23n0001_1438	Cholesterol and fatty acid synthesis in swine.	In incubation studies with swine tissue slices, acetate-1-14C or glucose-U-14C as substrates were incorporated more readily into fatty acids and cholesterol in adipose tissue than other tissues tested. Cholesterol and fatty acid synthesizing acitivity was substantial in the small intestine. When acetate was available, liver, small intestine, and adipose tissue were important sites for cholesterol synthesis. Heart and aortic tissue had marginal levels of cholesterol synthesizing ability. Lipogenesis in adult swine liver, heart, and aortic tissue was extremely low. As in tissue slices, incorporation of acetyl-1-14C CoA into fatty acids by adipose homogenates indicated high lipogenic activity. Subcellular fractionations of heart and aortic tissue indicated that the heart microsomal fraction had the highest lipogenic activity as measured by the incroporation of acetyl-4-14C CoA into fatty acids. In adult swine adipose tissue, the incorporation of glucose-U-14C into fatty acid was higher than its incorporation into glyceride-glycerol. The synthesis of glyceride-glycerol from glucose-U-14C or acetate-1-14C in liver was higher than for fatty acid synthesis. The acitivity of acetyl CoA carboxylase, fatty acid synthetase, citrate cleavage enzyme, nicotinamide adenine dinucleotide phosphat-malate dehydrogenase, glucose-6-phosphate dehydrogenase, and 6-phosphogluconate dehydrogenase was considerably higher in adipose tissue than in other tissues tested, paralleling its high lipogenic capacity.	Cholesterol and fatty acid synthesis in swine. In incubation studies with swine tissue slices, acetate-1-14C or glucose-U-14C as substrates were incorporated more readily into fatty acids and cholesterol in adipose tissue than other tissues tested. Cholesterol and fatty acid synthesizing acitivity was substantial in the small intestine. When acetate was available, liver, small intestine, and adipose tissue were important sites for cholesterol synthesis. Heart and aortic tissue had marginal levels of cholesterol synthesizing ability. Lipogenesis in adult swine liver, heart, and aortic tissue was extremely low. As in tissue slices, incorporation of acetyl-1-14C CoA into fatty acids by adipose homogenates indicated high lipogenic activity. Subcellular fractionations of heart and aortic tissue indicated that the heart microsomal fraction had the highest lipogenic activity as measured by the incroporation of acetyl-4-14C CoA into fatty acids. In adult swine adipose tissue, the incorporation of glucose-U-14C into fatty acid was higher than its incorporation into glyceride-glycerol. The synthesis of glyceride-glycerol from glucose-U-14C or acetate-1-14C in liver was higher than for fatty acid synthesis. The acitivity of acetyl CoA carboxylase, fatty acid synthetase, citrate cleavage enzyme, nicotinamide adenine dinucleotide phosphat-malate dehydrogenase, glucose-6-phosphate dehydrogenase, and 6-phosphogluconate dehydrogenase was considerably higher in adipose tissue than in other tissues tested, paralleling its high lipogenic capacity.	2,832
pubmed23n0001_1439	Insulin receptors of skeletal muscle: specific insulin binding sites and demonstration of decreased numbers of sites in obese rats.	A membrane preparation was obtained from rat striated muscle. The preparation used has been shown to contain plasma membranes by electron microscopy as well as by enrichment in specific activity of both a plasma membrane enzyme "marker" (5'-nucleotidase) and cell surface 125I-incorporated radioactivity. The characteristics of 125I-insulin binding to this striated muscle preparation were studied, and it was found that 125I-insulin readily and specifically binds to this membrane preparation. The binding reaction was time, pH, and temperature dependent with optimal steady-state binding conditions occurring at 20 degrees C and at pH 7.6. Under these conditions (20 degrees C, pH 7.6) skeletal muscle plasma membranes displayed little ability to degrade insulin. Binding of 125I-insulin was readily inhibited at physiologic concentrations of unlabeled insulin and the specificity of this receptor for insulin was demonstrated by finding that high concentrations of glucagon, b-LH, b-FSH, p-PRL, hCG, TSH, and HGH were without effect on 125I-insulin binding and that insulin analogues inhibited binding in proportion to their biologic activity. When membranes from older, fatter rats were compared to membranes from younger, lean animals, 5'-nucleotidase specific activity and insulin degrading activity were found to be comparable. On the other hand, insulin binding to membrane receptors was decreased 30%-40% in the older, fatter animals. Thus, these studies indicate that (1) specific insulin receptors exist in skeletal muscle plasma membranes, and (2) membranes from older, fatter rats have fewer receptors than those from younger, lean animals.	Insulin receptors of skeletal muscle: specific insulin binding sites and demonstration of decreased numbers of sites in obese rats. A membrane preparation was obtained from rat striated muscle. The preparation used has been shown to contain plasma membranes by electron microscopy as well as by enrichment in specific activity of both a plasma membrane enzyme "marker" (5'-nucleotidase) and cell surface 125I-incorporated radioactivity. The characteristics of 125I-insulin binding to this striated muscle preparation were studied, and it was found that 125I-insulin readily and specifically binds to this membrane preparation. The binding reaction was time, pH, and temperature dependent with optimal steady-state binding conditions occurring at 20 degrees C and at pH 7.6. Under these conditions (20 degrees C, pH 7.6) skeletal muscle plasma membranes displayed little ability to degrade insulin. Binding of 125I-insulin was readily inhibited at physiologic concentrations of unlabeled insulin and the specificity of this receptor for insulin was demonstrated by finding that high concentrations of glucagon, b-LH, b-FSH, p-PRL, hCG, TSH, and HGH were without effect on 125I-insulin binding and that insulin analogues inhibited binding in proportion to their biologic activity. When membranes from older, fatter rats were compared to membranes from younger, lean animals, 5'-nucleotidase specific activity and insulin degrading activity were found to be comparable. On the other hand, insulin binding to membrane receptors was decreased 30%-40% in the older, fatter animals. Thus, these studies indicate that (1) specific insulin receptors exist in skeletal muscle plasma membranes, and (2) membranes from older, fatter rats have fewer receptors than those from younger, lean animals.	2,834