
eae. see. 508

eae. see. 508, jyala astradiol 17β-(1-(4-(aminosulphonyl) benzoil)-- prolin) asehi mhanatat, heey eka astrogen aahe jeey rajonivrutti samprerak upcharat aanee mahilanmadhye garbhadharana rokhanyasathi samprerak garbhanirodhak mhanoon ivastradvare vikasit kele jaat aahe. heey tondawate sakriy asalele istrogen ester aahe-visheshtah, naisargik aanee jaivavaichitryapurn istrogen istradiolache see17β sulphonamide-proline ester-aanee shariratil istradiolache utpadan mhanoon karya karate. tathapi, maukhik astradiol aanee astradiol vallet sarkhya paramparik maukhik astradiol esterchya ulat, eae. see. 508 madhye qamee kinwa pratham-paas chayapachay hote, tondawate jaivupalabdhata jaast asate aanee yakrutavar tyache istrogenic prabhav asman nasatat. tyamule, tyache maukhik astradiolpeksha, parenteral astradiolpramanech, parantu maukhik prashasanachya soyinusar, vividh prakarche vanchhaniy fayade aahet. eae. see. 508 haah eka assa umedvar aahe jyamadhye vaidyakeey vyavharat keval tondi astradiolach navhe tarr tondi garbhanirodhakanmadhye ethinilestradiol dekhil badalanyachi kshamata aahe. 2018 chya dusya timahit eae. see. 508 sathee naveen aushadh sthitee shodhanyacha ivastracha manas aahe.
yonimarg, transdermal aanee injection sarkhya astradiolchya parenteral marganchya sapeksh, maukhik astradiol qamee jaivupalabdhata aanee yakrut prathin sanshleshanavar asman parinam darshavate. estron aanee estron sulfate sarkhya astrogen sanyugmanmadhye pahilya-paas darmyan vyapak chayapachayamule, astradiol aanee astradiol vallet sarkhya paramparik astradiol esterchi maukhik jaivupalabdhata keval 5 takke aahe aanee astradiolchya patalit uchch aantar-vaiyaktik parivartansheelata prapt hote. shivay, first-pasmule, maukhik estradiolamule yakrutatil astradiolchi patali parisancharanatil patalipeksha 4 kinwa 5 putt jaast asate. parinami, maukhik astradiolche lipids, haemostatic ghatak, vaadh samprerak/insulinsarkhe vaadh ghatak 1 aksh prathine, angiotensinogen aanee itar prathinanchya yakrutachya utpadanavar istrogenic prabhav asman pramanat asato. heey pratikool aahe aanee parinami shiraparak thromboembolism, hriday v raktavahinyasambandhi ghatana aanee itar pratikool parinamancha dhoka vadhu shakato.
eae. see. 508 chya pharmacokineticsche moolyankan undaranmadhye karnyat aale; tyachi jaivupalabdhata purn (100%) asalyache aadhalun aale, raktatil tyachi clearance qamee hotee aanee tyache jaivik ardhayushya sumare 5 tasanvar lamble hote. undaranmadhye 5 mii. gra./kilo eae. see. 508 chya eka tondawate dilelya matremule astradiolchi patali 6,104 enji/miilii (6,104,000 piji/miilii) itaki uchch jhaali. eae. see. 508 neey swatah astrogen receptorcha agonist mhanoon kharab kriyakalap darshavila, astradiolasathi 2.3 nmchya tulanet 432 nmche moolya (188 putt farak), heey soochit karate qee sanyugchi astrogenic kriyakalap keval astradiolmadhye hydrolysismule aahe. eae. see. 508 madhye tondawate istrogenic shakti khoop jaast disun aalee, jee undaranmadhye istradiolchya sumare 100 putt aanee ethinilestradiolchya 10 putt hotee. heey andashayatil undaranmadhil garbhashayprabhavi prabhavadvare nirdharit kele gele; 10 microgram/divasachya tondawate dilelya matremule garbhashayache vajan eae. see. 508 saha duppat jhaale, tarr astradiols konatahi parinam disun aala nahee aanee garbhashayachya vajanavar keval eka lahan parinam ethinilestradiolne mojala gela. yaulat, moolyamapan kelelya dosemadhye, tondawate astradiol aanee ethinilestradiolche collesterol aanee angiotensinogenchya patalivar lakshaniy parinam disun aale, tarr tondawate eae. see. 508 aanee parenteral astradiolcha yaa yakrutachya prathinanvar ajibat parinam disun aala nahee. heey nishkarsh yaa kalpanenusar aahet qee maukhik eae. see. 508, maukhik astradiol aanee ethinilestradiolchya ulat parantu parenteral astradiolpramanech, first-paas chayapachay aanee yakrutala bipass karate.
first-paas chayapachay nasane aanee eae. see. 508 saha asman yakrutachya samparkat naan yene heey eae. see. 508 chya sulphonamide bhagache carbonic enhydress II (kaee) navachya enzymeshee ulat karata yenyajoge bandhan asalyamule asalyache manale jaate. eae. see. 508 110 nmchya bandhan pratibandhasah manvi kaisathi madhyam aakarshan darshavite. kaiee heey erythrocytesmadhye (laal rakt peshi) jaast pramanat kendrit asate, jeey yakrutachya portal venchya raktat mothya pramanat asatat. asey manale jaate qee aatadyanmadhye tyache shoshan jhalyanantar aanee yakrut portal nasanmadhye pravesh kelyanantar, eae. see. 508 erythrocytesdware ghetale jaate aanee mothya pramanat jamaa hote, jyamule teey yakrutat pravesh karnyapasoon rokhate aanee parinami erythrocytesdware thet parisancharanat vahoon nele jaate. parisanchari erythrocytespasoon, eae. see. 508 haloohaloo sodale jaate aanee nantar astradiolmadhye hydrolyse kele jaate asey manale jaate. tathapi, eae. see. 508shhee sambandhit astradiolchya eka sulphonamide estermadhye, jyala eae. see. 518 mhanoon olakhale jaate, kaishi bandhaniche samaan gunadharm khoop qamee kinwa anupasthit asalyache disun aale aanee tyamule kadachit erythrocyte bandhanicha abhav aahe, jyamule asha gunadharmansathi kaii bindingchi aavashyakta aanee jyaa yantranedvare teey udbhavtat tyabaddal prashna upasthit hotat. 
astradiol sulfamate (eae2mett) heey astradiolche see3 sulfamate ester aahe jeey 1990 chya dashakat vikasit kele gele hote aanee eae. see. 508 chey purvavarti hote. teey kaishi bandhale jaate, erythrocytesmadhye ghetale jaate aanee sathavale jaate aanee eae. see. 508 sarkhech gunadharm darshavate. parinami, eae2mett tondawate istrogen mhanoon sambhavya vaidyakeey vaparasathi vikasit kele jaat hote. tathapi, hyamule astradiolchya patalit konatihi vaadh jhaleli nahee aanee manvi chikitsalayin chachanyanmadhye astrogenic parinam disun aale naheet. asey disate qee undeer aanee narvanar yanchyat eae2metchya prajatinmadhye farak aahe aanee manavanmadhye kriyakalapancha abhav aahe kaaran eae2mett atiriktapane steroid sulfatscha atyant shaktishali avarodhak mhanoon karya karato. heey enzyme sulfur-aadharit astradiol ester jase qee eae2mett aanee eae. see. 508 chya astradiolmadhye jalvichhedanasathi jababdar aahe. steroid sulphatage rokhoon, eae2mett astradiolmadhye swatache sakriyakaran rokhate, jeey tyachi astrogenic kriya prabhavipane radd karate. yavyatirikt, asey aadhalun aale qee erythrocytesmadhye eae2metche estron sulfamatemadhye (emate) mothya pramanat rupantar jhaale hote, jyamule astradiolmadhye sakriy honyachi tyachi kshamata aanakhi badhit jhaali asavi. eae2metchya ulat, eae. see. 508 haah steroid sulphatage avarodhak manla jaat nahee aanee sambandhit estron samatulyamadhye rupantarit keela jaau shakat nahee.
eae. see. 586 mhanoon olakhale jaanare see. 17β sulphonamide-proline testosterone ester, jyache gunadharm eae. see. 508 sarkhech aahet, heey dekhil ivastradvare vikasit kele jaat aahe, visheshtah purushanmadhye androgen replacement therapimadhye vaparnyasathi androgen aanee shaktishali maukhik testosterone prodrug mhanoon.