
receptor virodhi

ack receptor virodhi ack prakaar kaa receptor ligand yaa dawa haye joe ack receptor koo agonist kii tarah sakriya karane key bajaay usey bandhkar aur avaruddh karke javic pratikriya koo avaruddh yaa cumm kartaa haye. virodhi davaayen receptor protein key praakritik sanchaalan mein hastakshep karati hain. unhein kabhi-kabhi avarodhak kahaa jaataa haye; udaharanon mein alfa avarodhak, beeta avarodhak aur calcium channel avarodhak shamil hain. pharmacology mein, virodhi key paas aatmiyata hoti haye lekin unake sangyanatmak receptors key liye koee prabhavkarita naheen hoti haye, aur bandhan antahkriya koo baadhit karega aur receptors parr ack agonist yaa inverse agonist key kaary koo roque dega. virodhi sakriya sthal yaa receptor parr allosteric site koo bandhkar apane prabhaavon kii madhyasthata karate hain, yaa way advitiya bandhan sthalon parr baatchit curr sakate hain joe aamtaur parr receptor kii gatividhi key javic viniyaman mein shamil naheen hotey hain. virodhi gatividhi virodhi-grahankarta parisar kii deerghaayu key aadhar parr prativarti yaa aparivartaniya hoe sakati haye, joe badale mein, virodhi-grahankarta bandhan kii prakriti parr nirbhar karati haye. adhikansh dawa virodhi receptors parr sanrachanaatmak roop seey paribhaashit bandhan sthalon parr antarjanit ligand yaa substrate key saath pratispardha karke apani shakti praapt karate hain.
vyutpatti.
aushadhiya shabdon mein angreji shabd virodhi yunani shabd ἀνταγωνιστις seey aataa haye-"virodhi", "pratidvandi, pratiyogi, khalnayak, dushman", joe "virodhi" ("khilaf") aur "agonizesthai" ("puraskar key liye pratispardha karna") seey liya gayaa haye. 20veen shatabdi mein americi jeevvigyaani bellie adgren dwara virodhi kii khoj kii gaee thee.
receptors.
jaiv rasayanik receptors badey protein anu hotey hain jinhen harmon yaa dawa jaise ligand key bandhan dwara sakriya kiya jaa sakata haye. receptors jhilli-baddh hoe sakate hain, koshika satah receptors key roop mein, yaa koshika key ander intracellular receptors key roop mein, jaise kii paramanu receptors jaise kii mitochondrian key. receptor aur usake ligand key beach gair-sahsanyojak baatchit key parinamswarup bandhan hotaa haye, receptor parr bandhan sthal naamak sthaanon parr. ack receptor mein vibhinn ligand key liye ack yaa adhik bandhan sthal hoe sakate hain. receptor parr sakriya site parr bandhan seedhe receptor sakriyan koo niyantrit kartaa haye. receptors kii gatividhi koo receptor parr anya saiton parr ligand key bandhan dwara bhee niyantrit kiya jaa sakata haye, jaisa kii allosteric bandhan saiton mein hotaa haye. virodhi agonist-prerit pratikriyaon koo rokkar receptor baatchit key madhyam seey apane prabhaavon kii madhyasthata karate hain. yeh sakriya sthal yaa allosteric sthal key saath judkar puuraa kiya jaa sakata haye. isake alawa, virodhi apane prabhaavon koo lagu karane key liye receptor kii gatividhi key javic viniyaman mein shamil naheen honey vaale advitiya bandhan sthalon parr baatchit curr sakate hain.
virodhi" shabd mool roop seey dawa prabhaavon key vibhinn profile kaa varnan karane key liye gadhaa gayaa thaa. receptor antignist kii jaiv rasayanik paribhasha 1950 key dashak mein erines aur stephenson dwara pesh kii gaee thee. receptor virodhi kii vartamaan sweekrit paribhasha receptor occupancy model parr adharit haye. yeh ack hii receptor mein kewal una yaugikon parr vichaar karane key liye virodh kii paribhasha koo sankuchit kartaa haye joe virodhi gatividhiyon key saath hain. agonists koo receptor koo bandhkar ack ekal cellular pratikriya koo "chaalu" karane key liye socha gayaa thaa, iss prakaar ack koshika key bheetar parivartan key liye ack jaiv rasayanik tantra shuru kiya gayaa thaa. virodhi koo agonist seey receptor koo 'avaruddh' karke usa pratikriya koo 'bund' karane key liye socha gayaa thaa. yeh paribhasha shaaririk virodhi padarthon key liye bhee upayog mein haye, joe shaaririk karyon kaa virodh karate hain, lekin vibhinn receptors parr kaary karate hain. udaaharan key liye, histamine aich1 receptor parr vasodilation key madhyam seey dhamani key dabaav koo cumm kartaa haye, jabaki adrenaline alfa-adrenergic receptor sakriyan dwara madhyasthata kiye gaye vassoconstion key madhyam seey dhamani key dabaav koo badhaata haye.
dawa-prerit receptor sakriyan aur receptor siddhant key tantra kii hamari samajh aur receptor virodhi kii jaiv rasayanik paribhasha vikasit hoti rahati haye. receptor sakriyan key dou-raajya model ney madhyavarti anuroop avasthaon key saath bahu-raajya model koo raasta diyaa haye. karyatmak chayanaatmaktaa kii khoj aur ligand-vishisht receptor anuroopan hotey hain aur vibhinn dusare sandeshvaahak pranaliyon key saath receptors kii baatchit koo prabhaavit curr sakate hain, iska matlab yeh hoe sakata haye kii davaaon koo receptor key kuchh downstream karyon koo sakriya karane key liye design kiya jaa sakata haye, lekin anya naheen. iska matlab haye kii prabhavkarita vaastav mein iss baat parr nirbhar curr sakati haye kii receptor kahaan vyakt kiya jaataa haye, iss drishtikon koo badalate hue kii receptor parr prabhavkarita ack dawa kii receptor-swatantra sampatti haye.
pharmacodynamics.
prabhavkarita aur shakti.
paribhasha key anusaar, virodhi una receptors koo sakriya karane key liye koee prabhavkarita pradarshit naheen karate hain jinhen way baandhate hain. virodhi ack receptor koo sakriya karane kii kshamata koo banaae naheen rakhate hain. ack baar baadhya honey key baad, halanki, virodhi agonist, vyutkram agonist aur aanshik agonist key kaary koo rokte hain. karyatmak virodhi parakh mein, ack khuraak-pratikriya vakr ack agonist kii gatividhi koo ulatane key liye virodhi kii sandrata kii ack shrinkhala kii kshamata key prabhaav koo maapata haye. ack virodhi kii shakti koo aamtaur parr isaki "ardh adhikatam avarodhak ekagrata" (i.ee., aaee. see. 50 maan). ack agonist kii adhikatam javic pratikriya key aadhe avrodh koo praapt karane key liye aavashyak virodhi kii ekagrata kaa nirdhaaran karke ack diye gaye virodhi key liye isaki ganana kii jaa sakati haye. samaan prabhavsheelta key saath davaaon kii shakti kii tulanaa karane key liye ack aaee. see. 50 moolya koo spasht karna upayogi haye, haalaanki donon dawa virodhi dwara utpaadit khuraak-pratikriya vakr samaan honey chaahiye. aaee. see. 50 jitna cumm hoga, virodhi kii shakti utani hii adhik hogi, aur adhikatam javic pratikriya koo rokane key liye aavashyak dawa kii ekagrata utani hii cumm hogi. davaaon kii cumm sandrata cumm dushprabhavon seey judee hoe sakati haye.
aatmiyata.
ack virodhi kii apani bandhan sthal (kii) key liye aatmiyata, i.ee. ack receptor koo baandhane kii isaki kshamata, agonist gatividhi key avrodh kii avadhi nirdhaarit karegi. ack virodhi kii aatmiyata koo praayogik roop seey shilled pratigaman kaa upayog karke yaa radiolegand binding adhyayanon mein pratispardhi virodhi key liye cheng-prusoff sameekaran kaa upayog karke nirdhaarit kiya jaa sakata haye. shilled regression kaa upayog pratidvandvita kii prakriti koo nirdhaarit karane key liye kiya jaa sakata haye kyonki shuruat yaa tou pratispardhi yaa gair-pratispardhi haye aur kii nirdhaaran upayog kiye jaane vaale agonist kii aatmiyata, prabhavkarita yaa ekagrata seey swatantra haye. haalaanki, yeh mahatvapurna haye kii santulan praapt hoe gayaa haye. santulan taka pahunchane parr receptor desensitization key prabhaavon koo bhee dhyaan mein rakhaa jaanaa chaahiye. dou yaa dou seey adhik prabhaavon koo pradarshit karane vaale virodhi key sambandh sthiraank, jaise kii pratispardhi tantrika-snaayu-avarodhak agents mein joe aayan chainalon koo avaruddh karate hain aur saath hii saath virodhi agonist binding kaa bhee, shilled pratigaman kaa upayog karke vishleshan naheen kiya jaa sakata haye. shilled pratigaman mein khuraak anupaat mein parivartan kii tulanaa karna shamil haye, ack khuraak pratikriya vakr parr nirdhaarit ack pratispardhi virodhi kii upasthiti mein akele ack agonist key ee. see. 50 key anupaat kii tulanaa mein. parakh mein upayog kiye jaane vaale virodhi kii matra mein badalaav khuraak anupaat koo badal sakata haye. shilled pratigaman mein, ack bhukhand logg (khuraak anupaat-1) banaam virodhi sandrata kii ack seema key liye virodhi kii logg sandrata seey banaa hotaa haye. aatmiyata yaa kii vaha jagah haye jahan rekha pratigaman bhukhand parr aiks-aksh koo kaatati haye. jabaki, shilled pratigaman key saath, virodhi ekagrata cheng-prusoff sameekaran seey kii moolyon koo praapt karane key liye upayog kiye jaane vaale prayogon mein vividh haye, agonist sandrata vividh hain. pratispardhi agonist aur virodhi key liye aatmiyata aaee. see. 50 mein badalaav seey kii (ack virodhi key liye aatmiyata sthiraank) kii ganana karane key liye upayog kiye jaane vaale cheng-prusoff kaarak seey sambandhit haye joe pratispardhi avrodh key dauran hotaa haye. cheng-prusoff kaarak pratispardhi virodhi dwara utpaadit avrodh parr receptor key liye agonist ekagrata aur agonist aatmiyata mein parivartan key prabhaav koo dhyaan mein rakhta haye.
prakaar.
pratispardhi.
pratispardhi virodhi antajanan ligand yaa agonist key roop mein usee bandhan sthal (sakriya sthal) parr receptors seey judate hain, lekin receptor koo sakriya kiye binaa. agonist aur virodhi receptor parr ack hii bandhan sthal key liye "pratispardha" karate hain. ack baar bandhe jaane key baad, ack virodhi agonist binding koo avaruddh curr dega. ack virodhi kii paryaapt sandrata badhyakari sthalon seey agonist koo visthaapit karegi, jisake parinamswarup receptor sakriyan kii cumm aavritti hogi. receptor kii gatividhi kaa star site key liye pratyek anu kii saapeksh aatmiyata aur unaki saapeksh sandrata dwara nirdhaarit kiya jaayega. ack pratispardhi agonist kii uchch sandrata receptors key anupaat koo badhaa degi joe agonist kaa kabja haye, virodhi kii uchch sandrata koo badhyakari site adhibhog kii samaan degree praapt karane key liye aavashyak hoga. pratispardhi virodhi kaa upayog karke karyatmak parakh mein, adhikatam pratikriya mein koee parivartan naheen honey key saath agonist khuraak-pratikriya vakron kaa ack samanantar daaeen or badalaav dekhaa jaataa haye.
pratispardhi virodhi kaa upayog davaaon kii gatividhi koo rokane key liye kiya jaataa haye, aur una davaaon key prabhaavon koo ulatane key liye kiya jaataa haye joe pahale seey hii sevan kii jaa chuki hain. nyloxone (jise narcan key roop mein bhee jaanaa jaataa haye) kaa upayog heroin yaa morphin jaisi davaaon key kaaran honey vaale opioid overdose koo ulatane key liye kiya jaataa haye. isi tarah, aar. oh. 15-4513 sharaab kaa ack pratijaivik haye aur flumazenil benzodiazepine kaa ack pratijaivik haye.
pratispardhi pratidvandiyon koo prativarti ("adhigamit") yaa aparivartaniya ("durgam") pratispardhi pratidvandiyon key roop mein upa-vargeekrit kiya jaataa haye, joe iss baat parr nirbhar kartaa haye kii way apane receptor protein lakshyon key saath kaise baatchit karate hain. prativarti virodhi, joe gair-sahsanyojak antar-aanvik balon key madhyam seey baandhate hain, antatah receptor seey alag hoe jaayenge, jisase receptor phir seey bandha hoga. aparivartaniya virodhi sahsanyojak antar-aanvik balon key madhyam seey baandhate hain. kyonki sthaaniya vatavaran mein sahsanyojak bandhanon koo todane key liye paryaapt mukt oorjaa naheen haye, isaliye bandhan anivarya roop seey "sthaayi" haye, jiska arth haye kii receptor-virodhi parisar kabhi alag naheen hoga. iss prakaar receptor sthaayi roop seey taba taka virodhi rahega jaba taka kii yeh sarvavyaapi naheen hoe jaataa aur iss prakaar nasht hoe jaataa haye.
gair-pratispardhi.
ack gair-pratispardhi virodhi ack prakaar kaa durgam virodhi haye joe dou tarikon mein seey ack mein kaary curr sakata haih receptor key ack allosteric site seey baadhya hocker, yaa receptor key sakriya site seey aparivartaniya roop seey baadhya karke. poorv arth koo ifer dwara maankeekrit kiya gayaa haye, aur yeh virodhi koo "allosteric virodhi" kahey jaane key barabar haye. jabaki inn donon ghatnaaon mein virodh kaa tantra alag-alag haye, donon koo "gair-pratispardhi" kahaa jaataa haye kyonki pratyek key antim parinam karyatmak roop seey bahut samaan hotey hain. pratispardhi virodhi key vipareet, joe ack adhikatam pratikriya praapt karane key liye aavashyak agonist kii matra koo prabhaavit kartaa haye, lekin usa adhikatam pratikriya key parimaan koo prabhaavit naheen kartaa haye, gair-pratispardhi virodhi adhikatam pratikriya key parimaan koo cumm karate hain joe kissy bhee matra mein agonist dwara praapt kiya jaa sakata haye. yeh sampatti unhein "gair-pratispardhi" naam arjit karati haye kyonki unake prabhaavon koo nakaar naheen jaa sakata haye, chaahe kitna bhee agonist maujood hoe. gair-pratispardhi virodhi key karyatmak parikshanon mein, agonist khuraak-pratikriya vakron kii adhikatam pratikriya kaa avasaad, aur kuchh mamalon mein, daaeen or kii paali, utpann hoti haye. dahini or kii shift ack receptor reserve (jise spare receptors key roop mein bhee jaanaa jaataa haye) key parinamswarup hogi aur agonist pratikriya kaa avrodh kewal tabhi hoga jaba yeh reserve samaapt hoe jaayega.
ack virodhi joe ack receptor key sakriya sthal seey judataa haye, usey "gair-pratispardhi" kahaa jaataa haye yadi sakriya sthal aur virodhi key beach kaa bandhan aparivartaniya yaa lagbhag aisaa hii haye. gair-pratispardhi" shabd kaa yeh upayog aadarsh naheen hoe sakata haye, halanki, kyonki "aparivartaniya pratispardhi virodh" shabd kaa upayog neeche charcha kiye gaye "gair-pratispardhi virodh" key dusare arth key saath bhram kii kshamata key binaa usee ghatana kaa varnan karane key liye bhee kiya jaa sakata haye.
gair-pratispardhi virodhi" kaa doosara roop ack allosteric site parr kaary kartaa haye. yeye virodhi agonist seey ack alag bandhan sthal seey judate hain, anya bandhan sthal key madhyam seey usa receptor parr apani kaarravaai karate hain. way sakriya sthal parr bandhan key liye agonist key saath pratispardha naheen karate hain. baadhya virodhi agonist key bandhan key baad receptor sakriyan key liye aavashyak receptor mein anuroop parivartanon koo roque sakate hain. cyclothiazide koo emglur1 receptor key prativarti gair-pratispardhi virodhi key roop mein kaary karane key liye dikhaaya gayaa haye.
apratispardhi.
gair-pratispardhi virodhi gair-pratispardhi virodhi seey alag hotey hain kyonki unhein ack alag allosteric binding site seey judane seey pahale ack agonist dwara receptor sakriyan kii aavashyakta hoti haye. iss prakaar kaa virodh ack gatij profile kaa utpaadan kartaa haye jisamen "virodhi kii samaan matra agonist kii cumm sandrata kii tulanaa mein agonist kii uchch sandrata koo behtar tareeke seey avaruddh karati haye. alzheimer roga key upchaar mein upayog kiya jaane vaalaa maymentine, aine. aim. dee. aeye. receptor kaa ack apratispardhi virodhi haye.
mook virodhi.
mook virodhi pratispardhi receptor virodhi hotey hain jinamen receptor koo sakriya karane key liye shoonya aantarik gatividhi hoti haye. way sachche virodhi hain, isaliye bolane key liye. yeh shabd poori tarah seey nishkriya virodhi koo kamjor aanshik agonist yaa vyutkram agonist seey alag karane key liye banaaya gayaa thaa.
aanshik agonist.
aanshik agonist koo una davaaon key roop mein paribhaashit kiya jaataa haye joe, ack diye gaye receptor parr, karyatmak pratikriya key ayam mein bhinn hoe sakate hain joe way adhikatam receptor adhibhog key baad praapt karate hain. haalaanki way agonist hain, aanshik agonist ack poorna agonist kii upasthiti mein ack pratispardhi virodhi key roop mein kaary curr sakate hain, kyonki yeh receptor adhibhog key liye poorna agonist key saath pratispardha kartaa haye, jisase kewal poorna agonist key saath dekhi gaee tulanaa mein receptor sakriyan mein shuddh kamee aatee haye. chikitsakiya roop seey, unaki upayogita ack saath atyadhik gatividhi koo avaruddh karate hue cumm pranali koo badhaane kii unaki kshamata seey praapt hoti haye. ack receptor koo ack uchch star key aanshik agonist key sampark mein laane seey yeh sunishchit hoga kii isaki gatividhi kaa ack nirantar, kamjor star haye, chaahe uska samanya agonist uchch yaa nimn star parr maujood hoe. isake alawa, yeh sujhaav diyaa gayaa haye kii aanshik agonism anukulansheel niyaamak tantra koo rokta haye joe shaktishali poorna agonist yaa virodhi key baar-baar sampark mein aaney key baad aksar vikasit hotaa haye. ee.jee. buprenorphin, joe kii ack aanshik agonist haye, kamjor morphin jaisi gatividhi key saath judataa haye aur dard prabandhan mein ack analgesic key roop mein aur opioid nirbharta key upchaar mein methadone key vikalp key roop mein chikitsakiya roop seey upayog kiya jaataa haye.
vyutkram agonist.
ack vyutkram agonist kaa prabhaav ack virodhi key samaan hoe sakata haye, lekin yeh neeche kii or javic pratikriyaon key ack alag samooh kaa kaaran banata haye. aantarik yaa besal gatividhi pradarshit karane vaale rachanaatmak roop seey sakriya receptors mein vyutkram agonist hoe sakate hain, joe naa kewal ack shaastriya virodhi kii tarah badhyakari agonist key prabhaavon koo avaruddh karate hain, balki receptor kii besal gatividhi koo bhee rokte hain. pahale virodhi key roop mein vargeekrit kaee davaaon koo abb rachanaatmak sakriya receptors kii khoj key kaaran vyutkram agonist key roop mein punah vargeekrit kiya jaanaa shuru hoe gayaa haye. histamine virodhi, jinhen mool roop seey histamine aich1 receptors key virodhi key roop mein vargeekrit kiya gayaa haye, koo vyutkram agonist key roop mein punah vargeekrit kiya gayaa haye.
prativartita.
kaee virodhi prativarti virodhi hotey hain joe adhikansh agonists kii tarah, receptor-ligand kinetics dwara nirdhaarit daron parr ack receptor koo baandhenge aur baandhenge.
aparivartaniya virodhi sahsanyojak roop seey receptor lakshya seey judate hain aur samanya roop seey, unhein hataaya naheen jaa sakata haye; virodhi prabhaavon kii avadhi key liye receptor koo nishkriya karna receptor turnover kii darr, nae receptors key sanshleshan kii darr seey nirdhaarit kiya jaataa haye. phenoxybenzamine ack aparivartaniya alfa blocker kaa ack udaaharan haye-yeh sthaayi roop seey adrenergic receptors seey judataa haye, adrenaline aur noradrenaline koo bandhan seey rokta haye. receptors key nishkriya honey key parinamswarup aam taur parr agonist khuraak-pratikriya vakr kii adhikatam pratikriya kaa avasaad hotaa haye aur vakr mein ack sahee badalaav hotaa haye jahaan gair-pratispardhi virodhi key samaan ack receptor reserve hotaa haye. parakh mein ack dhone kaa kadam aamtaur parr gair-pratispardhi aur aparivartaniya virodhi davaaon key beach antar karega, kyonki gair-pratispardhi virodhi key prabhaav prativarti hotey hain aur agonist kii gatividhi koo bahaal kiya jaayega.
aparivartaniya pratispardhi pratidvandiyon mein receptor key agonist aur virodhi key beach pratispardha bhee shamil hoti haye, lekin sahsanyojak bandhan kii darr alag hoti haye aur virodhi kii aatmiyata aur pratikriyashilta parr nirbhar karati haye. kuchh virodhi key liye, ack alag avadhi hoe sakati haye jisake dauran way pratispardhi roop seey vyavhaar karate hain (besal prabhavkarita kii parwah kiye binaa), aur receptor-ligand kinetics dwara nirdhaarit receptor seey swatantra roop seey judate hain aur alag hoe jaate hain. lekin, ack baar aparivartaniya bandhan honey key baad, receptor nishkriya hoe jaataa haye aur kharaab hoe jaataa haye. aparivartaniya pratispardhi davaaon key saath karyatmak parakh mein gair-pratispardhi pratidvandiyon aur aparivartaniya pratidvandiyon key liye, logg ekagrata-prabhaav vakr mein daaeen or badalaav hoe sakata haye, lekin, samanya roop seey, dhalaan mein kamee aur adhikatam mein kamee donon praapt kii jaati hain.

