Pregabalin

Sharax Gaaban:

Magaca API Tilmaam Faahfaahinta US DMF  EU DMF  CEP
Pregabalin Suuxdinta / Neuralgia Guriga gudihiisa / EP 22223 CEP2016-141

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Pregabalin maahan GABAA ama GABAB agonist reseptor.
Pregabalin waa gabapentinoid wuxuuna ku dhaqmaa isagoo xakameynaya kanaalada kalsiyumka qaarkood. Gaar ahaan waa isku xirka aaladda 'ili2δ subunit subunit' ee kanaallada kalsiyum ee ku tiirsan danabyada qaarkood (VDCCs), oo markaa waxay u dhaqmeysaa sidii ka-hortagga α2δ subunit-ku jira VDCCs. Waxaa jira laba qaybood oo daroogada ku xidha α2δ, α2δ-1 iyo α2δ-2, pregabalin-na waxay muujisaa isku xirnaan (iyo sidaa darteed xulasho la’aan udhaxeysa) labadan goobood. Pregabalin waa mid xul ah ku xirnaanta α2δ VDCC. In kasta oo xaqiiqda ah in pregabalin ay tahay analogga GABA, kuma xirna dhakhaatiirta GABA, uma beddelayo GABA ama agonist soo-dhawre GABA ah oo ku nool vivo, oo si toos ah uma beddelayso gaadiidka GABA ama dheef-shiid kiimikaadka Si kastaba ha noqotee, pregabalin waxaa lagu ogaadey inay soo saareyso koror ku tiirsan qiyaasta muujinta maskaxda ee L-glutamic acid decarboxylase (GAD), enzyme-ka mas'uulka ka ah soo saarista GABA, sidaa awgeedna waxaa laga yaabaa inay saameyn xoog leh ku yeelato GABAergic iyadoo kordhinaysa heerarka GABA ee maskaxda. Xilligan ma jirto wax caddayn ah in saameynta pregabalin ay dhexdhexaadinayso qaab kasta oo aan ahayn ka-hortagga α2δ-ku jira VDCCs. Iyadoo la raacayo, joojinta α2α-1-ay kujirto VDCCs ee pregabalin ayaa umuuqata inay mas'uul ka tahay saameynteeda daawada 'anticonvulsant', 'analgesic', iyo anxiolytic.
Dhiigga α-amino acids L-leucine iyo L-isoleucine, oo si aad ah ugu eg pregabalin iyo gabapentinoids kale ee qaabdhismeedka kiimikada, ayaa ah isku xirnaanta apparent2δ VDCC oo leh xiriir la mid ah sida gabapentinoids (tusaale, IC50 = 71 nM ee L- isoleucine), oo waxay kujiraan dareeraha maskaxda ee bini'aadamka ee iskuxirka micromolar (tusaale, 12.9 μM ee L-leucine, 4.8 μM L-isoleucine). Waxaa loo qoondeeyay inay noqon karaan xididada hidde-wadayaasha ee subunit-ka iyo inay si tartiib tartiib ah uga soo horjeedaan saameynta gabapentinoids. Si waafaqsan, halka gabapentinoids sida pregabalin iyo gabapentin ay leeyihiin isku xirnaansho nanomolar ah oo loo yaqaan ',2δ subunit', awoodooda in vivo ay kujiraan heerarka hooseeya ee 'micromolar', iyo tartanka ku xirnaanshaha endogenous L-amino acids ayaa la sheegay inay u badan tahay inuu mas'uul ka yahay khilaafkan.

Pregabalin waxaa lagu ogaadey inuu leeyahay 6-laab isku xirnaansho ka sareysa gabapentin α2α subunit-ku jira VDCCs hal daraasad. Si kastaba ha noqotee, daraasad kale ayaa lagu ogaaday in pregabalin iyo gabapentin ay leeyihiin isku mid ah iskucelceliska bini'aadamka ee '2δ-1 subunit (Ki = 32 nM iyo 40 nM, siday u kala horreeyaan). Si kastaba xaalku ha ahaadee, pregabalin waxay 2 ilaa 4 jeer ka awood badan tahay gabapentin sida xanuunka oo kale, xayawaanaadka, waxay umuuqataa inay 3 ilaa 10 jeer ka xoog badan yihiin gabapentin oo loo yaqaan 'anticonvulsant'.

SHAHAADO

2018 GMP-2
原料药GMP证书201811(captopril ,thalidomide etc)
GMP-of-PMDA-in-Chanyoo-平成28年08月03日 Nantong-Chanyoo-Pharmatech-Co
FDA-EIR-Letter-201901

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