Pregabalin

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Pregabalin Qaug dab peg / Neuralgia Hauv Tsev / EP 22223 CEP2016-141

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KHOOM NTES

Pregabalin tsis yog GABAA lossis GABAB receptor agonist.
Pregabalin yog gabapentinoid thiab ua los ntawm inhibiting qee cov calcium calcium. Tshwj xeeb nws yog ligand ntawm qhov chaw pabcuam α2δ subunit qhov chaw ntawm qee qhov hluav taws xob-calcium calcium raws (VDCCs), thiab yog li ua cov tshuaj tiv thaiv ntawm α2δ subunit-muaj VDCCs. Muaj ob qho yeeb tshuaj-khi α2δ subunits, α2δ-1 thiab α2δ-2, thiab pregabalin qhia qhov sib thooj zoo sib xws rau (thiab vim li no tsis muaj qhov xaiv ntau ntawm) ob qho chaw no. Pregabalin yog qhov xaiv nyob rau hauv nws khi rau α2δ VDCC qhov haujlwm me. Txawm hais tias pregabalin yog GABA analogue, nws tsis khi rau GABA cov txais, tsis hloov mus rau GABA lossis lwm GABA receptor agonist hauv vivo, thiab tsis ncaj qha kev hloov GABA kev thauj lossis metabolism. Txawm li cas los xij, pregabalin tau pom los tsim cov koob tshuaj nce qib hauv lub hlwb qhia ntawm L-glutamic acid decarboxylase (GAD), lub enzyme lub luag haujlwm rau synthesizing GABA, thiab yog li tej zaum yuav muaj qee qhov tsis ncaj GABAergic los ntawm qhov nce GABA ntau ntau hauv lub hlwb. Tam sim no tsis muaj pov thawj pom tias cov teebmeem ntawm pregabalin yog kho kom haum xeeb los ntawm ib qho txheej txheem uas tsis yog kev txwv ntawm α2δ-uas muaj cov VDCC. Raws li txoj cai, kev txwv tsis pub cov α2δ-1-muaj VDCCs los ntawm pregabalin zoo li muaj lub luag haujlwm rau nws cov teebmeem anticonvulsant, analgesic, thiab anxiolytic.
Cov endogenous α-amino acids L-leucine thiab L-isoleucine, uas zoo ib yam li pregabalin thiab lwm yam gabapentinoids hauv cov qauv tshuaj, yog pom tseeb ligands ntawm α2δ VDCC subunit nrog qhov zoo sib xws li gabapentinoids (piv txwv li, IC50 = 71 nM rau L- isoleucine), thiab muaj nyob rau hauv tib neeg cerebrospinal kua ntawm micromolar ntau (piv txwv li, 12.9 μM rau L-leucine, 4.8 μM rau L-isoleucine). Nws tau raug tso cai tias lawv yuav yog lig kev ua rau ntawm subunit thiab tias lawv yuav muaj kev sib tw los tiv thaiv cov teebmeem ntawm gabapentinoids. Raws li, thaum gabapentinoids nyiam pregabalin thiab gabapentin muaj nanomolar kev sib raug zoo rau α2δ subunit, lawv cov peev xwm hauv vivo yog nyob rau hauv ntau micromolar ntau, thiab kev sib tw rau kev khi los ntawm endogenous L-amino acids tau hais tias yuav muaj lub luag haujlwm rau qhov tsis sib xws no.

Pregabalin tau pom tias muaj 6-npaug ntau dua qhov muaj sib npaug dua li gabapentin rau α2δ subunit-muaj VDCCs hauv ib txoj kev tshawb nrhiav. Txawm li cas los xij, lwm txoj kev tshawb nrhiav pom tias pregabalin thiab gabapentin muaj kev sib raug zoo sib xws rau tib neeg cov neeg tso α2δ-1 subunit (Ki = 32 nM thiab 40 nM, feem). Nyob rau hauv txhua rooj plaub, pregabalin yog 2 txog 4 npaug ntau dua li gabapentin uas yog cov tshuaj tiv thaiv kab mob thiab, hauv cov tsiaj, zoo li muaj 3 mus rau 10 npaug ntau dua li gabapentin li tshuaj anticonvulsant.

TXUJ CI NTSEEG

Quality management1

Kev Tawm Tsam 18 Cov Kev Ntsuas Xyuas Kom Zoo Kom Zoo Li Qub uas tau pom zoo 4, thiab 6 tej yaam num yog nyob rau hauv kev pom zoo.

Quality management2

Advanced thoob ntiaj teb zoo tswj system tau tso paus ruaj khov rau kev muag khoom.

Quality management3

Kev saib xyuas kev ua tau zoo khiav thoob plaws lub neej tag nrho ntawm cov khoom kom ntseeg tau tias qhov zoo thiab ua kom zoo. 

Quality management4

Pawg kws tshaj lij ntxawg koom tes txhawb nqa qhov kev xav tau zoo thaum thov thiab sau npe.

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