Pregabalin

Tsananguro Pfupi:

Zita re API Chiratidzo Tsanangudzo US DMF  EU DMF  CEP
Pregabalin Pfari / Neuralgia Mukati-Imba / EP 22223 CEP2016-141

Chigadzirwa Chigadzirwa

Chigadzirwa Mateki

CHIDZIDZO CHIDZIDZO

Pregabalin haisi GABAA kana GABAB receptor agonist.
Pregabalin igabapentinoid uye inoshanda nekudzivirira dzimwe nzira dzecalcium. Kunyanya iri ligand yeiyo yekubatsira α2δ subunit saiti yemamwe magetsi-anoenderana calcium chiteshi (VDCCs), uye nekudaro inoshanda sehibitor ye α2δ subunit-ine VDCCs. Kune maviri akasunga zvinodhaka-anosunga α2δ masununiti, α2δ-1 uye α2δ-2, uye pregabalin inoratidza yakafanana hukama hwe (uye nekudaro kushomeka kwekusarudzika pakati) eaya maviri masosi. Pregabalin inosarudza mukusunga kwayo kune α2δ VDCC subunit. Kunyangwe paine chokwadi chekuti pregabalin ndeye GABA analogue, haina kusunga kune iyo GABA inogamuchira, haishandure kuita GABA kana imwe GABA receptor agonist mu vivo, uye haina kunyatso gadzirisa GABA kutakura kana metabolism. Zvisinei, pregabalin yakawanikwa ichiburitsa kuwedzera kunoenderana nedosi muuropi kutaura kweL-glutamic acid decarboxylase (GAD), iyo enzyme inokonzeresa kugadzira GABA, uye nekudaro inogona kunge iine zvisina kunangana GABAergic mhedzisiro nekuwedzera mazinga eGABA muuropi. Ikozvino hapana humbowo hwekuti mhedzisiro ye pregabalin inopindirana nechero maitiro kunze kwekudzivirira kwe α2δ-ine VDCCs. Mukuenderana, inhibition ye α2δ-1-ine VDCCs ne pregabalin inoita kunge inokonzeresa anticonvulsant, analgesic, uye anxiolytic mhedzisiro.
Iyo endo native α-amino acids L-leucine uye L-isoleucine, iyo inonyatso fananidzwa pregabalin uye imwe gabapentinoids mukuumbwa kwemakemikari, anoonekwa kunge ligands eiyo δ2δ VDCC subunit ine hukama hwakafanana seye gabapentinoids (semuenzaniso, IC50 = 71 nM yeL- isoleucine), uye aripo muvanhu cerebrospinal fluid pa micromolar concentrations (semuenzaniso, 12.9 μM yeL-leucine, 4.8 μM yeL-isoleucine). Izvo zvakafungidzirwa kuti vanogona kunge vari endo native ligands yesubuniti uye kuti vanogona kukwikwidza kupesana nemhedzisiro ye gabapentinoids. Saizvozvo, nepo gabapentinoids senge pregabalin uye gabapentin ine nanomolar affinities yeiyo α2δ subunit, masimba avo mu vivo ari mune yakaderera micromolar renji, uye kukwikwidza kwekusunga neinogumira L-amino acids zvakanzi zvingangove zvine mhosva yekusawirirana uku.

Pregabalin yakawanikwa iine 6-yakapetwa yakakwikwidzana kupfuura gabapentin ye α2δ subunit-ine VDCCs muchidzidzo chimwe. Nekudaro, kumwe kuongorora kwakaratidza kuti pregabalin uye gabapentin vaive nehukama hwakafanana hweyevanhu recombinant α2δ-1 subunit (Ki = 32 nM uye 40 nM, zvichiteerana). Chero zvazvingaitika, pregabalin ndeye 2 kusvika ku4 zvakapetwa zvine simba kupfuura gabapentin seanalgesic uye, mumhuka, inoita kunge katatu kusvika kagumi zvine simba kupfuura gabapentin seanticonvulsant.

CERTIFICATE

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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