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Vofopitant dihydrochloride (Synonyms: GR 205171A)

カタログ番号GC37918

ボフォピタント二塩酸塩 (GR 205171A) は、強力で選択的な経口投与可能なタキキニン ニューロキニン 1(NK1) 受容体アンタゴニストであり、ラットおよびヒトの膜でそれぞれ 9.5 および 10.6 の pKi 値で NK1 受容体への [3H]SP 結合を阻害し、潜在的な広域制吐剤。

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Vofopitant dihydrochloride 化学構造

Cas No.: 168266-51-1

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Vofopitant dihydrochloride (GR 205171A) is a potent, selective and orally available tachykinin neurokinin 1(NK1) receptor antagonist, inhibits [3H]SP binding to the NK1 receptor with pKi values of 9.5 and 10.6 in rat and human membranes respectively, acts as a potential broad-spectrum anti-emetic agent[1]. pKi: 9.5 (NK1, rat), 10.6 (NK1, human)[1]

[1]. Gardner CJ, et al. GR205171: a novel antagonist with high affinity for the tachykinin NK1 receptor, and potent broad-spectrum anti-emetic activity. Regul Pept. 1996 Aug 27;65(1):45-53.

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