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神经激肽1(NK1)受体拮抗剂CP-99,994对家麝鼩(Suncus murinus)中尼古丁诱导的呕吐的对映体特异性抑制作用。

Enantiospecific inhibition of emesis induced by nicotine in the house musk shrew (Suncus murinus) by the neurokinin1 (NK1) receptor antagonist CP-99,994.

作者信息

Tattersall F D, Rycroft W, Marmont N, Cascieri M, Hill R G, Hargreaves R J

机构信息

Merck, Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Essex, UK.

出版信息

Neuropharmacology. 1995 Dec;34(12):1697-9. doi: 10.1016/0028-3908(95)00164-6.

Abstract

Effects of the NK1 receptor antagonist CP-99,994 on nicotine-induced emesis were examined in Suncus murinus. CP-99,994 (3 and 10 mg/kg i.p.) attenuated emesis to (-)nicotine (4 mg/kg s.c.). CP-100,263 (3 and 10 mg/kg i.p.), the enantiomer of CP-99,994 with 1000 fold lower affinity for the NK1 receptor was without effect and RP67580 reduced emesis only at a dose of 30 mg/kg i.p. Responses to NK1 antagonists were ranked according to their affinities for the Suncus murinus NK1 receptor.

摘要

在麝鼩中研究了NK1受体拮抗剂CP-99,994对尼古丁诱发呕吐的影响。CP-99,994(腹腔注射3和10mg/kg)减轻了对皮下注射(-)尼古丁(4mg/kg)的呕吐反应。CP-100,263是CP-99,994的对映体,对NK1受体的亲和力低1000倍,腹腔注射3和10mg/kg无作用,而RP67580仅在腹腔注射30mg/kg时能减轻呕吐。对NK1拮抗剂的反应根据它们对麝鼩NK1受体的亲和力进行排序。

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