THE NONPEPTIDE NEUROKININ(1)-RECEPTOR ANTAGONIST, RP-67580, BLOCKS NEUROGENIC PLASMA EXTRAVASATION IN THE DURA-MATER OF RATS

被引：90

作者：

SHEPHEARD, SL

WILLIAMSON, DJ

HILL, RG

HARGREAVES, RJ

机构：

[1] Department of Pharmacology, Dohme Research Laboratories, Neuroscience Research Centre, Harlow, Essex, Terlings Park

来源：

BRITISH JOURNAL OF PHARMACOLOGY | 1993年 / 108卷 / 01期

关键词：

NEUROKININ(1)-RECEPTOR EXTRAVASATION; TRIGEMINAL GANGLION; MIGRAINE;

D O I：

10.1111/j.1476-5381.1993.tb13432.x

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

A non-peptide neurokinin, (NK1) receptor antagonist, RP 67580, that is selective for the rodent subtype of the NK1 receptor, dose-dependently reduced plasma extravasation in the dura mater produced by electrical stimulation of the trigeminal ganglion in rats, with an ID50 of 0.6 mug kg-1. Its enantiomer RP 68651 was some 400 fold less active. The results indicate that neurogenic plasma extravasation within the dura mater is NK1 receptor-mediated and suggest that NK1 receptor antagonists may have a role as antimigraine agents.

引用

页码：11 / 12

页数：2

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