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

被引:89
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
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
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页码:11 / 12
页数:2
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