5-HT1F receptor agonists inhibit neurogenic dural inflammation in guinea pigs

被引：134

作者：

Johnson, KW

Schaus, JM

Durkin, MM

Audia, JE

Kaldor, SW

Flaugh, ME

Adham, N

Zgombick, JM

Cohen, ML

Branchek, TA

Phebus, LA

机构：

[1] ELI LILLY & CO,LILLY CORP CTR,INDIANAPOLIS,IN 46285

[2] SYNAPT PHARMACEUT CORP,PARAMUS,NJ 07652

来源：

NEUROREPORT | 1997年 / 8卷 / 9-10期

关键词：

migraine; receptor localization; saphenous vein; serotonin receptor; trigeminal; vasoconstriction;

D O I：

10.1097/00001756-199707070-00029

中图分类号：

Q189 [神经科学];

学科分类号：

071006 ;

摘要：

THE serotonin (5-HT) receptor subtype mediating inhibition of neurogenic dural inflammation in guinea pigs was investigated using a series of serotonin agonists differing affinities for the 5-HT1B, 5-HT1D and 5-HT1F receptors. When agonist potencies for inhibiting neurogenic inflammation were compared with affinities for these receptor subtypes, a significant positive correlation was seen only with the 5-HT1F receptor. The potency of agonists in inhibiting adenylate cyclase in cells transfected with human 5-HT1F receptor was also highly correlated with their potency in the animal model of migraine. In situ hybridization demonstrated 5-HT1F receptor mRNA in guinea pig trigeminal ganglion neurons. These data suggest that the 5-HT1F receptor is a rational target for migraine therapeutics.

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收藏

页码：2237 / 2240

页数：4

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