2. Academic Validation
  3. 5-HT1F receptor agonists inhibit neurogenic dural inflammation in guinea pigs

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

  • Neuroreport. 1997 Jul 7;8(9-10):2237-40. doi: 10.1097/00001756-199707070-00029.
K W Johnson 1,  J M Schaus,  M M Durkin,  J E Audia,  S W Kaldor,  M E Flaugh,  N Adham,  J M Zgombick,  M L Cohen,  T A Branchek,  L A Phebus
Affiliations

Affiliation

  • 1 Eli Lilly & Co., Lilly Corporate Center, Indianapolis, IN 46285, USA.
PMID: 9243618 DOI: 10.1097/00001756-199707070-00029
Abstract

The serotonin (5-HT) receptor subtype mediating inhibition of neurogenic dural inflammation in guinea pigs was investigated using a series of serotonin agonists with 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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