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
  • 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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