The pharmacological effect of BGC20-1531, a novel prostanoid EP 4 receptor antagonist, in the Prostaglandin E 2 human model of headache

Abstract

Using a human Prostaglandin E 2 (PGE 2) model of headache, we examined whether a novel potent and selective EP 4 receptor antagonist, BGC20-1531, may prevent headache and dilatation of the middle cerebral (MCA) and superficial temporal artery (STA). In a three-way cross-over trial, eight healthy volunteers were randomly allocated to receive 200 and 400 mg BGC20-1531 and placebo, followed by a 25-min infusion of PGE 2. We recorded headache intensity on a verbal rating scale, MCA blood flow velocity and STA diameter. There was no difference in headache response or prevention of the dilation of the MCA or the STA (P > 0.05) with either dose of BGC20-1531 relative to placebo, although putative therapeutic exposures were not reached in all volunteers. In conclusion, these data suggest that the other EP receptors may be involved in PGE 2 induced headache and dilatation in normal subjects. © 2011 The Author(s).