The pharmacological effect of BGC20-1531, a novel prostanoid EP4 receptor antagonist, in the prostaglandin E2 human model of headache

Maria Antonova, Troels Wienecke, Karen Maubach, Emma Thomas, Jes Olesen, Messoud Ashina

22 Citations (Scopus)

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.
Original languageEnglish
JournalJournal of Headache and Pain
Volume12
Issue number5
Pages (from-to)551-9
Number of pages9
ISSN1129-2369
DOIs
Publication statusPublished - 2011

Keywords

  • Adult
  • Analgesics
  • Cerebrovascular Circulation
  • Cross-Over Studies
  • Dinoprostone
  • Double-Blind Method
  • Female
  • Headache
  • Humans
  • Male
  • Pyridines
  • Receptors, Prostaglandin E, EP4 Subtype
  • Sulfonamides
  • Vasodilation
  • Young Adult

Fingerprint

Dive into the research topics of 'The pharmacological effect of BGC20-1531, a novel prostanoid EP4 receptor antagonist, in the prostaglandin E2 human model of headache'. Together they form a unique fingerprint.

Cite this