Comparison of the Vasoconstrictor Effects of the Calcitonin Gene-Related Peptide (CGRP) Receptor Antagonist Telcagepant (MK-0974) and Zolmitriptan in Human Isolated Coronary Arteries.

Research output: Contribution to journalArticle

Abstract

Studies were conducted in human isolated coronary arteries to explore the vascular effects of the calcitonin gene-related peptide (CGRP) receptor antagonist telcagepant, and to compare its coronary vasoconstrictive potential to that of zolmitriptan. KCl-precontracted coronary vessels were shown to relax to human alphaCGRP, with the CGRP-mediated vasorelaxation completely blocked with 30 muM telcagepant. In coronary vessels at basal tone, zolmitriptan caused a concentration-dependent contraction (pEC50 = 6.9 +/- 0.1, slope 0.94), with the greatest contraction obtained between 1-10 muM in most tissues. In contrast, telcagepant at concentrations up to 30 muM evoked no change in contractile tone. These findings suggest the potential for CGRP receptor antagonists to exert antimigraine efficacy in the absence of adverse effects on coronary tone.

Details

Authors
  • Joseph J Lynch
  • Christopher P Regan
  • Lars Edvinsson
  • Richard J Hargreaves
  • Stefanie A Kane
Organisations
Research areas and keywords

Subject classification (UKÄ) – MANDATORY

  • Other Clinical Medicine

Keywords

  • coronary artery, telcagepant, zolmitriptan
Original languageEnglish
Pages (from-to)518-521
JournalJournal of Cardiovascular Pharmacology
Volume55
Issue number5
Publication statusPublished - 2010
Publication categoryResearch
Peer-reviewedYes