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

Lynch, Joseph J; Regan, Christopher P; Edvinsson, Lars LU ; Hargreaves, Richard J and Kane, Stefanie A (2010) In Journal of Cardiovascular Pharmacology 55(5). p.518-521
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... (More)
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. (Less)
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author
organization
publishing date
type
Contribution to journal
publication status
published
subject
keywords
coronary artery, telcagepant, zolmitriptan
in
Journal of Cardiovascular Pharmacology
volume
55
issue
5
pages
518 - 521
publisher
Lippincott Williams & Wilkins
external identifiers
  • wos:000278205900013
  • pmid:20164785
  • scopus:77952979510
ISSN
1533-4023
DOI
10.1097/FJC.0b013e3181d7665f
language
English
LU publication?
yes
id
0fc03b59-f46e-4dec-8093-a8507f4e9db3 (old id 1552538)
alternative location
http://www.ncbi.nlm.nih.gov/pubmed/20164785?dopt=Abstract
date added to LUP
2010-03-03 13:35:46
date last changed
2018-05-29 10:04:47
@article{0fc03b59-f46e-4dec-8093-a8507f4e9db3,
  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.},
  author       = {Lynch, Joseph J and Regan, Christopher P and Edvinsson, Lars and Hargreaves, Richard J and Kane, Stefanie A},
  issn         = {1533-4023},
  keyword      = {coronary artery,telcagepant,zolmitriptan},
  language     = {eng},
  number       = {5},
  pages        = {518--521},
  publisher    = {Lippincott Williams & Wilkins},
  series       = {Journal of Cardiovascular Pharmacology},
  title        = {Comparison of the Vasoconstrictor Effects of the Calcitonin Gene-Related Peptide (CGRP) Receptor Antagonist Telcagepant (MK-0974) and Zolmitriptan in Human Isolated Coronary Arteries.},
  url          = {http://dx.doi.org/10.1097/FJC.0b013e3181d7665f},
  volume       = {55},
  year         = {2010},
}