Comparison of the Vasoconstrictor Effects of the Calcitonin Gene-Related Peptide (CGRP) Receptor Antagonist Telcagepant (MK-0974) and Zolmitriptan in Human Isolated Coronary Arteries.
(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)
Please use this url to cite or link to this publication:
https://lup.lub.lu.se/record/1552538
- author
- Lynch, Joseph J ; Regan, Christopher P ; Edvinsson, Lars LU ; Hargreaves, Richard J and Kane, Stefanie A
- organization
- publishing date
- 2010
- 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
- pmid:20164785
- 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
- 2016-04-01 10:52:52
- date last changed
- 2024-01-07 03:26:21
@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}},
keywords = {{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}},
doi = {{10.1097/FJC.0b013e3181d7665f}},
volume = {{55}},
year = {{2010}},
}