BIBN4096BS is a potent competitive antagonist of the relaxant effects of α‐CGRP on human temporal artery: comparison with CGRP(8‐37)

Release of CGRP during migraine may produce harmful dilatation of cranial arteries, thereby possibly causing pain. We have compared the antagonism by BIBN4096BS and CGRP(8‐37) of the relaxant effects of α‐CGRP on rings of human temporal artery. α‐CGRP relaxed the arteries precontracted with 9 – 24 m...

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Bibliographic Details
Published in:British journal of pharmacology 2002-05, Vol.136 (1), p.120-126
Main Authors: Verheggen, Raphaela, Bumann, Katja, Kaumann, Alberto J.
Format: Article
Language:English
Subjects:
Adolescent
Adult
Aged
BIBN4096BS
Calcitonin Gene-Related Peptide - antagonists & inhibitors
Calcitonin Gene-Related Peptide - pharmacology
CGRP(8‐37)
Female
Human temporal artery
Humans
In Vitro Techniques
Male
Middle Aged
migraine
Muscle Relaxation - drug effects
Muscle, Smooth, Vascular - drug effects
Muscle, Smooth, Vascular - physiology
Nitroprusside - pharmacology
Papaverine - pharmacology
Peptide Fragments - pharmacology
Piperazines - pharmacology
Quinazolines - pharmacology
Receptors, Calcitonin Gene-Related Peptide - drug effects
Temporal Arteries - drug effects
Temporal Arteries - physiology
Vasodilator Agents - pharmacology
α‐CGRP‐evoked relaxation
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Summary:Release of CGRP during migraine may produce harmful dilatation of cranial arteries, thereby possibly causing pain. We have compared the antagonism by BIBN4096BS and CGRP(8‐37) of the relaxant effects of α‐CGRP on rings of human temporal artery. α‐CGRP relaxed the arteries precontracted with 9 – 24 mM KCl (−logEC50=9.4) nearly as efficaciously as sodium nitroprusside (10 μM). BIBN4096BS (0.1 – 100 nM) antagonized the effects of α‐CGRP in surmountable manner with slopes of Schild‐plots not different from unity. −LogKB values of 10.1 and 10.4 were estimated for BIBN4096BS when administered before or during the KCl‐contracture respectively. BIBN4096BS (1 μM) did not modify the relaxant effects of papaverine and sodium nitroprusside. CGRP(8‐37) (1 – 10 μM) antagonized the effects of α‐CGRP in a surmountable manner with slopes of Schild‐plots not different from unity. −LogKB values of 6.6 and 6.7 were estimated for CGRP(8‐37) administered before or during the KCl‐contracture respectively. The high affinity of BIBN4096BS for CGRP receptors of human temporal artery makes it an excellent tool to explore the hypothesis of CGRP‐evoked cerebral vasodilation in migraine. British Journal of Pharmacology (2002) 136, 120–126; doi:10.1038/sj.bjp.0704682
ISSN:0007-1188
1476-5381
DOI:10.1038/sj.bjp.0704682