Literature DB >> 11976276

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

Raphaela Verheggen1, Katja Bumann, Alberto J Kaumann.   

Abstract

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 alpha-CGRP on rings of human temporal artery. alpha-CGRP relaxed the arteries precontracted with 9 - 24 mM KCl (-logEC50=9.4) nearly as efficaciously as sodium nitroprusside (10 microM). BIBN4096BS (0.1 - 100 nM) antagonized the effects of alpha-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 microM) did not modify the relaxant effects of papaverine and sodium nitroprusside. CGRP(8-37) (1 - 10 microM) antagonized the effects of alpha-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.

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Year:  2002        PMID： 11976276      PMCID： PMC1762122          DOI： 10.1038/sj.bjp.0704682

Source DB:  PubMed          Journal:  Br J Pharmacol        ISSN： 0007-1188            Impact factor:   8.739


  26 in total

1.  Arterial dilations in response to calcitonin gene-related peptide involve activation of K+ channels.

Authors:  M T Nelson; Y Huang; J E Brayden; J Hescheler; N B Standen
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3.  Vasoactive peptide release in the extracerebral circulation of humans during migraine headache.

Authors:  P J Goadsby; L Edvinsson; R Ekman
Journal:  Ann Neurol       Date:  1990-08       Impact factor: 10.422

4.  Calcitonin gene-related peptide is released from capsaicin-sensitive nerve fibres and induces vasodilatation of human cerebral arteries concomitant with activation of adenylyl cyclase.

Authors:  I Jansen-Olesen; A Mortensen; L Edvinsson
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Authors:  J M Quayle; A D Bonev; J E Brayden; M T Nelson
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6.  The peptidergic innervation of the human superficial temporal artery: immunohistochemistry, ultrastructure, and vasomotility.

Authors:  I J Olesen; S Gulbenkian; A Valença; J L Antunes; J Wharton; J M Polak; L Edvinsson
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7.  Neuronal versus endothelial origin of vasoactive acetylcholine in pial vessels.

Authors:  E Hamel; C Assumel-Lurdin; L Edvinsson; D Fage; E T MacKenzie
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8.  Participation of 5-HT1-like and 5-HT2A receptors in the contraction of human temporal artery by 5-hydroxytryptamine and related drugs.

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9.  Calcitonin gene-related peptide activates the K+ channels of vascular smooth muscle cells via adenylate cyclase.

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Authors:  P J Goadsby; L Edvinsson; R Ekman
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  13 in total

Review 1.  Inhibition of calcitonin gene-related peptide function: a promising strategy for treating migraine.

Authors:  Paul L Durham
Journal:  Headache       Date:  2008-09       Impact factor: 5.887

2.  Calcitonin gene-related peptide (CGRP) receptor antagonists in the treatment of migraine.

Authors:  Paul L Durham; Carrie V Vause
Journal:  CNS Drugs       Date:  2010-07       Impact factor: 5.749

Review 3.  CGRP receptor antagonism and migraine.

Authors:  Lars Edvinsson; Tony W Ho
Journal:  Neurotherapeutics       Date:  2010-04       Impact factor: 7.620

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Authors:  Bart J Van der Schueren; Rebecca Blanchard; M Gail Murphy; John Palcza; Inge De Lepeleire; Anne Van Hecken; Marleen Depré; Jan N de Hoon
Journal:  Br J Clin Pharmacol       Date:  2011-05       Impact factor: 4.335

Review 5.  The extracranial vascular theory of migraine: an artificial controversy.

Authors:  Elliot Shevel
Journal:  J Neural Transm (Vienna)       Date:  2011-01-05       Impact factor: 3.575

6.  A role for the sensory neuropeptide calcitonin gene-related peptide in endothelial cell proliferation in vivo.

Authors:  Paul I Mapp; Daniel F McWilliams; Matthew J Turley; Edward Hargin; David A Walsh
Journal:  Br J Pharmacol       Date:  2012-06       Impact factor: 8.739

7.  BIBN4096BS and CGRP(8-37) antagonize the relaxant effects of alpha-CGRP more than those of beta-CGRP in human extracranial arteries.

Authors:  Raphaela Verheggen; Kordian Wojtas; Martin Webel; Steffi Hoffmann; Alberto J Kaumann
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  2005-06-28       Impact factor: 3.000

8.  Effects of the CGRP receptor antagonist BIBN4096BS on capsaicin-induced carotid haemodynamic changes in anaesthetised pigs.

Authors:  Kapil Kapoor; Udayasankar Arulmani; Jan P C Heiligers; Ingrid M Garrelds; Edwin W Willems; Henri Doods; Carlos M Villalón; Pramod R Saxena
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9.  Functional 5-HT receptors in human occipital artery.

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10.  Noncompetitive antagonism of BIBN4096BS on CGRP-induced responses in human subcutaneous arteries.

Authors:  Majid Sheykhzade; Henrik Lind; Lars Edvinsson
Journal:  Br J Pharmacol       Date:  2004-10-11       Impact factor: 8.739
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