ArticleBritish journal of pharmacology2002
BIBN4096BS is a potent competitive antagonist of the relaxant effects of alpha-CGRP on human temporal artery: comparison with CGRP(8-37).
Article in British journal of pharmacology, 2002. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers, 1 of them a synthesis that pooled it.
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Who cites it
16 citing papers in PubMed, 1 synthesis or guideline pooled it, 64 citations in OpenAlex.
- Efficacy and Safety of Rimegepant for the Acute Treatment of Migraine: Evidence From Randomized Controlled Trials.Frontiers in pharmacology · 2019Pooled it
- The potent calcitonin gene-related peptide receptor antagonist, telcagepant, does not affect nitroglycerin-induced vasodilation in healthy men.British journal of clinical pharmacology · 2011Trial
- Gepants: targeting the CGRP pathway for migraine relief.Frontiers in pharmacology · 2025Review
- A Pharmacological Review of Calcitonin Gene-Related Peptide Biologics and Future Use for Chronic Pain.Cureus · 2023Review
- Gel-forming antagonist provides a lasting effect on CGRP-induced vasodilation.Frontiers in pharmacology · 2022Article
- Article
- Spotlight on Anti-CGRP Monoclonal Antibodies in Migraine: The Clinical Evidence to Date.Clinical pharmacology in drug development · 2017Review
- A role for the sensory neuropeptide calcitonin gene-related peptide in endothelial cell proliferation in vivo.British journal of pharmacology · 2012Article
- The extracranial vascular theory of migraine: an artificial controversy.Journal of neural transmission (Vienna, Austria : 1996) · 2011Review
- Calcitonin gene-related peptide (CGRP) receptor antagonists in the treatment of migraine.CNS drugs · 2010Article
- CGRP receptor antagonism and migraine.Neurotherapeutics : the journal of the American Society for Experimental NeuroTherapeutics · 2010Review
- Inhibition of calcitonin gene-related peptide function: a promising strategy for treating migraine.Headache · 2008Review
- BIBN4096BS and CGRP(8-37) antagonize the relaxant effects of alpha-CGRP more than those of beta-CGRP in human extracranial arteries.Naunyn-Schmiedeberg's archives of pharmacology · 2005Article
- Noncompetitive antagonism of BIBN4096BS on CGRP-induced responses in human subcutaneous arteries.British journal of pharmacology · 2004Article
- Functional 5-HT receptors in human occipital artery.Naunyn-Schmiedeberg's archives of pharmacology · 2004Article
- Effects of the CGRP receptor antagonist BIBN4096BS on capsaicin-induced carotid haemodynamic changes in anaesthetised pigs.British journal of pharmacology · 2003Article
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Authors and funding
3 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
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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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.