The preclinical pharmacology of BIBN4096BS, a CGRP antagonist.

Abstract

CGRP is an important neuropeptide found throughout the cardiovascular system. However, until recently it has been difficult to define its pharmacology or physiological role because of the lack of suitable antagonists. BIBN4096BS is a high-affinity, nonpeptide antagonist that shows much greater selectivity for human CGRP1 receptors compared to any other drug. Its pharmacology has been defined with studies on transfected cells or cell lines endogenously expressing receptors of known composition. These have allowed confirmation that in many human blood vessels, CGRP is working via CGRP1 receptors. However, it also interacts with other CGRP-activated receptors, of unknown composition. In vivo, clinical studies have shown that BIBN4096BS is likely to be useful in the treatment of migraine. It has also been used to define the role of CGRP in phenomena such as plasma extravasation and cardioprotection following ischemia.

• Authors: Debbie L Hay, David Poyner
• Journal: Cardiovascular drug reviews (Cardiovasc Drug Rev) Vol. 23 Issue 1 Pg. 31-42 ( 2005) ISSN: 0897-5957 [Print] United States
• PMID: 15867946 (Publication Type: Comparative Study, Journal Article, Research Support, Non-U.S. Gov't, Review)

Chemical References

• Calcitonin Gene-Related Peptide Receptor Antagonists
• Piperazines
• Quinazolines
• Receptors, Calcitonin Gene-Related Peptide
• Calcitonin Gene-Related Peptide
• olcegepant

Topics

• Animals
• Calcitonin Gene-Related Peptide (antagonists & inhibitors, pharmacology, therapeutic use)
• Calcitonin Gene-Related Peptide Receptor Antagonists
• Drug Evaluation, Preclinical (methods)
• Humans
• Piperazines (chemistry, pharmacology, therapeutic use)
• Quinazolines (chemistry, pharmacology, therapeutic use)
• Receptors, Calcitonin Gene-Related Peptide (drug effects, therapeutic use)