The preclinical pharmacology of BIBN4096BS, a CGRP antagonist

Debbie L. Hay, David Poyner

Research output: Contribution to journalArticle

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.
Original languageEnglish
Pages (from-to)31-42
Number of pages12
JournalCardiovascular Therapeutics
Volume23
Issue number1
DOIs
Publication statusPublished - Mar 2005

Fingerprint

Calcitonin Gene-Related Peptide Receptors
Pharmacology
Cardiovascular System
Neuropeptides
Migraine Disorders
Blood Vessels
Ischemia
Cell Line
Pharmaceutical Preparations
BIBN 4096BS
Clinical Studies

Keywords

  • calcitonin gene-related peptide receptors
  • calcitonin gene-related peptide
  • preclinical drug evaluation
  • quinazolines
  • piperazines

Cite this

@article{c1db60e0c44045caacb764bfa4be4b01,
title = "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.",
keywords = "calcitonin gene-related peptide receptors, calcitonin gene-related peptide, preclinical drug evaluation, quinazolines, piperazines",
author = "Hay, {Debbie L.} and David Poyner",
year = "2005",
month = "3",
doi = "10.1111/j.1527-3466.2005.tb00155.x",
language = "English",
volume = "23",
pages = "31--42",
journal = "Cardiovascular Therapeutics",
issn = "0897-5957",
publisher = "Neva Press, Inc.",
number = "1",

}

The preclinical pharmacology of BIBN4096BS, a CGRP antagonist. / Hay, Debbie L.; Poyner, David.

In: Cardiovascular Therapeutics , Vol. 23, No. 1, 03.2005, p. 31-42.

Research output: Contribution to journalArticle

TY - JOUR

T1 - The preclinical pharmacology of BIBN4096BS, a CGRP antagonist

AU - Hay, Debbie L.

AU - Poyner, David

PY - 2005/3

Y1 - 2005/3

N2 - 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.

AB - 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.

KW - calcitonin gene-related peptide receptors

KW - calcitonin gene-related peptide

KW - preclinical drug evaluation

KW - quinazolines

KW - piperazines

UR - http://onlinelibrary.wiley.com/doi/10.1111/j.1527-3466.2005.tb00155.x/abstract

UR - http://www.scopus.com/inward/record.url?scp=17744379790&partnerID=8YFLogxK

U2 - 10.1111/j.1527-3466.2005.tb00155.x

DO - 10.1111/j.1527-3466.2005.tb00155.x

M3 - Article

C2 - 15867946

VL - 23

SP - 31

EP - 42

JO - Cardiovascular Therapeutics

JF - Cardiovascular Therapeutics

SN - 0897-5957

IS - 1

ER -