BIBN 4096Cat. No. 4561 |
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Alternative Name: Olcegepant Chemical Name: 1-[3,5-Dibromo-N-[[4-(1,4-dihydro-2-oxo-3(2H)-quinazolinyl)-1-piperidinyl]carbonyl]-D-tyrosyl-L-lysyl]-4-(4-pyridinyl)-piperazine |
Biological Activity
Potent and selective CGRP receptor antagonist (IC50 values are 0.03 and 6.4 nM for human and rat CGRP receptors respectively). Displays high affinity for human CGRP receptors (Ki = 14.4 pM); exhibits no significant affinity for 75 other receptors.Certificate of Analysis / Safety Data Sheet
References
Doods et al (2000) Pharmacological profile of BIBN4096BS, the first selective small molecule CGRP antagonist. Br.J.Pharmacol. 129 420. PMID: 10711339.
Rudolf et al (2005) Development of human calcitonin gene-related peptide (CGRP) receptor antagonists. 1. Potent and selective small molecule CGRP antagonists. 1-[N2-[3,5-Dibromo-N-[[4-(3,4-dihydro-2(1H)-oxoquinazolin-3-yl)-1- piperidinyl]carbonyl]-D-tyrosyl]-L-lysyl]-4-(4-pyridinyl)piperazine: the first CGRP antagonist for clinical trials in acute migraine. J.Med.Chem. 48 5921. PMID: 16161996.
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Keywords: BIBN 4096, supplier, BIBN4096, migraine, potent, selective, CGRP, receptors, antagonists, calcitonin, gene-related, peptides, Olcegepant
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