| Identification | Back Directory | [Name]
Olcegepant (hydrochloride) | [CAS]
586368-06-1 | [Synonyms]
BIBN-4096 hydrochloride
BIBN4096BS hydrochloride
BIBN-4096BS hydrochloride
BIBN 4096BS hydrochloride
Olcegepant (hydrochloride)
BIBN-4096 HYDROCHLORIDE; BIBN-4096BS HYDROCHLORIDE; BIBN4096BS HYDROCHLORIDE; BIBN 4096BS HYDROCHLORIDE | [Molecular Formula]
C38H48Br2ClN9O5 | [MOL File]
586368-06-1.mol | [Molecular Weight]
906.12 |
| Hazard Information | Back Directory | [Uses]
Olcegepant hydrochloride (BIBN-4096 hydrochloride) is a potent and selective non-peptide antagonist of the calcitonin gene-related peptide 1 (CGRP1) receptor with IC50 of 0.03 nM and with a Ki of 14.4 pM for human CGRP[1][2]. | [Biological Activity]
Olcegepant hydrochloride (BIBN-4096 hydrochloride) is a potent and selective calcitonin gene-related peptide (CGRP) antagonist with a Ki value of 14.4 pM for human CGRP. | [in vivo]
Olcegepant (BIBN4096BS) in doses between 1 and 30 μg/kg (i.v.) inhibits the effects of CGRP, released by stimulation of the trigeminal ganglion, on facial blood flow in marmoset monkeys. Pre-treatment with Olcegepant (900 μg/kg) inhibits the capsaicin-induced expression of Fos throughout the spinal trigeminal nucleus by 57%. | [target]
IC50: 0.03 nM (CGRP1)
Ki: 14.4 pM (hCGRP) | [storage]
Store at -20°C | [References]
[1] Rudolf K, et al. 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. 2005 Sep 22;48(19):5921-31. DOI:10.1021/jm0490641
[2] Edvinsson L, et al. Effect of the CGRP receptor antagonist BIBN4096BS in human cerebral, coronary and omentalarteries and in SK-N-MC cells. Eur J Pharmacol. 2002 Jan 2;434(1-2):49-53. DOI:10.1016/s0014-2999(01)01532-1
[3] Doods H, et al. Pharmacological profile of BIBN4096BS, the first selective small molecule CGRP antagonist. Br J Pharmacol. 2000 Feb;129(3):420-3. DOI:10.1038/sj.bjp.0703110
[4] Sixt ML, et al. Calcitonin gene-related peptide receptor antagonist Olcegepant acts in the spinal trigeminal nucleus. Brain. 2009 Nov;132(Pt 11):3134-41. DOI:10.1093/brain/awp168
[5] Michot B, et al. Differential effects of calcitonin gene-related peptide receptor blockade by Olcegepant on mechanical allodynia induced by ligation of the infraorbital nerve vs the sciatic nerve in the rat. Pain. 2012 Sep;153(9):1939-48. DOI:10.1016/j.pain.2012.06.009 |
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