Olcegepant 是一种选择性的降钙素基因相关肽1 (CGRP1) 受体拮抗剂，IC50=0.03 nM，Ki=14.4 pM。

Olcegepant is an effective and selective non-peptide calcitonin gene-related peptide 1 (CGRP1) receptor antagonist (IC50 of 0.03 nM and Ki of 14.4 pM for human CGRP).

Olcegepant is extremely effective at primate CGRP receptors exhibiting an affinity (Ki) for human CGRP receptors of 14.4±6.3 (n=4) pM. Olcegepant possesses a higher affinity for the human CGRP receptor than the endogenous ligand CGRP and 150-fold higher affinity compared to the peptidic antagonist CGRP8-37. CGRP induces a concentration-dependent relaxation that is antagonized by Olcegepant in a competitive manner. Olcegepant reverses CGRP-mediated vasodilation in human cerebral vessels and inhibits neurogenic vasodilation in a surrogate animal model of migraine pathophysiology. Several lines of evidence suggest that a calcitonin-gene related peptide (CGRP) receptor antagonist may serve as a novel abortive migraine treatment. Olcegepant shows competitive antagonism at the CGRP receptor present in SK-N-MC cells. Isolated human cerebral, coronary, and omental arteries are studied with a sensitive myograph technique[1][2][3].

Pre-treatment with Olcegepant (900 μg/kg) inhibits the capsaicin-induced expression of Fos throughout the spinal trigeminal nucleus by 57%. The expression of the phosphorylated extracellular signal-regulated kinase in the trigeminal ganglion is not changed by Olcegepant pre-treatment. Olcegepant in doses between 1 and 30 μg/kg (i.v.) suppresses the effects of CGRP, released by stimulation of the trigeminal ganglion, on facial blood flow in marmoset monkeys. Olcegepant (0.3 to 0.9 mg/kg, i.v.) markedly decreases mechanical allodynia in CCI-ION rats. Olcegepant (0.6 mg/kg, i.v.) significantly decreases the number of c-Fos immunolabeled cells in the spinal nucleus of the trigeminal nerve and upregulation of ATF3 transcript (a marker of neuron injury) but not that of interleukin-6 in the trigeminal ganglion of CCI-ION rats [2][4][5].

204697-65-4

C38H47Br2N9O5

869.65

BIBN-4096;BIBN 4096BS

DMSO:48 mg/mL (55.19 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years