Olcegepant (hydrochloride)

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