Olcegepant hydrochloride is a potent and selective non-peptidethe calcitonin gene-related peptide 1 (CGRP1) receptor antagonist (with IC50 of 0.03 nM for human CGRP).

CGRP1:0.03 nM , CGRP (human):(ki)14.4 pM

Olcegepant (BIBN4096BS) is extremely potent at primate CGRP receptors exhibiting an affinity (Ki) for human CGRP receptors of 14.4±6.3 (n=4) pM[2].?Several lines of evidence suggest that a calcitonin-gene related peptide (CGRP) receptor antagonist may serve as a novel abortive migraine treatment.?Olcegepant (BIBN4096BS) exhibits 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.?CGRP induces a concentration-dependent relaxation that is antagonized by Olcegepant in a competitive manner[3].

Pre-treatment with Olcegepant (900 μg/kg) inhibits the capsaicin-induced expression of Fos throughout the spinal trigeminal nucleus by 57%.?In contrast, the expression of phosphorylated extracellular signal-regulated kinase in the trigeminal ganglion is not changed by Olcegepant pre-treatment[4].