BIBN 4096BS

Uses

Olcegepant is a potent and selective calcitonin gene-related peptide (CGRP) receptor antagonist. Olcegepant displays high affinity for human CGRP receptors and exhibits no significant affinity for 75 other receptors. Olcegepant may a be viable option for the treatment of acute migraines.

Biological Activity

BIBN4096BS (Olcegepant) is a potent calcitonin gene-related peptide (CGRP) receptor antagonist with higher affinity/potency toward human over r at & mouse receptor (human/r at Ki = 14.4 pM/3.4 nM by binding assay; human/mouse Kb = 8 pM//7.711 nM by cellular cAMP assay). BIBN4096BS inhibits facial blood flow by electrical stimulation of marmoset monkey trigeminal ganglion (IC50 = 3 μg/kg i.v.) without any intrinsic cardiovascular effects. Studies using anaesthetized rats reveals th at BIBN4096BS antagonism against trigeminal nociceptive stimulation by capsaicin is limited to the spinal trigeminal nucleus, but not trigeminal ganglion. Also widely employed for in vivo studies in mice.

target

CGRP1

storage

Store at -20°C