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Vazegepant is a calcitonin gene-related peptide (CGRP) receptor antagonist (Ki = 23 pM in SK-N-MC membrane preparations).1 It is >10,000-fold selective for the CGRP receptor over the adrenomedullin receptor 1 (AM1 receptor), AM2 receptor, calcitonin (CT) receptor, amylin 1 (AMY1) receptor, and AMY3 receptor. Ex vivo, vazegepant reverses CGRP-induced dilation of human intracranial arteries (EC50 = 880 pM) but does not induce contractions in human coronary arteries when used at concentrations up to 10 µM. It reduces human α-CGRP-induced increases in facial blood flow in marmosets when administered subcutaneously at a dose of 0.03 mg/kg. Formulations containing vazegepant have been used in the treatment of migraines.
WARNING This product is not for human or veterinary use.
1. Discovery of (R)-