Characterization of Ubrogepant: A Potent and Selective Antagonist of the Human Calcitonin Gene‒Related Peptide Receptor

• Published in: The Journal of pharmacology and experimental therapeutics Vol. 373; no. 1; pp. 160 - 166
• Main Authors: Moore, Eric, Fraley, Mark E., Bell, Ian M., Burgey, Christopher S., White, Rebecca B., Li, Chi-Chung, Regan, Christopher P., Danziger, Andrew, Michener, Maria Stranieri, Hostetler, Eric, Banerjee, Pradeep, Salvatore, Christopher
• Format: Journal Article
• Language: English
• Published: United States Elsevier Inc 01.04.2020
• Subjects: CTR; hERG; CIDV; CLR; CNS; AM; cAMP; AMY; CT; HEK293; PD; RAMP; CSF; PK; CGRP; PET; blood-brain barrier; migraine; calcitonin; pharmacodynamics; CGRP/amylin; headache
• ISSN: 0022-3565; 1521-0103; 1521-0103
• DOI: 10.1124/jpet.119.261065

A growing body of evidence has implicated the calcitonin gene–related peptide (CGRP) receptors in migraine pathophysiology. With the approval of monoclonal antibodies targeting CGRP or the CGRP receptor, the inhibition of CGRP-mediated signaling emerged as a promising approach for preventive treatme...