Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10594839 | Bioorganic & Medicinal Chemistry Letters | 2014 | 5 Pages |
Abstract
Calcitonin gene-related peptide (CGRP) has been implicated in acute migraine pathogenesis. In an effort to identify novel CGRP receptor antagonists for the treatment of migraine, we have discovered thiazolidinone 49, a potent (Ki = 30 pM, IC50 = 1 nM), orally bioavailable, CNS-penetrant CGRP antagonist with good pharmacokinetic properties.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Pramod Joshi, Corey Anderson, Hayley Binch, Sabine Hadida, Sanghee Yoo, Danielle Bergeron, Caroline Decker, Ernst terHaar, Jonathan Moore, Miguel Garcia-Guzman, Andreas Termin,