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Start Over Author "Bergeron, Danielle" Topic calcitonin gene-related peptide
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1. Identification of potent CNS-penetrant thiazolidinones as novel CGRP receptor antagonists.

Author

Joshi, Pramod, Anderson, Corey, Binch, Hayley, Hadida, Sabine, Yoo, Sanghee, Bergeron, Danielle, Decker, Caroline, terHaar, Ernst, Moore, Jonathan, Garcia-Guzman, Miguel, and Termin, Andreas

Subjects
*CALCITONIN gene-related peptide, *THIAZOLIDINEDIONES, *HEADACHE treatment, *MIGRAINE, *PHARMACOKINETICS, *CALCITONIN receptors
Abstract

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 (K i =30pM, IC50 =1nM), orally bioavailable, CNS-penetrant CGRP antagonist with good pharmacokinetic properties. [Copyright &y& Elsevier]

Published
2014
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