期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 51, 期 16, 页码 4858-4861出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm800546t
关键词
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Calcitonin gene-related peptide (CGRP) has been implicated in the pathogenesis of migraine. Early chemistry leads suffered from modest potency, significant CYP3A4 inhibition, and poor aqueous solubility. Herein. we describe the optimization of these leads to give 4 (BMS-694153), a molecule with outstanding potency, a favorable predictive toxicology profile, and remark-able aqueous solubility. Compound 4 has good intranasal bioavailablity in rabbits and shows close-dependent activity in validated in vivo and ex vivo migraine models.
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