降钙素基因相关肽
偏头痛
药理学
敌手
生物利用度
体内
医学
狨猴
受体
口服
降钙素
广告
受体拮抗剂
药代动力学
内科学
神经肽
生物
古生物学
生物技术
作者
Guanglin Luo,Ling Chen,Charles M. Conway,Rex Denton,Deborah Keavy,Michael Gulianello,Yanling Huang,Walter Kostich,Kimberley A. Lentz,Stephen E. Mercer,Richard Schartman,Laura J. Signor,Marc Browning,John E. Macor,Gene M. Dubowchik
摘要
Calcitonin gene-related peptide (CGRP) receptor antagonists have been clinically shown to be effective in the treatment of migraine, but identification of potent and orally bioavailable compounds has been challenging. Herein, we describe the conceptualization, synthesis, and preclinical characterization of a potent, orally active CGRP receptor antagonist 5 (BMS-846372). Compound 5 has good oral bioavailability in rat, dog, and cynomolgus monkeys and overall attractive preclinical properties including strong (>50% inhibition) exposure-dependent in vivo efficacy in a marmoset migraine model.
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