具有口服活性和脑穿透性的脯氨酸酰胺类化合物，作为高度选择性 5-HT2c 激动剂，可用于治疗肥胖症。
Orally active and brain permeable proline amides as highly selective 5HT2c agonists for the treatment of obesity.
机构信息
Pfizer Global Research and Development, Chemistry Department, 10770 Science Center Drive, La Jolla, CA 92120, United States.
出版信息
Bioorg Med Chem Lett. 2010 Apr 1;20(7):2365-9. doi: 10.1016/j.bmcl.2010.01.107. Epub 2010 Jan 25.
PMID:20202843
Abstract
Brain-penetrable proline amides were developed as 5HT2c agonists with more than 1000-fold binding selectivity against 5HT2b receptor. After medicinal chemistry optimization and SAR studies, orally active proline amides with robust efficacy in a rodent food intake inhibition model were uncovered.
摘要
脑可渗透脯氨酸酰胺作为 5-HT2c 激动剂被开发出来，对 5-HT2b 受体具有超过 1000 倍的结合选择性。经过药物化学优化和 SAR 研究，发现了具有在啮齿动物食物摄入抑制模型中具有强大疗效的口服活性脯氨酸酰胺。
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