F. Hoffmann-La Roche Ltd, Pharma Research, CH-4070 Basel, Switzerland.
Bioorg Med Chem Lett. 2011 Feb 15;21(4):1227-31. doi: 10.1016/j.bmcl.2010.12.075. Epub 2010 Dec 21.
High throughput screening of the Roche compound library identified benzanilides such as 1 and 2 as antagonists of TAAR1. Optimisation of this hit series led to the first selective TAAR1 antagonist (N-(3-Ethoxy-phenyl)-4-pyrrolidin-1-yl-3-trifluoromethyl-benzamide EPPTB (RO5212773, 9f) having IC(50) of 28 nM at mouse TAAR1.
罗氏化合物文库的高通量筛选发现苯甲酰苯胺类化合物，如 1 和 2，是 TAAR1 的拮抗剂。对这一命中系列的优化导致了第一个选择性 TAAR1 拮抗剂（N-(3-乙氧基-苯基)-4-吡咯烷-1-基-3-三氟甲基-苯甲酰胺 EPPTB（RO5212773，9f），其对小鼠 TAAR1 的 IC50 为 28 nM。
