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Bioorg Med Chem Lett. 2011 Feb 15;21(4):1227-31. doi: 10.1016/j.bmcl.2010.12.075. Epub 2010 Dec 21.

Selective antagonists of mouse trace amine-associated receptor 1 (mTAAR1): discovery of EPPTB (RO5212773).

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  • 1F. Hoffmann-La Roche Ltd, Pharma Research, CH-4070 Basel, Switzerland.


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.

Copyright © 2010 Elsevier Ltd. All rights reserved.

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