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Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission
Published on: August 16, 2018
Selective antagonists of mouse trace amine-associated receptor 1 (mTAAR1): discovery of EPPTB (RO5212773)
Henri Stalder1, Marius C Hoener, Roger D Norcross
1F. Hoffmann-La Roche Ltd, Pharma Research, CH-4070 Basel, Switzerland. henri.stalder@roche.com
Bioorganic & Medicinal Chemistry Letters
|January 18, 2011
Abstract:
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.
