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.
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Potential of Ligands for Trace Amine-Associated Receptor 1 (TAAR1) in the Management of Substance Use Disorders.
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Department of Pharmacology and Toxicology, University at Buffalo, The State University of New York, 955 Main Street, Buffalo, NY, 14214, USA.
Trace amines, including β-phenylethylamine (β-PEA), p-tyramine (TYR), tryptamine (TRP), and p-octopamine (OCT), represent a group of amines expressed at low levels in the mammalian brain. Given the close structural similarities to traditional monoamines, links between trace amines and the monoaminergic system have long been suspected. Trace amine-associated receptor 1 (TAAR1), the most well characterized receptor in the TAAR family, has been shown to be potently activated by trace amines such as TYR and PEA.
View Article and Find Full Text PDFRenal artery responses to trace amines: Multiple and differential mechanisms of action.
Life Sci
July 2021
Faculty of Health Sciences and Medicine, Bond University, 4229, Queensland, Australia. Electronic address:
Article Synopsis
- The study examined how trace amines (p-tyramine, p-synephrine, and p-octopamine) affect renal arteries, which are important for regulating blood pressure and can have cardiovascular side effects.
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Selective antagonists of mouse trace amine-associated receptor 1 (mTAAR1): discovery of EPPTB (RO5212773).
Bioorg Med Chem Lett
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F. 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.
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