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J Med Chem. 2015 Jun 25;58(12):5096-107. doi: 10.1021/acs.jmedchem.5b00526. Epub 2015 Jun 5.

Design, Synthesis, and Evaluation of Thyronamine Analogues as Novel Potent Mouse Trace Amine Associated Receptor 1 (mTAAR1) Agonists.

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†Department of Pathology, University of Pisa, 56100 Pisa, Italy.
‡Deptartment of Pharmacy, University of Pisa, via Bonanno 6, 56100 Pisa, Italy.
§Department of Neuroscience and Brain Technologies, Istituto Italiano di Tecnologia, 16163 Genova, Italy.
∥Department of NEUROFARBA, Section of Pharmacology, University of Florence, 50121 Firenze, Italy.
⊥Department of Pharmacy, University of Genoa, 16126 Genoa, Italy.
#Institute of Translational Biomedicine, St. Petersburg State University, St. Petersburg, 199034, Russia.
¶Skolkovo Institute of Science and Technology (Skoltech), Skolkovo, Moscow region, 143025, Russia.


Trace amine associated receptor 1 (TAAR1) is a G protein coupled receptor (GPCR) expressed in brain and periphery activated by a wide spectrum of agonists that include, but are not limited to, trace amines (TAs), amphetamine-like psychostimulants, and endogenous thyronamines such as thyronamine (T0AM) and 3-iodothyronamine (T1AM). Such polypharmacology has made it challenging to understand the role and the biology of TAAR1. In an effort to understand the molecular basis of TAAR1 activation, we rationally designed and synthesized a small family of thyronamine derivatives. Among them, compounds 2 and 3 appeared to be a good mimic of the parent endogenous thyronamine, T0AM and T1AM, respectively, both in vitro and in vivo. Thus, these compounds offer suitable tools for studying the physiological roles of mouse TAAR1 and could represent the starting point for the development of more potent and selective TAAR1 ligands.

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