Design, Synthesis, and Evaluation of Thyronamine Analogues as Novel Potent Mouse Trace Amine Associated Receptor 1 (mTAAR1) Agonists. / Chiellini, G; Nesi, G; Digiacomo, M; Malvasi, R; Espinoza, S; Sabatini, M; Frascarelli, S; Laurino, A; Cichero, E; Macchia, M; Gainetdinov, RR; Fossa, P; Raimondi, L; Zucchi, R; Rapposelli, S.
In: Journal of Medicinal Chemistry, 2015.Research output: Contribution to journal › Article
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TY - JOUR
T1 - Design, Synthesis, and Evaluation of Thyronamine Analogues as Novel Potent Mouse Trace Amine Associated Receptor 1 (mTAAR1) Agonists.
AU - Chiellini, G
AU - Nesi, G
AU - Digiacomo, M
AU - Malvasi, R
AU - Espinoza, S
AU - Sabatini, M
AU - Frascarelli, S
AU - Laurino, A
AU - Cichero, E
AU - Macchia, M
AU - Gainetdinov, RR
AU - Fossa, P
AU - Raimondi, L
AU - Zucchi, R
AU - Rapposelli, S.
PY - 2015
Y1 - 2015
N2 - 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.
AB - 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.
M3 - статья
JO - Journal of Medicinal Chemistry
JF - Journal of Medicinal Chemistry
SN - 0022-2623
ER -
ID: 5835141