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Design, Synthesis, and Evaluation of Thyronamine Analogues as Novel Potent Mouse Trace Amine Associated Receptor 1 (m TAAR1) Agonists. / Chiellini, Grazia; Nesi, Giulia; Digiacomo, Maria; Malvasi, Rossella; Espinoza, Stefano; Sabatini, Martina; Frascarelli, Sabina; Laurino, Annunziatina; Cichero, Elena; Macchia, Marco; Gainetdinov, Raul R.; Fossa, Paola; Raimondi, Laura; Zucchi, Riccardo; Rapposelli, Simona.

In: Journal of Medicinal Chemistry, Vol. 58, No. 12, 25.06.2015, p. 5096-5107.

Research output: Contribution to journal › Article › peer-review

Harvard

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 2015, 'Design, Synthesis, and Evaluation of Thyronamine Analogues as Novel Potent Mouse Trace Amine Associated Receptor 1 (m TAAR1) Agonists', Journal of Medicinal Chemistry, vol. 58, no. 12, pp. 5096-5107. https://doi.org/10.1021/acs.jmedchem.5b00526

APA

Chiellini, G., Nesi, G., Digiacomo, M., Malvasi, R., Espinoza, S., Sabatini, M., Frascarelli, S., Laurino, A., Cichero, E., Macchia, M., Gainetdinov, R. R., Fossa, P., Raimondi, L., Zucchi, R., & Rapposelli, S. (2015). Design, Synthesis, and Evaluation of Thyronamine Analogues as Novel Potent Mouse Trace Amine Associated Receptor 1 (m TAAR1) Agonists. Journal of Medicinal Chemistry, 58(12), 5096-5107. https://doi.org/10.1021/acs.jmedchem.5b00526

Vancouver

Chiellini G, Nesi G, Digiacomo M, Malvasi R, Espinoza S, Sabatini M et al. Design, Synthesis, and Evaluation of Thyronamine Analogues as Novel Potent Mouse Trace Amine Associated Receptor 1 (m TAAR1) Agonists. Journal of Medicinal Chemistry. 2015 Jun 25;58(12):5096-5107. https://doi.org/10.1021/acs.jmedchem.5b00526

Author

Chiellini, Grazia ; Nesi, Giulia ; Digiacomo, Maria ; Malvasi, Rossella ; Espinoza, Stefano ; Sabatini, Martina ; Frascarelli, Sabina ; Laurino, Annunziatina ; Cichero, Elena ; Macchia, Marco ; Gainetdinov, Raul R. ; Fossa, Paola ; Raimondi, Laura ; Zucchi, Riccardo ; Rapposelli, Simona. / Design, Synthesis, and Evaluation of Thyronamine Analogues as Novel Potent Mouse Trace Amine Associated Receptor 1 (m TAAR1) Agonists. In: Journal of Medicinal Chemistry. 2015 ; Vol. 58, No. 12. pp. 5096-5107.

BibTeX

@article{ac9c77cf9f9644d0b175426e88abb8a9,
title = "Design, Synthesis, and Evaluation of Thyronamine Analogues as Novel Potent Mouse Trace Amine Associated Receptor 1 (m TAAR1) Agonists",
abstract = "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.",
author = "Grazia Chiellini and Giulia Nesi and Maria Digiacomo and Rossella Malvasi and Stefano Espinoza and Martina Sabatini and Sabina Frascarelli and Annunziatina Laurino and Elena Cichero and Marco Macchia and Gainetdinov, {Raul R.} and Paola Fossa and Laura Raimondi and Riccardo Zucchi and Simona Rapposelli",
year = "2015",
month = jun,
day = "25",
doi = "10.1021/acs.jmedchem.5b00526",
language = "English",
volume = "58",
pages = "5096--5107",
journal = "Journal of Medicinal Chemistry",
issn = "0022-2623",
publisher = "American Chemical Society",
number = "12",

}

RIS

TY - JOUR

T1 - Design, Synthesis, and Evaluation of Thyronamine Analogues as Novel Potent Mouse Trace Amine Associated Receptor 1 (m TAAR1) Agonists

AU - Chiellini, Grazia

AU - Nesi, Giulia

AU - Digiacomo, Maria

AU - Malvasi, Rossella

AU - Espinoza, Stefano

AU - Sabatini, Martina

AU - Frascarelli, Sabina

AU - Laurino, Annunziatina

AU - Cichero, Elena

AU - Macchia, Marco

AU - Gainetdinov, Raul R.

AU - Fossa, Paola

AU - Raimondi, Laura

AU - Zucchi, Riccardo

AU - Rapposelli, Simona

PY - 2015/6/25

Y1 - 2015/6/25

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.

UR - http://www.scopus.com/inward/record.url?scp=84933054343&partnerID=8YFLogxK

U2 - 10.1021/acs.jmedchem.5b00526

DO - 10.1021/acs.jmedchem.5b00526

M3 - Article

C2 - 26010728

AN - SCOPUS:84933054343

VL - 58

SP - 5096

EP - 5107

JO - Journal of Medicinal Chemistry

JF - Journal of Medicinal Chemistry

SN - 0022-2623

IS - 12

ER -

ID: 36301884