Standard

Trace amine-associated receptor 1 partial agonism reveals novel paradigm for neuropsychiatric therapeutics. / Revel, F.G.; Moreau, J.-L.; Gainetdinov, R.R.; Ferragud, A.; Velázquez-Sánchez, C.; Sotnikova, T.D.; Morairty, S.R.; Harmeier, A.; Groebke Zbinden, K.; Norcross, R.D.; Bradaia, A.; Kilduff, T.S.; Biemans, B.; Pouzet, B.; Caron, M.G.; Canales, J.J.; Wallace, T.L.; Wettstein, J.G.; Hoener, M.C.

в: Biological Psychiatry, 2012, стр. 934-942.

Результаты исследований: Научные публикации в периодических изданиях › статья

Harvard

Revel, FG, Moreau, J-L, Gainetdinov, RR, Ferragud, A, Velázquez-Sánchez, C, Sotnikova, TD, Morairty, SR, Harmeier, A, Groebke Zbinden, K, Norcross, RD, Bradaia, A, Kilduff, TS, Biemans, B, Pouzet, B, Caron, MG, Canales, JJ, Wallace, TL, Wettstein, JG & Hoener, MC 2012, 'Trace amine-associated receptor 1 partial agonism reveals novel paradigm for neuropsychiatric therapeutics.', Biological Psychiatry, стр. 934-942. https://doi.org/10.1016/j.biopsych.2012.05.014

APA

Revel, F. G., Moreau, J-L., Gainetdinov, R. R., Ferragud, A., Velázquez-Sánchez, C., Sotnikova, T. D., Morairty, S. R., Harmeier, A., Groebke Zbinden, K., Norcross, R. D., Bradaia, A., Kilduff, T. S., Biemans, B., Pouzet, B., Caron, M. G., Canales, J. J., Wallace, T. L., Wettstein, J. G., & Hoener, M. C. (2012). Trace amine-associated receptor 1 partial agonism reveals novel paradigm for neuropsychiatric therapeutics. Biological Psychiatry, 934-942. https://doi.org/10.1016/j.biopsych.2012.05.014

Vancouver

Revel FG, Moreau J-L, Gainetdinov RR, Ferragud A, Velázquez-Sánchez C, Sotnikova TD и пр. Trace amine-associated receptor 1 partial agonism reveals novel paradigm for neuropsychiatric therapeutics. Biological Psychiatry. 2012;934-942. https://doi.org/10.1016/j.biopsych.2012.05.014

Author

Revel, F.G. ; Moreau, J.-L. ; Gainetdinov, R.R. ; Ferragud, A. ; Velázquez-Sánchez, C. ; Sotnikova, T.D. ; Morairty, S.R. ; Harmeier, A. ; Groebke Zbinden, K. ; Norcross, R.D. ; Bradaia, A. ; Kilduff, T.S. ; Biemans, B. ; Pouzet, B. ; Caron, M.G. ; Canales, J.J. ; Wallace, T.L. ; Wettstein, J.G. ; Hoener, M.C. / Trace amine-associated receptor 1 partial agonism reveals novel paradigm for neuropsychiatric therapeutics. в: Biological Psychiatry. 2012 ; стр. 934-942.

BibTeX

@article{9347ab28cbe445cda0b86b3fb9cc8713,
title = "Trace amine-associated receptor 1 partial agonism reveals novel paradigm for neuropsychiatric therapeutics.",
abstract = "BACKGROUND: Trace amines, compounds structurally related to classical biogenic amines, represent endogenous ligands of the trace amine-associated receptor 1 (TAAR1). Because trace amines also influence the activity of other targets, selective ligands are needed for the elucidation of TAAR1 function. Here we report on the identification and characterization of the first selective and potent TAAR1 partial agonist. METHODS: The TAAR1 partial agonist RO5203648 was evaluated for its binding affinity and functional activity at rodent and primate TAAR1 receptors stably expressed in HEK293 cells, for its physicochemical and pharmacokinetic properties, for its effects on the firing frequency of monoaminergic neurons ex vivo, and for its properties in vivo with genetic and pharmacological models of central nervous system disorders. RESULTS: RO5203648 showed high affinity and potency at TAAR1, high selectivity versus other targets, and favorable pharmacokinetic properties. In mouse brain slices, RO5203648 increased the",
author = "F.G. Revel and J.-L. Moreau and R.R. Gainetdinov and A. Ferragud and C. Vel{\'a}zquez-S{\'a}nchez and T.D. Sotnikova and S.R. Morairty and A. Harmeier and {Groebke Zbinden}, K. and R.D. Norcross and A. Bradaia and T.S. Kilduff and B. Biemans and B. Pouzet and M.G. Caron and J.J. Canales and T.L. Wallace and J.G. Wettstein and M.C. Hoener",
year = "2012",
doi = "10.1016/j.biopsych.2012.05.014",
language = "English",
pages = "934--942",
journal = "Biological Psychiatry",
issn = "0006-3223",
publisher = "Elsevier",

}

RIS

TY - JOUR

T1 - Trace amine-associated receptor 1 partial agonism reveals novel paradigm for neuropsychiatric therapeutics.

AU - Revel, F.G.

AU - Moreau, J.-L.

AU - Gainetdinov, R.R.

AU - Ferragud, A.

AU - Velázquez-Sánchez, C.

AU - Sotnikova, T.D.

AU - Morairty, S.R.

AU - Harmeier, A.

AU - Groebke Zbinden, K.

AU - Norcross, R.D.

AU - Bradaia, A.

AU - Kilduff, T.S.

AU - Biemans, B.

AU - Pouzet, B.

AU - Caron, M.G.

AU - Canales, J.J.

AU - Wallace, T.L.

AU - Wettstein, J.G.

AU - Hoener, M.C.

PY - 2012

Y1 - 2012

N2 - BACKGROUND: Trace amines, compounds structurally related to classical biogenic amines, represent endogenous ligands of the trace amine-associated receptor 1 (TAAR1). Because trace amines also influence the activity of other targets, selective ligands are needed for the elucidation of TAAR1 function. Here we report on the identification and characterization of the first selective and potent TAAR1 partial agonist. METHODS: The TAAR1 partial agonist RO5203648 was evaluated for its binding affinity and functional activity at rodent and primate TAAR1 receptors stably expressed in HEK293 cells, for its physicochemical and pharmacokinetic properties, for its effects on the firing frequency of monoaminergic neurons ex vivo, and for its properties in vivo with genetic and pharmacological models of central nervous system disorders. RESULTS: RO5203648 showed high affinity and potency at TAAR1, high selectivity versus other targets, and favorable pharmacokinetic properties. In mouse brain slices, RO5203648 increased the

AB - BACKGROUND: Trace amines, compounds structurally related to classical biogenic amines, represent endogenous ligands of the trace amine-associated receptor 1 (TAAR1). Because trace amines also influence the activity of other targets, selective ligands are needed for the elucidation of TAAR1 function. Here we report on the identification and characterization of the first selective and potent TAAR1 partial agonist. METHODS: The TAAR1 partial agonist RO5203648 was evaluated for its binding affinity and functional activity at rodent and primate TAAR1 receptors stably expressed in HEK293 cells, for its physicochemical and pharmacokinetic properties, for its effects on the firing frequency of monoaminergic neurons ex vivo, and for its properties in vivo with genetic and pharmacological models of central nervous system disorders. RESULTS: RO5203648 showed high affinity and potency at TAAR1, high selectivity versus other targets, and favorable pharmacokinetic properties. In mouse brain slices, RO5203648 increased the

U2 - 10.1016/j.biopsych.2012.05.014

DO - 10.1016/j.biopsych.2012.05.014

M3 - Article

SP - 934

EP - 942

JO - Biological Psychiatry

JF - Biological Psychiatry

SN - 0006-3223

ER -

ID: 8183766