Evaluation of Functional Selectivity of Haloperidol, Clozapine, and LASSBio-579, an Experimental Compound With Antipsychotic-Like Actions in Rodents, at G Protein and Arrestin Signaling Downstream of the Dopamine D2 Receptor

Autor: Lucas T. Parreiras-e-Silva, Thais E.T. Pompeu, Eliezer J. Barreiro, François Noël, Carlos A. M. Fraga, Diego A. Duarte, Rafaela R. Silva, Ricardo Menegatti, Claudio M. Costa-Neto

Publikováno v: Frontiers in Pharmacology, Vol 10 (2019)
Repositório Institucional da USP (Biblioteca Digital da Produção Intelectual)
Universidade de São Paulo (USP)
instacron:USP

LASSBio-579, an N-phenylpiperazine antipsychotic lead compound, has been previously reported as a D2 receptor (D2R) ligand with antipsychotic-like activities in rodent models of schizophrenia. In order to better understand the molecular mechanism of

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e8d896401b0f1c425259d386218fad34
https://www.frontiersin.org/article/10.3389/fphar.2019.00628/full

Functional binding assays for estimation of the intrinsic efficacy of ligands at the 5-HT1A receptor: Application for screening drug candidates

Autor: Bruna C. Moura, Thais E.T. Pompeu, François Noël

Publikováno v: Journal of Pharmacological and Toxicological Methods. 70:12-18

Introduction Determination of the intrinsic efficacy of ligands at the 5-HT 1A receptor is important for selecting drug candidates, e.g. in the case of schizophrenia where partial agonism is a favorable property shared by different atypical antipsych

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6afac54621022aa3d3b25ef29541e8c2
https://doi.org/10.1016/j.vascn.2014.03.002

LASSBio-1422: a new molecular scaffold with efficacy in animal models of schizophrenia and disorders of attention and cognition

Autor: Thais E.T. Pompeu, Camila B. Antonio, Carlos A. M. Fraga, Eliezer J. Barreiro, Vivian Herzfeldt, Thaise S. Martins, Eveline Dischkaln Stolz, Andresa Heemann Betti, Stela Maris Kuze Rates, François Noël

Publikováno v: Behavioural pharmacology. 28(1)

Aiming to identify new antipsychotic lead-compounds, our group has been working on the design and synthesis of new N-phenylpiperazine derivatives. Here, we characterized LASSBio-1422 as a pharmacological prototype of this chemical series. Adult male

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::77ba3db7755eb453456cd241b1cced01
https://pubmed.ncbi.nlm.nih.gov/27755061

Evaluation of Functional Selectivity of Haloperidol, Clozapine, and LASSBio-579, an Experimental Compound With Antipsychotic-Like Actions in Rodents, at G Protein and Arrestin Signaling Downstream of the Dopamine D2 Receptor.

Autor: Silva, Rafaela R., Parreiras-e-Silva, Lucas T., Pompeu, Thais E.T., Duarte, Diego A., Fraga, Carlos A.M., Barreiro, Eliezer J., Menegatti, Ricardo, Costa-Neto, Claudio M., Noël, François

Publikováno v: Frontiers in Pharmacology; 6/4/2019, pN.PAG-N.PAG, 10p