Výsledky vyhledávání - "Thais E.T. Pompeu"

Akademický článek

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

Publikováno v: Frontiers in Pharmacology, Vol 10 (2019)

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://doaj.org/article/f45cf0135861424db33630b83e2d0e5f

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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

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

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Partial agonism and fast dissociation of LASSBio-579 at dopamine D2 receptor

Autor: Thais E.T. Pompeu, Barbara Bosier, François Noël, Emmanuel Hermans, Carlos A. M. Fraga, Fernando M. do Monte, Ricardo Menegatti, Eliezer J. Barreiro

Publikováno v: Progress in Neuro-Psychopharmacology and Biological Psychiatry. 62:1-6

In an attempt to better understand the molecular mechanism of action of the antipsychotic lead LASSBio-579 and of its main metabolite LQFM 037, the aim of this work was to evaluate their intrinsic activity and binding kinetics at the dopamine D2 rece

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4d3db42bb69ee3982d36b7e7a4640877

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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

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Biotransformation of LASSBio-579 and pharmacological evaluation of p -hydroxylated metabolite a N -phenylpiperazine antipsychotic lead compound

Autor: Teresa Dalla Costa, Camila B. Antonio, Tatiana F. Gomes, Thais E.T. Pompeu, Eric de Souza Gil, Stela Maris Kuze Rates, Carlos A. M. Fraga, Carolina Horta Andrade, José R. Sabino, Eliezer J. Barreiro, Ricardo Menegatti, Andresa Heemann Betti, Daniel Alencar Rodrigues, François Noël, Valéria de Oliveira

Publikováno v: European Journal of Medicinal Chemistry. 62:214-221

Using a combination of docking and molecular dynamics simulations, we predicted that p-hydroxylation by CYP1A2 would be the main metabolic pathway for the 1-[1-(4-chlorophenyl)-1H-4pyrazolylmethyl] phenylhexahydropiperazine, LASSBio-579 (3). As the r

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::eb4563ededee11799ef4cc174394602c
https://doi.org/10.1016/j.ejmech.2012.08.011

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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

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Synthesis and pharmacological evaluation of new N-phenylpiperazine derivatives designed as homologues of the antipsychotic lead compound LASSBio-579

Autor: Eliezer J. Barreiro, Carolina D.M. Figueiredo, Carlos A. M. Fraga, Stela Maris Kuze Rates, Fernando Rodrigues de Sa Alves, Camila B. Antonio, François Noël, Vivian Herzfeldt, Bruna C. Moura, Thais E.T. Pompeu

Publikováno v: European journal of medicinal chemistry. 66

In an attempt to increase the affinity of our antipsychotic lead compound LASSBio-579 (1-((1-(4-chlorophenyl)-1H-pyrazol-4-yl)methyl)-4-phenylpiperazine; ( 2 )) for the 5-HT 2A receptor, we synthesized five new N -phenylpiperazine derivatives using a

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c20f4f1699334dd19327ea1a836142ae
https://pubmed.ncbi.nlm.nih.gov/23792350

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