Author | Opretzka, Luíza Carolina França | |
Author | Viana, Max Denisson Maurício | |
Author | Lima, Alyne Almeida de | |
Author | Souza, Thalisson Amorim de | |
Author | Scotti, Marcus Tullius | |
Author | Tavares, Josean Fechine | |
Author | Silva, Marcelo Sobral da | |
Author | Soares, Milena Botelho Pereira | |
Author | Villarreal, Cristiane Flora | |
Access date | 2024-02-23T17:40:40Z | |
Available date | 2024-02-23T17:40:40Z | |
Document date | 2023 | |
Citation | OPRETZKA, Luíza Carolina França et al. Cleomin exerts acute antinociceptive effects in mice via GABAB and muscarinic receptors. Pharmaceuticals, v. 16, n. 11, p. 1-16, 2023. | en_US |
ISSN | 1424-8247 | en_US |
URI | https://www.arca.fiocruz.br/handle/icict/62788 | |
Sponsorship | o Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq).
Fundação de Amparo à Pesquisa do Estado da Bahia (FAPESB).
Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES). | en_US |
Language | eng | en_US |
Publisher | MDPI | en_US |
Rights | open access | en_US |
Subject in Portuguese | Cleomina | en_US |
Subject in Portuguese | Antinocicepção | en_US |
Subject in Portuguese | Receptor | en_US |
Subject in Portuguese | GABAérgico | en_US |
Subject in Portuguese | Receptor colinérgico | en_US |
Subject in Portuguese | Dor | en_US |
Subject in Portuguese | Neocalyptrocalix longifolium | en_US |
Title | Cleomin exerts acute antinociceptive effects in mice via GABAB and muscarinic receptors | en_US |
Type | Article | en_US |
DOI | 10.3390/ ph16111547 | |
Abstract | Cleomin, a 1,3-oxazolidine-2-thione, was recently isolated from Neocalyptrocalyx longifolium, a species traditionally used for treating painful conditions. Reports about the pharmacological activities of cleomin are lacking. Here, the antinociceptive effects of cleomin were investigated using mice models of pain, namely the formalin, the cold plate, and the tail flick tests. Motor integrity was assessed in the rota-rod test. Antagonism assays and in silico docking analyses were performed to investigate the putative mechanisms of action. Cleomin (12.5–25 mg/kg), at doses that did not induce motor impairment, induced dose-dependent antinociception in both early and late phases of the formalin test and reduced nociceptive behaviors in both the cold plate and tail flick tests. Pretreatments with phaclofen and atropine attenuated the antinociceptive effects of cleomin, implicating the involvement of GABAB and muscarinic receptors. In silico docking studies suggested satisfactory coupling between cleomin and GABAB and M2 receptors, hence corroborating their role in cleomin’s activity. Pretreatments with naloxone, yohimbine, bicuculline, and methysergide did not affect the antinociception of cleomin. In silico pharmacokinetics prediction showed a good drug ability profile of cleomin. In conclusion, cleomin promoted antinociception mediated by GABAB and muscarinic receptors. These findings support further investigation of the analgesic potential of cleomin. | en_US |
Affilliation | Universidade Federal da Bahia. Faculdade de Farmácia. Salvador, BA, Brasil. | en_US |
Affilliation | Universidade Federal da Bahia. Faculdade de Farmácia. Salvador, BA, Brasil. | en_US |
Affilliation | Fundação Oswaldo Cruz. Instituto Gonçalo Moniz. Salvador, BA, Brasil. | en_US |
Affilliation | Universidade Federal da Paraíba. Instituto de Pesquisas em Fármacos e Medicamentos. João Pessoa, PB, Brasil. | en_US |
Affilliation | Universidade Federal da Paraíba. Instituto de Pesquisas em Fármacos e Medicamentos. João Pessoa, PB, Brasil. | en_US |
Affilliation | Universidade Federal da Paraíba. Instituto de Pesquisas em Fármacos e Medicamentos. João Pessoa, PB, Brasil. | en_US |
Affilliation | Universidade Federal da Paraíba. Instituto de Pesquisas em Fármacos e Medicamentos. João Pessoa, PB, Brasil. | en_US |
Affilliation | Fundação Oswaldo Cruz. Instituto Gonçalo Moniz. Salvador, BA, Brasil / Universidade Federal da Paraíba. Instituto de Pesquisas em Fármacos e Medicamentos. João Pessoa, PB, Brasil / Instituto de Sistemas Avançados em Saúde. SENAI CIMATEC. Salvador, BA, Brasil. | en_US |
Affilliation | Universidade Federal da Bahia. Faculdade de Farmácia. Salvador, BA, Brasil. | en_US |
Subject | Cleomin | en_US |
Subject | Antinociception | en_US |
Subject | GABAergic receptor | en_US |
Subject | Cholinergic receptor | en_US |
Subject | Pain | en_US |
Subject | Neocalyptrocalix longifolium | en_US |
DeCS | Receptores Colinérgicos | en_US |
DeCS | Dor | en_US |