Oleanolic acid acrylate elicits antidepressant-like effect mediated by 5-HT 1A receptor

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dc.creatorFajemiroye, James Oluwagbamigbe
dc.creatorPolepally, Prabhakar R.
dc.creatorChaurasiya, Narayan D.
dc.creatorTekwani, Babu L.
dc.creatorZjawiony, Jordan K.
dc.creatorCosta, Elson Alves
dc.date.accessioned2018-09-04T12:24:52Z
dc.date.available2018-09-04T12:24:52Z
dc.date.issued2015-07
dc.description.abstractThe development of new drugs for the treatment of depression is strategic to achieving clinical needs of patients. This study evaluates antidepressant-like effect and neural mechanisms of four oleanolic acid derivatives i.e. acrylate (D1), methacrylate (D2), methyl fumarate (D3) and ethyl fumarate (D4). All derivatives were obtained by simple one-step esterification of oleanolic acid prior to pharmacological screening in the forced swimming (FS) and open field (OF) tests. Pharmacological tools like α-methyl-p-tyrosine (AMPT, catecholamine depletor), p-chlorophenylalanine (serotonin depletor), prazosin (PRAZ, selective α1-receptor antagonist), WAY-100635 (selective serotonin 5-HT 1A receptor antagonist) as well as monoamine oxidase (MAO) and functional binding assays were conducted to investigate possible neural mechanisms. In the FS test, D1 showed the most promising antidepressant-like effect without eliciting locomotor incoordination. Unlike group of mice pretreated with AMPT 100 mg/kg, PCPA 100 mg/kg or PRAZ 1 mg/kg, the effect of D1 was attenuated by WAY-100635 0.3 mg/kg pretreatment. D1 demonstrated moderate inhibition of MAO-A (IC 50 = 48.848 ± 1.935 μM), potency (pEC 50 = 6.1 ± 0.1) and intrinsic activity (E max = 26 ± 2.0%) on 5-HT 1A receptor. In conclusion, our findings showed antidepressant-like effect of D1 and possible involvement of 5-HT 1A receptor.pt_BR
dc.identifier.citationFAJEMIROYE, James O. et al. Oleanolic acid acrylate elicits antidepressant-like effect mediated by 5-HT1A receptor. Scientific Reports, Berlim, v. 2015, n. 11582, p. 1-12, July 2015.pt_BR
dc.identifier.doi10.1038/srep11582
dc.identifier.issne- 2045-2322
dc.identifier.urihttp://repositorio.bc.ufg.br/handle/ri/15815
dc.language.isoengpt_BR
dc.publisher.countryAlemanhapt_BR
dc.publisher.departmentInstituto de Ciências Biológicas - ICB (RG)pt_BR
dc.rightsAcesso Abertopt_BR
dc.titleOleanolic acid acrylate elicits antidepressant-like effect mediated by 5-HT 1A receptorpt_BR
dc.typeArtigopt_BR

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