Anxiolytic Properties of New Chemical Entity, 5TIO1
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2-[(2,6-dichlorobenzylidene)amino]-5,6-dihydro-4H-cyclopenta[b]thiophene-3-carbonitrile), 5TIO1, is a new 2-aminothiophene derivative with a promising pharmacological activity. The aim of this work was to evaluate the potential anxiolytic effect of 5TIO1 in animal models. In the elevated plus-maze test, 5TIO1 (0.1, 1.0 and 10.0 mg/kg, i.p) increased the time of permanence and the number of entries in the open arms. In the light/dark box test, 5TIO1 at dose of 0.1 mg/kg (i.p) also showed anxiolytic-like effect indicated by an increase in the time spent in the light box, similar to diazepam 2.0 mg/kg (i.p). 5TIO1 groups did not change locomotor and coordination activities in open field and rotarod tests, respectively, when compared to vehicle. Dose dependent process was not observed and the anxiolytic effects demonstrated were not completely reversed by flumazenil 25 mg/kg (i.p). Our results suggest that 5TIO1 can bind with other receptors, besides the benzodiazepine site of the GABA receptor in mouse brain.
KeywordsThiophene Anxiety Plus-maze Light/dark box Mice
We would like to thank the National Council of Technological and Scientific Development (CNPq/Brazil), Coordination for the Improvement of Higher Level Personnel (CAPES), the Research Supporting Foundation of State of Piaui (FAPEPI/Brazil) and the Development Program of the Research and Post-graduation of the State University of Paraiba (PROPESQ-UEPB) for financial support, and Dr. Paulo Michel Pinheiro Ferreira (UFPI, Department of Biological Sciences, Picos, Piauí) for English edition.
- 11.Amr AE-GE, Sherif MH, Assy MG, Al-Omar MA, Ragab I (2010) Antiarrythmic, serotonin antagonist and antianxiety activities of novel substituted thiophene derivatives synthesized from 2-amino-4,5,6,7-tetrahydro-N-phenylbenzol[b]thiophene-3-carboxamide. Eur J Med Chem 45:5935–5942. doi: 10.1016/j.ejmech.2010.09.059 CrossRefGoogle Scholar
- 12.Mendonça-Junior FJB, Lima-Neto RG, Oliveira TG, Lima MCA, Pitta IR, Galdino SL, Cruz RMD, Araújo RSA, Neves RP (2011) Synthesis and evaluation of the antifungal activity of 2-(substituted-amino)-4,5-dialkyl-thiophene-3-carbonitrile derivatives. Lat Am J Pharm 30:1492–1499Google Scholar
- 16.Carlini EA, Burgos V (1979) Screening farmacológico de ansiolíticos: metodologia laboratorial e comparação entre o diazepam e o clorobenzapam. Rev Assoc Bras Psiquiatr 1:25–31Google Scholar
- 26.Wierońska JM, Śmiałowska M, Brański P, Gasparini F, Kłodzińska A, Szewczyk B, Pałucha A, Chojnacka-Wójcik E, Pilic A (2004) In the amygdala anxiolytic action of mGlu5 receptors antagonist MPEP involves neuropeptide Y but not GABAA signaling. Neuropsychopharmacology 29:514–521. doi: 10.1038/sj.npp.1300322 PubMedCrossRefGoogle Scholar