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Anxiolytic Properties of New Chemical Entity, 5TIO1

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Abstract

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.

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Acknowledgments

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.

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Authors and Affiliations

  1. Department of Biochemistry and Pharmacology, Federal University of Piaui, Teresina, Piaui, Brazil

    Amanda C. Fortes, Antonia Amanda C. Almeida & Rivelilson M. Freitas

  2. Department of Biological Sciences, State University of Paraiba, João Pessoa, Paraiba, Brazil

    Francisco Jaime B. Mendonça-Júnior

  3. Department of Pharmaceutical Sciences, Federal University of Pernambuco, Recife, Pernambuco, Brazil

    José Lamartine Soares-Sobrinho & Monica Felts de La Roca Soares

  4. Programa de Pós-Graduação em Ciências Farmacêuticas/Núcleo de Tecnologia Farmacêutica do Centro de Ciências da Saúde da Universidade Federal do Piauí, Ininga, Teresina, Piauí, CEP 64.049-550, Brazil

    Rivelilson M. Freitas

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  1. Amanda C. Fortes
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  2. Antonia Amanda C. Almeida
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  3. Francisco Jaime B. Mendonça-Júnior
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Correspondence to Rivelilson M. Freitas.

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Fortes, A.C., Almeida, A.A.C., Mendonça-Júnior, F.J.B. et al. Anxiolytic Properties of New Chemical Entity, 5TIO1. Neurochem Res 38, 726–731 (2013). https://doi.org/10.1007/s11064-013-0970-y

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  • DOI: https://doi.org/10.1007/s11064-013-0970-y

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