Anxiolytic-like effects of 4-phenyl-2-trichloromethyl-3H-1,5-benzodiazepine hydrogen sulfate in mice

Brazilian Journal of Medical and Biological Research

M.a. Rubin¹  C.a. Albach¹  D.b. Berlese¹  H.g. Bonacorso¹  S.r.t. Bittencourt¹  C.m.t. Queiroz¹  A.e. Maixner¹  C.f. Mello¹ 

[1] ,Universidade Federal de Santa Maria Centro de Ciências Naturais e Exatas Departamento de QuímicaSanta Maria RS ,Brasil

关键词: anxiolytic;    1;    5-benzodiazepine;    diazepam;    elevated plus-maze;    holeboard;    picrotoxin;   

DOI  :  10.1590/S0100-879X2000000900013

来源: SciELO

【 摘 要 】

The pharmacological effects of 4-phenyl-2-trichloromethyl-3H-1,5-benzodiazepine hydrogen sulfate (PTMB), a novel synthetic benzodiazepine, were examined in mice. In the elevated plus-maze test of anxiety, 0.3-1 mg/kg diazepam ip (F(3,53) = 3.78; P<0.05) and 1-10 mg/kg PTMB ip increased (F(5,98) = 3.26; P<0.01), whereas 2 mg/kg picrotoxin ip decreased (F(3,59) = 8.32; P<0.001) the proportion of time spent in the open arms, consistent with an anxiolytic action of both benzodiazepines, and an anxiogenic role for picrotoxin. In the holeboard, 1.0 mg/kg diazepam ip increased (F(3,54) = 2.78; P<0.05) and 2 mg/kg picrotoxin ip decreased (F(3,59) = 4.69; P<0.01) locomotor activity. Rotarod assessment revealed that 1 mg/kg diazepam ip and 3, 10 and 30 mg/kg PTMB ip produced significant motor incoordination compared to vehicle control (F(4,70) = 7.6; P<0.001). These data suggest that the recently synthesized PTMB compound possesses anxiolytic activity and produces motor incoordination similar to those observed with diazepam.

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