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

• Main Authors: M.A. Rubin, C.A. Albach, D.B. Berlese, H.G. Bonacorso, S.R.T. Bittencourt, C.M.T. Queiroz, A.E. Maixner, C.F. Mello
• Format: Article
• Language: English
• Published: Associação Brasileira de Divulgação Científica 2000-09-01
• Series: Brazilian Journal of Medical and Biological Research
• Subjects: anxiolytic; 1,5-benzodiazepine; diazepam; elevated plus-maze; holeboard; picrotoxin
• Online Access: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2000000900013
• ISSN: 0100-879X; 1414-431X

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.