Behavioural effects of thieno and pyrazolo [2,1]
benzothiazepine derivatives in mice

Exposito-Orta MA, Albertos LM,
Darias V, Sanchez-Mateo CC.
Departamento de Farmacologia,
Facultad de Farmacia,
Universidad de La Laguna,
La Laguna, Tenerife, Spain.
Arzneimittelforschung. 2004;54(7):365-70.


Behavioural studies were conducted in mice with a number of hetero[2,1]benzothiazepine derivatives, analogues of tianeptine. Previously published studies in mice have shown that some of these compounds were effective in the tetrabenazine and Porsolt tests. In the present study, four of the 15 compounds under study potentiated the actions of 5-hydroxytryptophan (5-HTP, 50 mg/kg i.p.), but no significant antagonism of the apomorphine (16 mg/kg s.c.)-induced hypothermia and potentiation of the amphetamine actions was found. Moreover, some of them inhibited the stereotyped behaviour and/or climbing behaviour of low doses of apomorphine and compound 2 was effective in the plus-maze test. These compounds also produced a slight inhibition of exploratory behaviour in the holeboard test. On the other hand, no significant muscle relaxant and anticonvulsant activities were observed at any dose employed. Together, these data suggest that some of the compounds under study combine the antidepressant effects with additional neuroleptic or anxiolytic activities in mice.
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