Psychopharmacological Effects of Tianeptine Analogous Hetero[2,1] benzothiazepine Derivatives

The psychopharmacological effects of a number of thieno and pyrazolo[2,1] benzothiazepine derivatives as well as several synthetic intermediate compounds were investigated in mice. Previously published studies in mice have shown that some of these compounds were effective in the tetrabenazine and Porsolt tests. In the present study, 7 of the 15 compounds under study clearly antagonized the apomorphine (16 mg/kg s.c.)-induced hypothermia, but no significant potentiation of the 5-hydroxytryptophan (5-HTP) and amphetamine actions was found. Five of them inhibited the syndrome induced by 5-HTP (250 mg/kg i.p.). Moreover, some of them were effective in the plus-maze test and antagonized the apomorphine (3 mg/kg s.c.)-induced effects. On the other hand, these compounds produced a moderate inhibition of exploratory behaviour in the holeboard test, but they had no significant muscle relaxant and anticonvulsant activities. The results indicate that some of the compounds under study combine a spectrum of antidepressant, anxiolytic and neuroleptic properties in mice with a lack of muscle relaxant and anticonvulsant activities.