title: Behavioural effects of thieno and pyrazolo [2,1] benzothiazepine derivatives in mice.
abstract: 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.
authors.affiliation: Departamento de Farmacología, Facultad de Farmacia, Universidad de La Laguna, La Laguna, Tenerife, Spain.
authors.forename: Maria A
authors.initials: MA
authors.lastname: Expósito-Orta
authors.forename: Luz M
authors.initials: LM
authors.lastname: Albertos
authors.forename: Victoriano
authors.initials: V
authors.lastname: Darias
authors.forename: Candelaria C
authors.initials: CC
authors.lastname: Sánchez-Mateo
mesh_terms: D006916:5-Hydroxytryptophan / Q000494:pharmacology; D000818:Animals; D014151:Anti-Anxiety Agents / Q000494:pharmacology; D000927:Anticonvulsants / Q000494:pharmacology; D000928:Antidepressive Agents / Q000494:pharmacology; D001058:Apomorphine / Q000037:antagonists & inhibitors / Q000494:pharmacology; D001522:Behavior, Animal / Q000187:drug effects*; D000697:Central Nervous System Stimulants / Q000037:antagonists & inhibitors / Q000494:pharmacology; D003913:Dextroamphetamine / Q000037:antagonists & inhibitors / Q000494:pharmacology; D018491:Dopamine Agonists / Q000494:pharmacology; D005106:Exploratory Behavior / Q000187:drug effects; D005260:Female; D006948:Hyperkinesis / Q000139:chemically induced / Q000517:prevention & control; D007035:Hypothermia / Q000139:chemically induced / Q000517:prevention & control; D008297:Male; D051379:Mice; D009125:Muscle Relaxants, Central / Q000138:chemical synthesis / Q000494:pharmacology; D011758:Pyrroles / Q000494:pharmacology*; D012640:Seizures / Q000139:chemically induced / Q000517:prevention & control; D013239:Stereotyped Behavior / Q000187:drug effects; D013841:Thiazepines / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D014151:Anti-Anxiety Agents; D000927:Anticonvulsants; D000928:Antidepressive Agents; D000697:Central Nervous System Stimulants; D018491:Dopamine Agonists; D009125:Muscle Relaxants, Central; D011758:Pyrroles; D013841:Thiazepines; C050504:tianeptine; D006916:5-Hydroxytryptophan; D001058:Apomorphine; D003913:Dextroamphetamine