Maprotiline: an antidepressant with an unusual pharmacological profile.

摘要: Maprotiline, which differs from other typical tricyclic antidepressants for its tetracyclic structure, is a highly selective inhibitor of norepinephrine reuptake. Despite in vitro and vivo inhibitory activity on NE uptake, 21 repeated daily injections maprotiline (20 mg/kg i.p.) neither attenuated the norepinephrine-stimulated cAMP accumulation nor reduced number beta adrenergic recognition sites rat frontal cortex. Also, brain serotonin2 labeled by [3H]ketanserin remained virtually unchanged rats receiving maprotiline. [3H]Desmethylimipramine [3H]mianserin specific binding were also unmodified injections. However, after 3 weeks administrations, elicited significant decrease [3H]flunitrazepam apparent affinity [3H]beta-carboline ethylester to crude synaptic membranes prepared hippocampal hypothalamic homogenates. These changes appear be unrelated modifications concentration endogenous gamma-aminobutyric acid present membrane preparation, since addition 100 microM bicuculline incubation mixture decreases same extent saline- maprotiline-treated rats. It suggested that may elicit an increase tissue levels substance(s) binds benzodiazepine/beta-carboline sites.