Neurochemical and pharmacological studies on a new 5HT-uptake inhibitor, FG4963, with potential antidepressant properties.

A new phenylpiperidine derivative, FG4963, and several tricyclic antidepressants were compared in various in vitro and in vivo tests for central 5HT- and NA-uptake inhibition. FG4963 was found to be a 5HT-pump blocker with activity similar to that of chlorimipramine. FG4963 inhibited NA-uptake less than the most potent tricyclic thymoleptics. In contrast to imipramine derivatives FG4963 was a weak inhibitor of peripheral NA-uptake. FG4963 seems to produce central 5HT-potentiation without affecting organ functions regulated by the autonomic nervous system as much as tricyclic antidepressants.