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.
D000818:Animals; D000840:Anisoles / Q000494:pharmacology; D000927:Anticonvulsants / Q000494:pharmacology; D000929:Antidepressive Agents, Tricyclic / Q000494:pharmacology*; D001341:Autonomic Nervous System / Q000187:drug effects; D001921:Brain / Q000378:metabolism; D006897:Hydroxyindoleacetic Acid / Q000378:metabolism; D007498:Iris / Q000378:metabolism; D051379:Mice; D009043:Motor Activity / Q000187:drug effects; D009638:Norepinephrine / Q000037:antagonists & inhibitors / Q000378:metabolism; D010880:Piperidines / Q000494:pharmacology*; D051381:Rats; D012701:Serotonin / Q000378:metabolism; D012702:Serotonin Antagonists; D013574:Synaptosomes / Q000378:metabolism; D014439:Tyramine / Q000037:antagonists & inhibitors; D010133:p-Chloroamphetamine / Q000378:metabolism
D000840:Anisoles; D000927:Anticonvulsants; D000929:Antidepressive Agents, Tricyclic; D010880:Piperidines; D012702:Serotonin Antagonists; D012701:Serotonin; D006897:Hydroxyindoleacetic Acid; D010133:p-Chloroamphetamine; D009638:Norepinephrine; D014439:Tyramine