Zetidoline, a specific dopamine antagonist devoid of antiserotonergic activity in rodent brain.
In the present study the interaction of zetidoline, a new antipsychotic, with the serotonergic system of the rodent brain was investigated in comparison with known neuroleptics. The pharmacological tests were L-5-hydroxytryptophan syndrome in mice and tryptamine-induced clonic seizures in rats. Biochemical tests were the in vitro binding of 3H-zetidoline to rat brain membranes and the serotonin metabolism and turnover in vivo in the rat cerebral cortex and brainstem. The results indicate that zetidoline, unlike haloperidol and chlorpromazine, at doses higher than those active on the dopaminergic system, shows no or very weak antiserotonergic activity in behavioral tests.
Pugnetti
P
P
Barone
D
D
Peruzzi
M
M
Restelli
A
A
D006916:5-Hydroxytryptophan / Q000494:pharmacology; D000818:Animals; D014150:Antipsychotic Agents / Q000378:metabolism / Q000494:pharmacology*; D001667:Binding, Competitive; D001921:Brain / Q000378:metabolism*; D002746:Chlorpromazine / Q000494:pharmacology; D018492:Dopamine Antagonists; D006220:Haloperidol / Q000494:pharmacology; D007093:Imidazoles / Q000378:metabolism / Q000494:pharmacology*; D066298:In Vitro Techniques; D008297:Male; D051379:Mice; D051381:Rats; D011919:Rats, Inbred Strains; D012018:Reflex / Q000187:drug effects; D012640:Seizures / Q000139:chemically induced / Q000378:metabolism; D012701:Serotonin / Q000378:metabolism*; D012702:Serotonin Antagonists; D013134:Spiperone / Q000494:pharmacology; D013570:Synaptic Membranes / Q000378:metabolism
D014150:Antipsychotic Agents; D018492:Dopamine Antagonists; D007093:Imidazoles; D012702:Serotonin Antagonists; D012701:Serotonin; C027277:zetidoline; D013134:Spiperone; D006916:5-Hydroxytryptophan; D006220:Haloperidol; D002746:Chlorpromazine