title: Antipsychotic properties of new N-(4-substituted-1-piperazinylethyl)- and N-(4-substituted-1-piperidinylethyl)-phthalimides.
abstract: A series of N-(4-phenyl- and 4-pyridyl-1-piperazinylethyl)- and N-(4-phenyl-1-piperidinylethyl)-phthalmides were synthesized and tested for antipsychotic activity. All compounds suppressed the spontaneous motor activity and the apomorphine-induced climbing in mice and pergolide-induced locomotor activity in rats, demonstrating psychotropic properties equal to the corresponding properties of sulpiride. Although the compounds, like sulpiride, were less potent than haloperidol in blocking the locomotor activities, they caused no catalepsy, a major side effect following treatment with conventional antipsychotic agents. It is likely that the new compounds produce their neuroleptic activities through inhibition of limbic dopamine receptors.
authors.affiliation: College of Pharmacy, Department of Pharmaceutical Chemistry, King Saud University, Riyadh, Saudi Arabia.
authors.forename: K A
authors.initials: KA
authors.lastname: al-Rashood
authors.forename: A A
authors.initials: AA
authors.lastname: Mustafa
authors.forename: A A
authors.initials: AA
authors.lastname: Alhaider
authors.forename: O T
authors.initials: OT
authors.lastname: Ginawi
authors.forename: A A
authors.initials: AA
authors.lastname: Madani
authors.forename: H A
authors.initials: HA
authors.lastname: el-Obeid
mesh_terms: D000818:Animals; D014150:Antipsychotic Agents / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D001058:Apomorphine / Q000494:pharmacology; D002375:Catalepsy / Q000139:chemically induced; D055598:Chemical Phenomena; D002621:Chemistry; D005260:Female; D006168:Guinea Pigs; D007928:Lethal Dose 50; D008297:Male; D051379:Mice; D009043:Motor Activity / Q000187:drug effects; D010276:Parasympatholytics / Q000138:chemical synthesis; D010479:Pergolide / Q000494:pharmacology; D010797:Phthalimides / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D010879:Piperazines / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D010880:Piperidines / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D051381:Rats; D011919:Rats, Inbred Strains; D013239:Stereotyped Behavior / Q000187:drug effects
chemical_list: D014150:Antipsychotic Agents; D010276:Parasympatholytics; D010797:Phthalimides; D010879:Piperazines; D010880:Piperidines; D010479:Pergolide; D001058:Apomorphine