[Pharmacological studies of an antipschotic agent, penfluridol. (1). The central pharmacological actions].
Neuropharmacological properties of penfluridol (TLP-607) were investigated in experimental animals and were compared with those of haloperidol and chlorpromazine. Locomotor activity of mice significantly decreased at doses of 16-32 mg/kg p.o. Like haloperidol and chlorpromazine, TLP-607 (4-16 mg/kg p.o.) demonstrated catalepsy lasting for 48-72 hr in rats. TLP-607 strongly inhibited apomorphine-induced emesis in dogs and the ED50 was 0.016 mg/kg p.o. This effect lasted for 192 hr when administered 0.04 mg/kg p.o. TLP-607 antagnonized methamphetamine-induced stereotyped behavior in rats, and the ED50 was 1.83 ng/kg p.o. TLP-607 also inhibited conditioned avoidance responses in rats, and the ED50's in the pole climbing and Sidman avoidance methods were 6.73 and 3.4 mg/kg p.o., respectively. TLP-607 neither inhibited motor coordination nor enhanced hexobarbital-induced anesthesia in mice. These results suggest that TLP-607 is a potent and long-acting antipsychotic drug which has less neurotoxic side-effects.
D000378:Agonistic Behavior / Q000187:drug effects; D000818:Animals; D001058:Apomorphine / Q000037:antagonists & inhibitors; D001362:Avoidance Learning / Q000187:drug effects; D001763:Blepharoptosis / Q000139:chemically induced; D001831:Body Temperature / Q000187:drug effects; D002375:Catalepsy / Q000139:chemically induced; D002415:Cats; D002490:Central Nervous System / Q000187:drug effects*; D002746:Chlorpromazine / Q000494:pharmacology; D003214:Conditioning, Classical / Q000187:drug effects; D003299:Cooperative Behavior / Q000187:drug effects; D004285:Dogs; D004305:Dose-Response Relationship, Drug; D004357:Drug Synergism; D005260:Female; D006220:Haloperidol / Q000494:pharmacology; D000882:Haplorhini; D006591:Hexobarbital / Q000494:pharmacology; D006801:Humans; D008124:Locomotion / Q000187:drug effects; D008297:Male; D008694:Methamphetamine / Q000037:antagonists & inhibitors; D051379:Mice; D010276:Parasympatholytics; D010395:Penfluridol / Q000494:pharmacology*; D010880:Piperidines / Q000494:pharmacology*; D051381:Rats
D010276:Parasympatholytics; D010880:Piperidines; D010395:Penfluridol; D008694:Methamphetamine; D006591:Hexobarbital; D006220:Haloperidol; D001058:Apomorphine; D002746:Chlorpromazine