title: Antipsychotic profile of 5-[2-[4-(6-fluoro-1H-indole-3-yl)piperidin-1-yl]ethyl]-4-(4-fluorophenyl)thiazole-2-carboxylic acid amide (NRA0562) in rats.
abstract: The antipsychotic profile of 5-[2-[4-(6-fluoro-1H-indole-3-yl)piperidin-1-yl]ethyl]-4-(4-fluorophenyl)thiazole-2-carboxylic acid amide (NRA0562) was investigated using the conditioned avoidance test in rats. NRA0562 is a putative "atypical" antipsychotic agent with moderate to high affinities for dopamine D(1), D(2), D(4), 5-hydroxytryptamine(2A) receptors and alpha(1) adrenoceptor. NRA0562 (1 and 3 mg/kg, p.o.) dose-dependently and significantly impaired the conditioned avoidance response. Likewise other atypical antipsychotics such as risperidone (1 and 3 mg/kg, p.o.) and clozapine (100 mg/kg, p.o.) dose-dependently and significantly impaired the conditioned avoidance response in rats. In addition, typical antipsychotics, haloperidol (1 and 3 mg/kg, p.o.) potently impaired the conditioned avoidance response.These results suggest that antipsychotic profile of NRA0562 is consistent with profiles of clozapine or risperidone and may be considered an atypical antipsychotic agent.
authors.affiliation: CNS Diseases Research, Medicinal Pharmacology Laboratory, Medicinal Research Laboratories, Taisho Pharmaceutical Co., Ltd., 1-403, Yoshino-cho, Saitama, Saitama 330-8530, Japan. k.takamori@po.rd.taisho.co.jp
authors.forename: Kazuaki
authors.initials: K
authors.lastname: Takamori
authors.forename: Takeo
authors.initials: T
authors.lastname: Funakoshi
authors.forename: Shiho
authors.initials: S
authors.lastname: Hirota
authors.forename: Shigeyuki
authors.initials: S
authors.lastname: Chaki
authors.forename: Kazuya
authors.initials: K
authors.lastname: Kameo
mesh_terms: D000818:Animals; D014150:Antipsychotic Agents / Q000494:pharmacology*; D001362:Avoidance Learning / Q000187:drug effects*; D001522:Behavior, Animal / Q000187:drug effects*; D003024:Clozapine / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D006220:Haloperidol / Q000494:pharmacology; D008297:Male; D010880:Piperidines / Q000494:pharmacology*; D051381:Rats; D017208:Rats, Wistar; D018967:Risperidone / Q000494:pharmacology; D013844:Thiazoles / Q000494:pharmacology*
chemical_list: C433508:5-(2-(4-(6-fluoro-1H-indole-3-yl)piperidine-1-yl)ethyl)-4-(4-fluorophenyl)thiazole-2-carboxylic acid amide; D014150:Antipsychotic Agents; D010880:Piperidines; D013844:Thiazoles; D003024:Clozapine; D006220:Haloperidol; D018967:Risperidone