Hagiwara Hiroko, Fujita Yuko, Ishima Tamaki, Kunitachi Shinsui, Shirayama Yukihiko, Iyo Masaomi, Hashimoto Kenji
Division of Clinical Neuroscience, Chiba University Center for Forensic Mental Health, Chiba, Japan.
Eur Neuropsychopharmacol. 2008 Jun;18(6):448-54. doi: 10.1016/j.euroneuro.2007.11.005. Epub 2007 Dec 31.
Accumulating evidence suggests that the serotonin 5-HT(1A) receptor may play a role in the pathophysiology of schizophrenia. The present study was undertaken to examine the effects of perospirone, an atypical antipsychotic drug with 5-HT(1A) receptor agonism, on cognitive deficits in mice after repeated administration of the NMDA receptor antagonist phencyclidine (PCP). Subsequent subchronic (14 days) administration of perospirone (1.0, 3.0, or 10 mg/kg) significantly attenuated PCP (10 mg/kg)-induced cognitive deficits in mice, in a dose-dependent manner. The effects of perospirone (10 mg/kg) were significantly antagonized by co-administration of the selective 5-HT(1A) receptor antagonist WAY100635 (1.0 mg/kg). Furthermore, hypothermia by the 5-HT(1A) receptor agonist 8-OH DPAT (0.25 mg/kg) was significantly attenuated in mice treated with PCP. Moreover, a receptor binding assay using [(3)H]WAY100635 revealed that levels of 5-HT(1A) receptors in the hippocampus, but not in the frontal cortex, of PCP-treated mice were significantly lower than those of saline-treated mice. These findings suggest that repeated PCP administration alters 5-HT(1A) receptor function in the mouse brain, and that subsequent subchronic administration of perospirone ameliorates PCP-induced cognitive deficits via 5-HT(1A) receptors. Therefore, perospirone could be a potential therapy for the cognitive deficits observed in schizophrenic patients.
越来越多的证据表明,血清素5-HT(1A)受体可能在精神分裂症的病理生理学中发挥作用。本研究旨在探讨哌罗匹隆(一种具有5-HT(1A)受体激动作用的非典型抗精神病药物)对反复给予N-甲基-D-天冬氨酸(NMDA)受体拮抗剂苯环利定(PCP)后小鼠认知缺陷的影响。随后对小鼠进行亚慢性(14天)给予哌罗匹隆(1.0、3.0或10mg/kg),以剂量依赖的方式显著减轻了PCP(10mg/kg)诱导的小鼠认知缺陷。选择性5-HT(1A)受体拮抗剂WAY100635(1.0mg/kg)共同给药可显著拮抗哌罗匹隆(10mg/kg)的作用。此外,5-HT(1A)受体激动剂8-OH DPAT(0.25mg/kg)引起的体温过低在接受PCP治疗的小鼠中显著减轻。此外,使用[(3)H]WAY100635进行的受体结合试验表明,PCP处理小鼠海马中的5-HT(1A)受体水平显著低于生理盐水处理小鼠,但额叶皮质中的5-HT(1A)受体水平无显著差异。这些发现表明,反复给予PCP会改变小鼠大脑中的5-HT(1A)受体功能,随后亚慢性给予哌罗匹隆可通过5-HT(1A)受体改善PCP诱导的认知缺陷。因此,哌罗匹隆可能是治疗精神分裂症患者认知缺陷的一种潜在疗法。