Kunitachi Shinsui, Fujita Yuko, Ishima Tamaki, Kohno Mami, Horio Mao, Tanibuchi Yuko, Shirayama Yukihiko, Iyo Masaomi, Hashimoto Kenji
Division of Clinical Neuroscience, Chiba University Center for Forensic Mental Health, Chiba, Japan.
Brain Res. 2009 Jul 7;1279:189-96. doi: 10.1016/j.brainres.2009.05.004. Epub 2009 May 9.
This study was undertaken to examine the effects of two acetylcholinesterase inhibitors (donepezil and physostigmine) on cognitive deficits in mice after repeated administration of the NMDA receptor antagonist phencyclidine (PCP). In the novel object recognition test, PCP (10 mg/kg/day for 10 days)-induced cognitive deficits were significantly improved by subsequent subchronic (14 days) administration of donepezil (1.0 mg/kg/day), but not donepezil (0.1 mg/kg/day). Furthermore, the effect of donepezil (1.0 mg/kg/day) on PCP-induced cognitive deficits was significantly antagonized by co-administration of the selective sigma-1 receptor antagonist NE-100 (1.0 mg/kg/day), suggesting the role of sigma-1 receptors in the active mechanisms of donepezil. In contrast, PCP-induced cognitive deficits were not improved by subsequent subchronic (14 days) administration of physostigmine (0.25 mg/kg/day). Moreover, repeated administration of PCP significantly caused the reduction of sigma-1 receptors in the hippocampus. The present study suggests that agonistic activity of donepezil at sigma-1 receptors plays a role in the active mechanisms of donepezil on PCP-induced cognitive deficits in mice. Therefore, it is likely that donepezil would be potential therapeutic drugs for the treatment of the cognitive deficits in schizophrenia.
本研究旨在探讨两种乙酰胆碱酯酶抑制剂(多奈哌齐和毒扁豆碱)对反复给予N-甲基-D-天冬氨酸(NMDA)受体拮抗剂苯环己哌啶(PCP)的小鼠认知缺陷的影响。在新颖物体识别试验中,PCP(10毫克/千克/天,共10天)诱导的认知缺陷通过随后亚慢性(14天)给予多奈哌齐(1.0毫克/千克/天)得到显著改善,但多奈哌齐(0.1毫克/千克/天)则无此效果。此外,多奈哌齐(1.0毫克/千克/天)对PCP诱导的认知缺陷的作用被选择性σ-1受体拮抗剂NE-100(1.0毫克/千克/天)共同给药显著拮抗,表明σ-1受体在多奈哌齐的作用机制中发挥作用。相比之下,PCP诱导的认知缺陷并未因随后亚慢性(14天)给予毒扁豆碱(0.25毫克/千克/天)而得到改善。此外,反复给予PCP显著导致海马中σ-1受体减少。本研究表明,多奈哌齐对σ-1受体的激动活性在其对PCP诱导的小鼠认知缺陷的作用机制中发挥作用。因此,多奈哌齐可能是治疗精神分裂症认知缺陷的潜在治疗药物。