Hashimoto Kenji, Ishima Tamaki, Fujita Yuko, Matsuo Masaaki, Kobashi Tatsuhiro, Takahagi Makoto, Tsukada Hideo, Iyo Masaomi
Division of Clinical Neuroscience, Chiba University Center for Forensic Mental Health, Chiba, Japan.
Biol Psychiatry. 2008 Jan 1;63(1):92-7. doi: 10.1016/j.biopsych.2007.04.034. Epub 2007 Jun 28.
Accumulating evidence suggests that alpha7 nicotinic receptor (alpha7 nAChR) agonists could be potential therapeutic drugs for cognitive deficits in schizophrenia. The present study was undertaken to examine the effects of the novel selective alpha7 nAChR agonist SSR180711 on cognitive deficits in mice after repeated administration of the N-methyl-D-aspartate receptor antagonist phencyclidine (PCP).
Saline or PCP (10 mg/kg/day for 10 days) was administered to mice. Subsequently, vehicle, SSR180711 (.3 or 3.0 mg/kg/day), SSR180711 (3.0 mg/kg/day) + the selective alpha7 nAChR antagonist methyllycaconitine (MLA; 3.0 mg/kg/day), or MLA (3.0 mg/kg/day) was administered IP for 2 consecutive weeks. Twenty-four hours after the final administration, a novel object recognition test was performed.
The PCP-induced cognitive deficits were significantly improved by subsequent subchronic (2-week) administration of SSR180711 (3.0 mg/kg). The effects of SSR180711 (3.0 mg/kg) were significantly antagonized by co-administration of MLA (3.0 mg/kg). Furthermore, Western blot analysis and immunohistochemistry revealed that levels of alpha7 nAChRs in the frontal cortex and hippocampus of the PCP (10 mg/kg/day for 10 days)-treated mice were significantly lower than those of saline-treated mice.
These findings suggest that repeated PCP administration significantly decreased the density of alpha7 nAChRs in the brain and that the alpha7 nAChR agonist SSR180711 could ameliorate cognitive deficits in mice after repeated administration of PCP. Therefore, alpha7 nAChR agonists including SSR180711 are potential therapeutic drugs for treating cognitive deficits in schizophrenic patients.
越来越多的证据表明,α7烟碱型受体(α7 nAChR)激动剂可能是治疗精神分裂症认知缺陷的潜在治疗药物。本研究旨在探讨新型选择性α7 nAChR激动剂SSR180711对反复给予N-甲基-D-天冬氨酸受体拮抗剂苯环利定(PCP)后小鼠认知缺陷的影响。
给小鼠注射生理盐水或PCP(10mg/kg/天,共10天)。随后,腹腔注射溶剂、SSR180711(0.3或3.0mg/kg/天)、SSR180711(3.0mg/kg/天)+选择性α7 nAChR拮抗剂甲基lycaconitine(MLA;3.0mg/kg/天)或MLA(3.0mg/kg/天),连续2周。最后一次给药24小时后,进行新物体识别测试。
随后亚慢性(2周)给予SSR180711(3.0mg/kg)可显著改善PCP诱导的认知缺陷。联合给予MLA(3.0mg/kg)可显著拮抗SSR180711(3.0mg/kg)的作用。此外,蛋白质免疫印迹分析和免疫组织化学显示,PCP(10mg/kg/天,共10天)处理的小鼠额叶皮质和海马中α7 nAChR的水平显著低于生理盐水处理的小鼠。
这些发现表明,反复给予PCP可显著降低脑中α7 nAChR的密度,并且α7 nAChR激动剂SSR180711可改善反复给予PCP后小鼠的认知缺陷。因此,包括SSR180711在内的α7 nAChR激动剂是治疗精神分裂症患者认知缺陷的潜在治疗药物。