A novel α7 nAChR agonist, 4-(5-methyloxazolo[4,5-b]pyridin-2-yl)-1,4-diazabicyclo[3.2.2]nonane (24, CP-810,123), has been identified as a potential treatment for cognitive deficits associated with psychiatric or neurological conditions including schizophrenia and Alzheimer’s disease. Compound 24 is a potent and selective compound with excellent pharmaceutical properties. In rodent, the compound displays high oral bioavailability and excellent brain penetration affording high levels of receptor occupancy and in vivo efficacy in auditory sensory gating and novel object recognition. The structural diversity of this compound and its preclinical in vitro and in vivo package support the hypothesis that α7 nAChR agonists may have potential as a pharmacotherapy for the treatment of cognitive deficits in schizophrenia.

中文翻译：

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发现一种新型的α7烟碱乙酰胆碱受体激动剂4-（5-甲基恶唑并[4,5- b ]吡啶-2-基）-1,4-二氮杂双环[3.2.2]壬烷（CP-810,123）。精神分裂症的认知障碍：合成，SAR发展和认知模型中的体内功效。

一种新型的α7nAChR激动剂4-（5-甲基恶唑并[4,5- b ]吡啶-2-基）-1,4-二氮杂双环[3.2.2]壬烷（24，CP-810,123）被鉴定为对与精神分裂症和阿尔茨海默氏病等精神病或神经病相关的认知缺陷的潜在治疗方法。化合物24是一种具有出色药物特性的强效选择性化合物。在啮齿动物中，该化合物具有很高的口服生物利用度和出色的脑部渗透性，可在听觉感觉门控和新型物体识别中提供高水平的受体占有率和体内功效。该化合物的结构多样性及其临床前和体内和体外包装均支持以下假设：α7nAChR激动剂可能具有作为治疗精神分裂症认知缺陷的药物疗法的潜力。