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α7 烟碱型乙酰胆碱受体(α7 nAChR)激动剂治疗精神分裂症相关认知障碍的治疗潜力。

The therapeutic potential of α7 nicotinic acetylcholine receptor (α7 nAChR) agonists for the treatment of the cognitive deficits associated with schizophrenia.

机构信息

Department of Radiology, Stanford University School of Medicine, Stanford, CA, 94305, USA.

出版信息

CNS Drugs. 2015 Jul;29(7):529-42. doi: 10.1007/s40263-015-0260-0.

Abstract

Homomeric α7 nicotinic acetylcholine receptors (α7 nAChRs) have implications in the regulation of cognitive processes such as memory and attention, and have shown promise as a therapeutic target for the treatment of the cognitive deficits associated with schizophrenia. Multiple α7 nAChR agonists have entered human trials; however, unfavorable side effects and pharmacokinetic issues have hindered the development of a clinical α7 nAChR agonist. Currently, EVP-6124 is in phase III clinical trials, and several other α7 nAChR agonists (GTS-21 and AQW051) are in earlier stages of development. This review will summarize the recent advances and failures of α7 nAChR agonists in clinical trials for the treatment of the aforementioned pathology.

摘要

同型 α7 烟碱型乙酰胆碱受体(α7 nAChRs)在调节认知过程(如记忆和注意力)方面具有重要意义,并且已被证明是治疗与精神分裂症相关认知缺陷的有希望的治疗靶点。多种 α7 nAChR 激动剂已进入人体试验;然而,不利的副作用和药代动力学问题阻碍了临床 α7 nAChR 激动剂的发展。目前,EVP-6124 正在进行 III 期临床试验,而其他几种 α7 nAChR 激动剂(GTS-21 和 AQW051)处于开发的早期阶段。本综述将总结 α7 nAChR 激动剂在治疗上述疾病的临床试验中的最新进展和失败。

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