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MK-7622: A First-in-Class M1 Positive Allosteric Modulator Development Candidate

机译:MK-7622:一流的M <亚> 1 积极变构调制器开发候选人

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摘要

Identification of ligands that selectively activate the M_(1) muscarinic signaling pathway has been sought for decades to treat a range of neurological and cognitive disorders. Herein, we describe the optimization efforts focused on addressing key physicochemical and safety properties, ultimately leading to the clinical candidate MK-7622, a highly selective positive allosteric modulator of the M_(1) muscarinic receptor that has entered Phase II studies in patients with Alzheimer’s disease.
机译:已经寻求鉴定选择性激活M_(1)毒蕈碱信令途径的配体,几十年来治疗一系列神经和认知障碍。 在此,我们描述了焦点地理化学和安全性质的优化力,最终导致临床候选MK-7622,M_(1)毒蕈碱受体的高度选择性正变构调制剂,该受体已经进入Alzheimer患者的II期研究 疾病。

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