Masupirdine free base (SUVN-502 free base) 是一种有效的，选择性的，具有口服生物可利用且可穿透脑屏障的5-HT6 受体拮抗剂 (对人 5-HT6 受体的 Ki 为 2.04 nM)。Masupirdine free base (SUVN-502 free base) 对 5-HT2A 受体和其他 100个 靶点显示高选择性，有治疗阿尔茨海默病的潜力。
Masupirdine free base (SUVN-502 free base) is a potent, selective, orally bioavailable, and brain penetrant 5-HT6 receptor antagonist (Ki of 2.04 nM for human 5-HT6 receptor). Masupirdine free base (SUVN-502 free base) shows high selectivity over 5-HT2A receptor and other 100 target sites, and has potential for treatment of Alzheimer's disease[1]. Ki: 2.04 nM (human 5-HT6 receptor)[1]
[1]. Nirogi R, et al. Discovery and Development of 1-[(2-Bromophenyl)sulfonyl]-5-methoxy-3-[(4-methyl-1-piperazinyl)methyl]-1H-indole Dimesylate Monohydrate (SUVN-502): A Novel, Potent, Selective and Orally Active Serotonin 6 (5-HT6) Receptor Antagonist for Potential Treatment of Alzheimer's Disease. J Med Chem. 2017 Mar 9;60(5):1843-1859.
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