用于治疗疼痛的第二代P2X3拮抗剂的鉴定。
Identification of second-generation P2X3 antagonists for treatment of pain.
作者信息
Ginnetti Anthony T, Paone Daniel V, Stauffer Shaun R, Potteiger Craig M, Shaw Anthony W, Deng James, Mulhearn James J, Nguyen Diem N, Segerdell Carolyn, Anquandah Juliana, Calamari Amy, Cheng Gong, Leitl Michael D, Liang Annie, Moore Eric, Panigel Jacqueline, Urban Mark, Wang Jixin, Fillgrove Kerry, Tang Cuyue, Cook Sean, Kane Stefanie, Salvatore Christopher A, Graham Samuel L, Burgey Christopher S
机构信息
Department of Medicinal Chemistry, MRL, Merck & Co., Inc., PO Box 4, West Point, PA 19486, USA.
Department of Medicinal Chemistry, MRL, Merck & Co., Inc., PO Box 4, West Point, PA 19486, USA.
出版信息
Bioorg Med Chem Lett. 2018 May 1;28(8):1392-1396. doi: 10.1016/j.bmcl.2018.02.039. Epub 2018 Feb 21.
A second-generation small molecule P2X3 receptor antagonist has been developed. The lead optimization strategy to address shortcomings of the first-generation preclinical lead compound is described herein. These studies were directed towards the identification and amelioration of preclinical hepatobiliary findings, reducing potential for drug-drug interactions, and decreasing the projected human dose of the first-generation lead.
第二代小分子P2X3受体拮抗剂已研发成功。本文介绍了针对第一代临床前先导化合物缺点的先导优化策略。这些研究旨在识别和改善临床前肝胆方面的发现，降低药物相互作用的可能性，并降低第一代先导化合物的预计人体剂量。
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