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Identification of second-generation P2X3 antagonists for treatment of pain |
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| Authors: | Anthony T Ginnetti Daniel V Paone Shaun R Stauffer Craig M Potteiger Anthony W Shaw James Deng James J Mulhearn Diem N Nguyen Carolyn Segerdell Juliana Anquandah Amy Calamari Gong Cheng Michael D Leitl Annie Liang Eric Moore Jacqueline Panigel Mark Urban Jixin Wang Christopher S Burgey |
| Institution: | 1. Department of Medicinal Chemistry, MRL, Merck & Co., Inc., PO Box 4, West Point, PA 19486, USA;2. Department of Pain Research, MRL, Merck & Co., Inc., PO Box 4, West Point, PA 19486, USA;3. Department of Drug Metabolism, MRL, Merck & Co., Inc., PO Box 4, West Point, PA 19486, USA |
| Abstract: | 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. |
| Keywords: | P2X3 Pain UGT1A1 Drug-drug interaction Purinergic receptor |
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