|
|||||
|
|
Identification of second-generation P2X3 antagonists for treatment of pain |
|
| 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 |
| Affiliation: | 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 |
| 本文献已被 ScienceDirect 等数据库收录！ | |