2. Academic Validation
  3. Identification of second-generation P2X3 antagonists for treatment of pain

Identification of second-generation P2X3 antagonists for treatment of pain

  • Bioorg Med Chem Lett. 2018 May 1;28(8):1392-1396. doi: 10.1016/j.bmcl.2018.02.039.
Anthony T Ginnetti 1,  Daniel V Paone 2,  Shaun R Stauffer 2,  Craig M Potteiger 2,  Anthony W Shaw 2,  James Deng 2,  James J Mulhearn 2,  Diem N Nguyen 2,  Carolyn Segerdell 2,  Juliana Anquandah 3,  Amy Calamari 3,  Gong Cheng 3,  Michael D Leitl 3,  Annie Liang 3,  Eric Moore 3,  Jacqueline Panigel 3,  Mark Urban 3,  Jixin Wang 3,  Kerry Fillgrove 4,  Cuyue Tang 4,  Sean Cook 3,  Stefanie Kane 3,  Christopher A Salvatore 3,  Samuel L Graham 2,  Christopher S Burgey 2
Affiliations

Affiliations

  • 1 Department of Medicinal Chemistry, MRL, Merck & Co., Inc., PO Box 4, West Point, PA 19486, USA. Electronic address: anthony_ginnetti@merck.com.
  • 2 Department of Medicinal Chemistry, MRL, Merck & Co., Inc., PO Box 4, West Point, PA 19486, USA.
  • 3 Department of Pain Research, MRL, Merck & Co., Inc., PO Box 4, West Point, PA 19486, USA.
  • 4 Department of Drug Metabolism, MRL, Merck & Co., Inc., PO Box 4, West Point, PA 19486, USA.
PMID: 29548573 DOI: 10.1016/j.bmcl.2018.02.039
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

Drug-drug interaction; P2X3; Pain; Purinergic receptor; UGT1A1.

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