EP1 antagonists for the treatment of inflammatory pain.
This review summarizes the publication and patent literature reporting on prostaglandin E(2) receptor 1 (EP(1)) antagonists from 2006 to the present. Pertinent references from 2005 are also included. New chemical entities disclosed as EP(1) antagonists are highlighted with particular focus on their potential to treat inflammatory pain. In the time period covered by this review there has been a significant increase in the number of publications describing EP(1) antagonists. Several papers detail in vivo efficacy in preclinical models of inflammatory pain and overactive bladder. It is evident that at least one molecule, if not more, has been selected as a development candidate. In addition to acidic antagonists, several research groups have detailed their efforts to identify non-acidic EP(1) antagonists. Progress in this challenging area is evident from the excellent in vitro activity that has been described to date.
Hall
Adrian
A
Neurology and Gastrointestinal Centre of Excellence for Drug Discovery, GlaxoSmithKline plc, New Frontiers Science Park North, Third Avenue, Harlow, Essex, CM19 5AW, UK. adrian.2.hall@gsk.com
Billinton
Andy
A
Giblin
Gerard M P
GM
D005260:Female; D006801:Humans; D007249:Inflammation / Q000188:drug therapy / Q000276:immunology / Q000378:metabolism; D008024:Ligands; D015394:Molecular Structure; D010146:Pain / Q000188:drug therapy / Q000276:immunology / Q000378:metabolism; D018078:Receptors, Prostaglandin E / Q000037:antagonists & inhibitors*; D058306:Receptors, Prostaglandin E, EP1 Subtype; D013329:Structure-Activity Relationship