イミダフェナシン

説明Imidafenacin, an M3/M1 muscarinic receptor antagonist, was introduced in Japan for the oral treatment of OAB. The majority of OAB symptoms are thought to result from overactivity of the detrusor muscle, which is primarily mediated by acetylcholine-induced stimulation of muscarinic M3 receptors in the bladder. Previously marketed muscarinic antagonists for OAB include propiverine, tolterodine, oxybutynin, trospium, darifenacin, and solifenacin. In vitro, imidafenacin is equally active against M1 and M3 receptors (Kb＝0.32 and 0.55nM, respectively), and approximately 10-fold less active against M2 receptors (Kb＝4.13nM). Imidafenacin is chemically synthesized in three steps starting with alkylation of diphenylacetonitrile with dibromoethane, followed by condensation with 2-methylimidazole, and hydrolysis of the cyano group to a carboxamide group with 70% sulfuric acid.

使用Imidafenacin-d10 is deutirium labelled imidafenacin which is a novel therapeutic agent for overactive bladder with antimuscarinic activity, on mediator release from urothelium and detrusor overactivity induced by cerebral infarction.