Imidafenacin Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
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 (K
b=0.32 and
0.55nM, respectively), and approximately 10-fold less active against M2 receptors
(K
b=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.
Chemische Eigenschaften
White Solid
Verwenden
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.
Nebenwirkungen
Like all medicines, imidafenacin can cause side effects, but not everybody will experience them. This drug can cause sleepiness, blurred vision, stomach upset, constipation, and increased triglyceride levels.
Imidafenacin Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte