CAS No.: | 170105-16-5 |
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Formula: | C20h21n3o |
EINECS: | 689-703-7 |
Type: | Pharmaceutical Intermediates |
Appearance: | Powder |
Quality: | Technical |
Customization: |
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Product Name: Imidafenacin
Synonyms: ONO 8025;KRP-197; ONO-8025;Imidafenacin-d10;Staybla;Uritos;1H-IMidazole-1-butanaMide,2-Methyl-a,a-diphenyl-;IMidafenacin DISCONTINUED-PATENTED PRODUCT;4-(2-METHYL-1H-IMIDAZOL-1-YL)-2,2-DIPHENYLBUTANAMIDE
CAS: 170105-16-5
MF: C20H21N3O
MW: 319.4
EINECS: 689-703-7
Melting point: 96-97°C
Boiling point: 579.7±50.0 °C
Density: 1.12±0.1 g/cm3
Storage temp.: Store at RT
Appearance: White Powder
Description:
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.
Uses:
A novel therapeutic agent for overactive bladder with antimuscarinic activity, on mediator release from urothelium and detrusor overactivity induced by cerebral infarction. A muscarinic antagonist.
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