Name | Diphemanil mesylate |
Synonyms | variton Variton prantal nivelona vagophemanil Diphemanil mesylate prantalmethylsulfate methyl hydrogen sulfate Diphemanil Methylsulfate vagophemanilmethylsulfate 4-benzhydrylidene-1,1-dimethyl-piperidin-1-ium DIPHEMANIL METHYLSULFATE (500 MG) DISCON-TINUED 4-(diphenylmethylidene)-1,1-dimethylpiperidinium methyl sulfate p-(alpha-phenylbenzylidene)-1,1-dimethylpiperidiniummethylsulfate |
CAS | 62-97-5 |
EINECS | 200-552-4 |
InChI | InChI=1/C20H24N.CH4O4S/c1-21(2)15-13-19(14-16-21)20(17-9-5-3-6-10-17)18-11-7-4-8-12-18;1-5-6(2,3)4/h3-12H,13-16H2,1-2H3;1H3,(H,2,3,4)/q+1 |
Molecular Formula | C20H24N.CH3O4S |
Molar Mass | 389.51 |
Melting Point | 194-195℃ |
Water Solubility | Soluble in water |
Appearance | powder to crystal |
Color | White to Almost white |
Storage Condition | Inert atmosphere,Store in freezer, under -20°C |
In vitro study | Diphemanil Methylsulfate exerts its effects by binding primarily to Muscarinic M3 receptors. In addition to its known antimuscarinic effect, Diphemanil Methylsulfate also has spasmolytic activity acting directly on smooth muscles. |
In vivo study | Pharmacokinetic experiments showed that the absorption of diphemanil methylsulphate was slow (tmax = 2 to 4 h) with a mean Half-Life of 8.35 h, within 48 hours the amount of drug recovered in the urine to 0.6 to 7.4 percent of the administered dose. Gastrointestinal absorption is poor, with a full bioavailability of 15% to 25%. |
Toxicity | LD50 in rats, mice, guinea pigs (mg/kg): 1107, 64, 404 orally (Margolin) |
Biological activity | Diphemanil Methylsulfate is a quaternary ammonium anticholinergic agent that can bind muscarinic acetylcholine receptor (mAchR). |
Target | Value |