Дифеманила метилсульфат

Описание

Diphemanil is a quaternary ammonium anticholinergic agent. It induces relaxation of isolated guinea pig trachea strips precontracted with methacholine (EC₅₀ = 0.12 nM). Diphemanil reverses increases in lung resistance and decreases in dynamic lung compliance induced by the non-selective acetylcholine receptor agonist carbachol (carbamoylcholine; ) in vagotomized cats (ED₅₀s = 17.5 and 19.3 μg/kg, respectively). It reduces salivation induced by the muscarinic acetylcholine receptor agonist pilocarpine in mice when administered subcutaneously at doses ranging from 1.25 to 10 mg/kg.

Использование

Bronchodilatator;Anticholinergic

Определение

ChEBI: The alkene resulting from the formal Wittig olefination of benzophenone and 1,1-dimethyl-4-bromopiperidinium methylsulfate. A quaternary ammonium anticholinergic, it binds muscarinic acetycholine receptors and thereby decreases secretory excretion of stoma h acids, saliva and sweat, It is used topically in the treatment of hyperhidorsis (excessive sweating).

Общее описание

Diphemanil methylsulfate,4-(diphenylmethylene)-1,1-dimethylpiperidiniummethylsulfate (Prantal), or diphemanil methylsulfate is apotent cholinergic blocking agent. In the usual dosagerange, it acts as an effective parasympatholytic by blockingnerve impulses at the parasympathetic ganglia, but it doesnot invoke a sympathetic ganglionic blockade. It is claimedto be highly specific in its action on those innervations thatactivate gastric secretion and GI motility. Although thisdrug can produce atropine-like side effects, they rarelyoccur at recommended doses. The highly specific nature ofits action on gastric functions makes the drug useful inthe treatment of peptic ulcer, and its lack of atropine-likeeffects makes its use much less distressing than other antispasmodicdrugs. In addition to its action in decreasinggastric hypermotility, diphemanil methylsulfate is valuablein hyperhidrosis in low doses (50 mg twice daily) or topically.The drug is not well absorbed from the GI tract,particularly in the presence of food, and should be administeredbetween meals. The methylsulfate salt was chosen asthe best, because the chloride is hygroscopic and the bromideand iodide ions have exhibited toxic manifestations inclinical use.