Diphemanil Methylsulfate (Synonyms: NSC 41725)

Diphemanil methylsulfate is a quaternary ammonium anticholinergic. It binds muscarinic acetycholine receptors and thereby decreases secretory excretion of stomach acids as well as saliva and sweat.IC50 value: Target: mAChRDiphemanil Methylsulfate exerts its action by primarily binding the muscarinic M3 receptor. M3 receptors are located in the smooth muscles of the blood vessels, as well as in the lungs. This means they cause vasodilation and bronchoconstriction. They are also in the smooth muscles of the gastrointestinal tract (GIT), which help in increasing intestinal motility and dilating sphincters. The M3 receptors are also located in many glands which help to stimulate secretion in salivary glands and other glands of the body.

References:
[1]. Küng M, Diamond L. Effect of inhaled diphemanil methylsulfate, a parasympatholytic agent, on histamine induced bronchoconstriction in asymptomatic asthmatics. Ann Allergy. 1984 Jan;52(1):22-5.
[2]. Vidal AM, Rey E, Pons G et al. Pharmacokinetics of diphemanil methylsulphate in healthy subjects. Eur J Clin Pharmacol. 1992;42(6):689-91.
[3]. Vidal AM, Chéron G, Rey E et al. Pharmacokinetics of diphemanil methylsulphate in infants. Eur J Clin Pharmacol. 1993;45(1):89-91.
[4]. Chéron G, Vidal AM, Rey E et al. [Pharmacokinetics of diphemanil methylsulfate in infants]. Arch Pediatr. 1994 Jan;1(1):33-7.
[5]. Adamantidis M, Dumotier B, Caron J, Dupuis B. [Electrophysiologic effects and arrhythmogenic potential of diphemanil methylsulfate on rabbit purkinje fibers. Correlations with clinical observations of QT prolongation in pediatrics]. Arch Mal Coeur Vaiss. 1998 Dec;91(12):1487-94.