Schistosoma mansoni: species-selective response to N-chloroethyl-acetylcholine derivatives

Experimental Parasitology
W S WillcocksonG R Hillman


Three new acetylcholine mustard analogs were tested on schistosome and vertebrate neuromuscular preparations. These compounds extend a previously reported structure-activity series. The new compounds investigated include isopropyl-, cyclohexyl-, and benzyl-2-acetoxyethyl-2'-chloroethylamine (PrM, ChM, and BzM). In schistosome motor activity studies, all of the compounds caused irreversible reductions in the activity of Schistosoma mansoni after 1 hr exposure followed by 19 hr in drug-free medium. Under nonlethal conditions of dosage and exposure time, all compounds blocked carbachol-induced paralysis, indicating a possible action at schistosome cholinergic sites. All the compounds also reduced the labeling of schistosomes by dimethylaminonapthalene-5-sulfonamidoethyl dimethylamine hydrochloride (DDNS), a fluorescent ACh analog. In isolated vertebrate tissue experiments. PrM and ChM had slight agonist activity in the guinea pig ileum, and only PrM had agonist activity in the frog rectus abdominis preparation. PrM and BzM were found to antagonize ACh responses in the guinea pig ileum. Exposure of vertebrate tissues for 1 hr to high concentrations of ChM caused no long-lasting inhibition of ACh, pilocarpine, and serotonin (5HT) re...Continue Reading


Mar 1, 1966·British Journal of Pharmacology and Chemotherapy·L R BarkerA R Timms
Jun 1, 1974·British Journal of Pharmacology·A S BurgenJ M Young
Jan 1, 1974·Journal of Neurochemistry·C R Hiley, A S Burgen
Apr 8, 1972·British Medical Journal·Z FaridH A Sparks
Aug 1, 1980·Journal of Medicinal Chemistry·P R McAllisterG R Hillman
Dec 1, 1952·British Journal of Pharmacology and Chemotherapy·E BUEDING
Mar 1, 1954·British Journal of Pharmacology and Chemotherapy·J D GRAHAM, G P LEWIS

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Jan 1, 1983·Pharmacology & Therapeutics·G R Hillman
Dec 1, 1984·Parasitology·G C Coles

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