Effects of dansylated acetylcholine analogs on Schistosoma mansoni.
A series of dansylated fluorescent analogs was synthesized and tested for cholinergic and anticholinergic activity in Schistosoma mansoni. The compounds were compared with a previously reported analog, 5-(dimethylamino)-N-(2-dimethylaminoethyl)naphthalenesulfonamide hydrochloride (I). All of the compounds produced some fluorescent labeling of a structure in the head region of the worms. Major differences were not seen among the compounds. The compounds also were tested as antagonists of carbachol-induced paralysis in an activity monitor. Significant carbachol antagonism was seen for all compounds. Effects on the serotonin response also were recorded. Only one compound, a dibutylaminopropylamine derivative, produced striking antagonism of serotonin-induced motor activity.
D000109:Acetylcholine / Q000031:analogs & derivatives* / Q000037:antagonists & inhibitors; D000818:Animals; D001665:Binding Sites; D002217:Carbachol / Q000037:antagonists & inhibitors / Q000494:pharmacology; D003619:Dansyl Compounds / Q000494:pharmacology*; D051379:Mice; D009068:Movement / Q000187:drug effects; D010276:Parasympatholytics / Q000494:pharmacology; D012550:Schistosoma mansoni / Q000187:drug effects*; D012701:Serotonin; D012702:Serotonin Antagonists; D012995:Solubility; D013050:Spectrometry, Fluorescence; D013329:Structure-Activity Relationship
D003619:Dansyl Compounds; D010276:Parasympatholytics; D012702:Serotonin Antagonists; D012701:Serotonin; D002217:Carbachol; D000109:Acetylcholine