Effects of calmodulin antagonists on human adenoidal mast cells.
N-(6-aminohexyl)-1-naphthalenesulfonamide (W5), N-(6-aminohexyl)-5-chloro-1-naphthalenesulfonamide (W7) and Triflupromazine (TFPr) are substances with calmodulin antagonistic properties. All of these compounds inhibited the Con A-induced histamine release from human adenoidal mast cells. Maximal inhibition for W5 was observed at 200 microM, for W7 at 50 microM and for TFPr at 20 microM. Higher concentrations of each substance induced a marked histamine release. The kinetics of the mediator release were found to be different for Con A and W7 only after 5 mins incubation. The kinetics of TFPr were found to be biphasic: a slow onset was followed by a fast release reaction.
Institut für Pharmakologie, Medizinische Fakultät, RWTH Aachen, FRG.
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Bent
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Braam
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Schmutzler
D000234:Adenoids / Q000166:cytology; D002147:Calmodulin / Q000037:antagonists & inhibitors*; D003208:Concanavalin A / Q000494:pharmacology; D006636:Histamine Release / Q000187:drug effects*; D006801:Humans; D066298:In Vitro Techniques; D007700:Kinetics; D008407:Mast Cells / Q000187:drug effects / Q000378:metabolism*; D013449:Sulfonamides / Q000494:pharmacology; D014273:Triflupromazine / Q000494:pharmacology
D002147:Calmodulin; D013449:Sulfonamides; D003208:Concanavalin A; C017967:W 7; C034700:N-(6-aminohexyl)-1-naphthalenesulfonamide; D014273:Triflupromazine