PMID: 2483312Oct 1, 1989Paper

Inhibition of immunological histamine release from guinea pig lungs and other organs by mepyramine, ketotifen, and picumast in vivo.

Arzneimittel-Forschung
L Sekardi, K D Friedberg

Abstract

The effect of mepyramine, ketotifen and picumast (3,4-dimethyl-7-[4-(4-chlorobenzyl)piperazine-1-yl]propoxycoumarin dihydrochloride) on anaphylactic histamine release from lungs, heart, stomach, and intestine of guinea pigs in response to antigen was examined in vivo. When sensitized animals were pretreated intraperitoneally with a single dose of these compounds 60 min before i.v. antigen challenge (native ovalbumin 20 mg/kg), a dose related inhibition of immunological histamine release from the lung was established. After pretreatment of the animals with 3 mg/kg of mepyramine, 10 mg/kg of ketotifen, and 6 mg/kg of picumast dihydrochloride, the inhibitory effect on histamine release from the lung was so marked that both the acute and the protracted anaphylactic shock were completely suppressed. The corresponding histamine levels in blood plasma, regularly measured 1.5 min after antigen stimulation, had dropped to about 40%, 50%, and 35%, respectively (p less than 0.05), whereas lung histamine content increased by about 60%, 150%, and 90% compared with unpretreated, shocked controls. According to these findings the number of lung mast cells in protected animals was significantly increased. In addition, ketotifen significantly re...Continue Reading

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