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Gen Pharmacol. 1997 Feb;28(2):237-43.

Inhibitory effects of caffeine on Ca2+ influx and histamine secretion independent of cAMP in rat peritoneal mast cells.

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Department of Toxicology, School of Veterinary Medicine, Rakuno Gakuen University, Ebetsu, Japan.


1. Caffeine did not evoke Ca2+ mobilization and histamine secretion. 2. Caffeine, as well as other methylxanthines but not forskolin or 8 bromo-cAMP, inhibited Ca2+ responses from compound 48/80. 3. Evoked histamine secretion was severely reduced by caffeine but not by cAMP analogs. 4. In beta-escin-permeabilized cells, caffeine did not affect resting and IP3-stimulated 45Ca2+ release, but it inhibited Ca(2+)-induced histamine secretion. 5. These results indicate that caffeine inhibits Ca2+ influx and Ca2+ efficacy in the secretory apparatus independent of cAMP, resulting in the inhibition of secretagogs-evoked histamine secretion from rat mast cells.

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