On the Mechanism of Chlorpromazine‐Induced Histamine Release from Rat Mast Cells

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Abstract
On exposure to chlorpromazine in concentrations above 20 μM, histamine was released by rat mast cells in vitro. Histamine release was unaffected by metabolic inhibitors, but was reduced by tetrodotoxin, elevated extracellular K+ and Ca++ concentrations. The cellular ratio of Na+ and K+ was changed, after treatment with chlorpromazine; sodium entered and potassium left the mast cells. It is concluded that chlorpromazine‐induced histamine release is secondary to permeability changes in the mast cell membranes and that Na+ plays an important part in the release mechanism.