Article date: August 1980
By: MARTIN K. CHURCH, CAROLYN F. GRADIDGE, in Volume 69, Issue 4, pages 663-667
A series of cationic, lipophilic histamine H1‐receptor antagonists, neuroleptics, antidepressants and monoamine oxidase inhibitors were tested for their effects on anti‐IgE‐induced histamine release from human lung fragments in vitro.
They had a biphasic effect: at low concentrations a dose‐related inhibition of histamine release was observed whereas, at higher concentrations, the drugs liberated histamine even in the absence of antigen.
Mepyramine, a much less lipophilic drug than the others tested, was only weakly active on mast cells at pharmacological concentrations.
The potency of the drugs as release inhibitors was not related quantitatively to their histamine liberating potency.
There was no correlation between activity on mast cells and histamine H1‐receptor antagonism.
Mast cell stabilization may play a part in the activity of these drugs as Antiallergic agents.
A series of cationic, lipophilic histamine H1‐receptor antagonists, neuroleptics, antidepressants and monoamine oxidase inhibitors were tested for their effects on anti‐IgE‐induced histamine release from human lung fragments in vitro.
They had a biphasic effect: at low concentrations a dose‐related inhibition of histamine release was observed whereas, at higher concentrations, the drugs liberated histamine even in the absence of antigen.
Mepyramine, a much less lipophilic drug than the others tested, was only weakly active on mast cells at pharmacological concentrations.
The potency of the drugs as release inhibitors was not related quantitatively to their histamine liberating potency.
There was no correlation between activity on mast cells and histamine H1‐receptor antagonism.
Mast cell stabilization may play a part in the activity of these drugs as Antiallergic agents.
DOI: 10.1111/j.1476-5381.1980.tb07919.x
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