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THE ACTIVITY OF SODIUM CROMOGLYCATE ANALOGUES IN HUMAN LUNG in vitro : A COMPARISON WITH RAT PASSIVE CUTANEOUS ANAPHYLAXIS AND CLINICAL EFFICACY
Author(s) -
CHURCH MARTIN K.,
GRADIDGE CAROLYN F.
Publication year - 1980
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.1980.tb07937.x
Subject(s) - histamine , cromolyn sodium , degranulation , sodium cromoglycate , pharmacology , asthma , in vitro , immunoglobulin e , chemistry , anaphylaxis , mast cell , allergy , lung , sodium , immunology , mechanism of action , medicine , biochemistry , receptor , antibody , organic chemistry
1 Eleven analogues of sodium cromoglycate have been tested for their ability to suppress histamine release induced by anti‐IgE from passively sensitized human lung fragments in vitro . 2 With the exception of WY 16922, which released histamine at high concentrations, all inhibited histamine release in a linear dose‐related manner. 3 The analogues were 30 to 1500 times more potent than sodium cromoglycate. However, their regression slopes of activity upon log‐concentration were only one‐third as steep as that for sodium cromoglycate, indicating a possible difference in their mechanism of action. 4 In comparison with sodium cromoglycate, the analogues were more potent in human lung than in rat passive cutaneous anaphylaxis (PCA); there was no quantitative correlation between potencies in the two tests. 5 The human lung model is not predictive of anti‐asthmatic activity in man as the six analogues tested clinically are less effective than sodium cromoglycate. 6 These results throw doubt on the use of models of mast cell degranulation in the search for Antiallergic drugs and, possibly, on the relative importance of mast cell degranulation in the pathogenesis of asthma.