Premium
EFFECT OF AMODIAQUINE ON GASTRIC HISTAMINE METHYLTRANSFERASE AND ON HISTAMINE‐STIMULATED GASTRIC SECRETION
Author(s) -
BARTH H.,
LORENZ W.,
TROIDL H.
Publication year - 1975
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.1476-5381.1975.tb06934.x
Subject(s) - amodiaquine , histamine , gastric mucosa , gastric acid , chemistry , antrum , pharmacology , stomach , medicine , histamine n methyltransferase , histaminergic , endocrinology , biology , biochemistry , immunology , histamine h2 receptor , antagonist , receptor , malaria , chloroquine
1 Amodiaquine was found to be a potent inhibitor in vitro of gastric histamine methyltransferase from human and canine corpus and from pig antrum. The ID 50 for the enzyme, purified from pig antrum mucosa by ultracentrifugation and chromatography on DEAE‐cellulose, was 2.5 μM. 2 In six dogs with Heidenhain pouches the maximum secretory response to histamine (40 μg/kg i.m.) was augmented by i.m. injection of amodiaquine. The augmentation depended on the dose of amodiaquine, the optimum effect (40% increase in volume of gastric juice, 80% in acid output) being achieved with 2 mg/kg. The maximum secretory response to betazole was also enhanced by amodiaquine. 3 It was suggested that amodiaquine may enhance the histamine and betazole stimulated gastric secretion by an inhibition of gastric histamine methyltransferase in vivo .