α-Fluoromethylhistidine dihydrochloride is an orally active histidine decarboxylase inhibitor. α-Fluoromethylhistidine dihydrochloride depletes histamine in enterochromaffin-like (ECL) cells, reduces the number and volume density of secretory vesicles in ECL cells, and does not affect histamine storage in mast cells. α-Fluoromethylhistidine dihydrochloride abolishes Omeprazole ( HY-B0113 )-induced vacuolization of ECL cells and decreases gastrin -induced histamine efflux from ECL cells. α-Fluoromethylhistidine dihydrochloride does not alter the granular characteristics of ECL cells, omeprazole-induced hypertrophy of ECL cells, gastrin-induced pancreastatin-like immunoreactivity efflux, nor does it affect gastric acid secretion induced by histamine or vagal stimulation. α-Fluoromethylhistidine dihydrochloride inhibits basal and gastrin-stimulated gastric acid secretion, reduces acid output induced by gastrin+IBMX ( HY-12318 ), but does not directly affect acid generation in isolated parietal cells.
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