{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2025,4,25]],"date-time":"2025-04-25T04:11:44Z","timestamp":1745554304464,"version":"3.40.4"},"reference-count":14,"publisher":"S. Karger AG","issue":"2-3","license":[{"start":{"date-parts":[[2003,1,1]],"date-time":"2003-01-01T00:00:00Z","timestamp":1041379200000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/www.karger.com\/Services\/SiteLicenses"},{"start":{"date-parts":[[2003,1,1]],"date-time":"2003-01-01T00:00:00Z","timestamp":1041379200000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/www.karger.com\/Services\/SiteLicenses"}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Digestion"],"published-print":{"date-parts":[[2003]]},"abstract":"<i>Background\/Aims:<\/i> Histamine H<sub>2<\/sub> receptor antagonists are considered to exert their effects on gastric acid secretion more rapidly than proton pump antagonists. However, there are no reports concerning the direct interaction of a histamine H<sub>2<\/sub> receptor antagonist with the human H<sub>2<\/sub> receptor in terms of onset of action. This study aims to characterize how rapidly famotidine and ranitidine, the most widely used histamine H<sub>2<\/sub> receptor antagonists, interact with the human histamine H<sub>2<\/sub> receptor. <i>Methods:<\/i> HEK293 cell lines, stably expressing human histamine H<sub>2<\/sub> receptors, were obtained. The dose- and time-dependent effects of famotidine and ranitidine on [<sup>3<\/sup>H]-tiotidine binding and histamine-stimulated cAMP production were analyzed. <i>Results:<\/i> Ranitidine inhibited both [<sup>3<\/sup>H]-tiotidine binding and histamine-stimulated cAMP production more promptly than did famotidine. Inhibition of histamine-stimulated cAMP production by C<sub>max<\/sub> doses of famotidine (20 mg p.o.) and ranitidine (150 mg p.o.) peaked by 15 and 2 min, respectively. [<sup>3<\/sup>H]-Tiotidine binding was not saturated by 60 min at the famotidine C<sub>max<\/sub>, while the ranitidine C<sub>max<\/sub> had produced saturation by 15 min. <i>Conclusion:<\/i> Ranitidine inhibits the human histamine H<sub>2<\/sub> receptor very rapidly.<\/jats:p>","DOI":"10.1159\/000075349","type":"journal-article","created":{"date-parts":[[2003,12,5]],"date-time":"2003-12-05T08:39:23Z","timestamp":1070613563000},"page":"145-152","source":"Crossref","is-referenced-by-count":0,"title":["Extremely Early Onset of Ranitidine Action on Human Histamine H<sub>2<\/sub> Receptors Expressed in HEK293 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