Extremely early onset of ranitidine action on human histamine H 2 receptors expressed in HEK293 cells

Yasushi Fukushima, Takashi Ishikawa, Toshihito Saitoh, Keisuke Tateishi, Takehide Ogihara, Midori Fujishiro, Nobuhiro Shojima, Miho Honda, Akifumi Kushiyama, Motonobu Anai, Hideyuki Sakoda, Hiraku Ono, Yukiko Onishi, Hiroko Otsuka, Hideki Katagiri, Ryozo Nagai, Masao Omata, Tomoichiro Asano

Research output: Contribution to journalArticlepeer-review

1 Citation (Scopus)


Background/Aims: Histamine H2 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 H2 receptor antagonist with the human H2 receptor in terms of onset of action. This study aims to characterize how rapidly famotidine and ranitidine, the most widely used histamine H2 receptor antagonists, interact with the human histamine H2 receptor. Methods: HEK293 cell lines, stably expressing human histamine H2 receptors, were obtained. The dose- and time-dependent effects of famotidine and ranitidine on [3H]-tiotidine binding and histamine-stimulated cAMP production were analyzed. Results: Ranitidine inhibited both [3H]-tiotidine binding and histamine-stimulated cAMP production more promptly than did famotidine. Inhibition of histamine- stimulated cAMP production by Cmax doses of famotidine (20 mg p.o.) and ranitidine (150 mg p.o.) peaked by 15 and 2 min, respectively. [ 3H]-Tiotidine binding was not saturated by 60 min at the famotidine Cmax, while the ranitidine Cmax had produced saturation by 15 min. Conclusion: Ranitidine inhibits the human histamine H2 receptor very rapidly.

Original languageEnglish
Pages (from-to)145-152
Number of pages8
Issue number2-3
Publication statusPublished - 2003


  • Famotidine
  • Histamine H receptor
  • Ranitidine, action onset


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