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

doi:10.1159/000075349

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

MED - Medical Sciences

Research output: Contribution to journal › Article › peer-review

1 Citation (Scopus)

Abstract

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 C_max 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 C_max, while the ranitidine C_max had produced saturation by 15 min. Conclusion: Ranitidine inhibits the human histamine H₂ receptor very rapidly.

Original language	English
Pages (from-to)	145-152
Number of pages	8
Journal	Digestion
Volume	68
Issue number	2-3
DOIs	https://doi.org/10.1159/000075349
Publication status	Published - 2003

Keywords

Famotidine
Histamine H receptor
Ranitidine, action onset

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10.1159/000075349

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Fukushima, Y., Ishikawa, T., Saitoh, T., Tateishi, K., Ogihara, T., Fujishiro, M., Shojima, N., Honda, M., Kushiyama, A., Anai, M., Sakoda, H., Ono, H., Onishi, Y., Otsuka, H., Katagiri, H., Nagai, R., Omata, M., & Asano, T. (2003). Extremely early onset of ranitidine action on human histamine H ₂ receptors expressed in HEK293 cells. Digestion, 68(2-3), 145-152. https://doi.org/10.1159/000075349

@article{1bc3c87e4cbb4eb78b740b243c41a5a1,

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

abstract = "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.",

keywords = "Famotidine, Histamine H receptor, Ranitidine, action onset",

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

year = "2003",

doi = "10.1159/000075349",

language = "English",

volume = "68",

pages = "145--152",

journal = "Digestion",

issn = "0012-2823",

publisher = "S. Karger AG",

number = "2-3",

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Fukushima, Y, Ishikawa, T, Saitoh, T, Tateishi, K, Ogihara, T, Fujishiro, M, Shojima, N, Honda, M, Kushiyama, A, Anai, M, Sakoda, H, Ono, H, Onishi, Y, Otsuka, H, Katagiri, H, Nagai, R, Omata, M & Asano, T 2003, 'Extremely early onset of ranitidine action on human histamine H ₂ receptors expressed in HEK293 cells', Digestion, vol. 68, no. 2-3, pp. 145-152. https://doi.org/10.1159/000075349

TY - JOUR

T1 - Extremely early onset of ranitidine action on human histamine H 2 receptors expressed in HEK293 cells

AU - Fukushima, Yasushi

AU - Ishikawa, Takashi

AU - Saitoh, Toshihito

AU - Tateishi, Keisuke

AU - Ogihara, Takehide

AU - Fujishiro, Midori

AU - Shojima, Nobuhiro

AU - Honda, Miho

AU - Kushiyama, Akifumi

AU - Anai, Motonobu

AU - Sakoda, Hideyuki

AU - Ono, Hiraku

AU - Onishi, Yukiko

AU - Otsuka, Hiroko

AU - Katagiri, Hideki

AU - Nagai, Ryozo

AU - Omata, Masao

AU - Asano, Tomoichiro

PY - 2003

Y1 - 2003

N2 - 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.

AB - 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.

KW - Famotidine

KW - Histamine H receptor

KW - Ranitidine, action onset

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UR - http://www.scopus.com/inward/citedby.url?scp=9144219586&partnerID=8YFLogxK

U2 - 10.1159/000075349

DO - 10.1159/000075349

M3 - Article

C2 - 14671421

AN - SCOPUS:9144219586

SN - 0012-2823

VL - 68

SP - 145

EP - 152

JO - Digestion

JF - Digestion

IS - 2-3

ER -

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

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