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- Title
Potent and Long-Lasting Action of Lafutidine on the Human Histamine H[sub 2] Receptor.
- Authors
Fukushima, Yasushi; Otsuka, Hiroko; Ishikawa, Minako; Asano, Tomoichiro; Anai, Motonobu; Katsube, Takao; Ogawa, Kenji; Kajiwara, Tetsuro; Ohkawa, Shinichiro; Ishikawa, Takashi; Omata, Masao; Saitoh, Toshihito
- Abstract
Background/Aim: Based on animal models, lafutidine, a novel histamine H[sub 2] receptor (H[sub 2] R) antagonist, is reported to show potent and long-lasting antagonisms of histamine H[sub 2] R-mediated effects. However, no reports have been published concerning its direct interaction with the human H[sub 2] R. This study aims at characterizing its interaction with human H[sub 2] R. Methods: Chinese hamster ovary cell lines stably expressing human H[sub 2] Rs were obtained. The dose-dependent effects of lafutidine and famotidine on [[sup 3] H]tiotidine binding and histamine-stimulated cAMP production were analyzed. The effects of preincubation with 2.78 × 10[sup –7] M of lafutidine or famotidine for 30 min on histamine-dependent cAMP production and [[sup 3] H]tiotidine binding were also examined after 0, 1, 2, 4, and 12 h. This concentration is below the C[sub max] of lafutidine (10 mg p.o.) and above the C[sub max] of famotidine (20 mg p.o.). Results: Lafutidine inhibited [[sup 3] H]tiotidine binding and histamine-stimulated cAMP production as or more potently than famotidine. At higher concentrations lafutidine was more potent than famotidine. In addition, preincubation with 2.78 × 10[sup –7] M lafutidine, but not with 10[sup –5] M famotidine, had marked inhibitory effects which persisted as long as after extensive washing. Conclusion: Lafutidine shows a potent and long-lasting antagonism on the human H[sub 2] R.Copyright © 2001 S. Karger AG, Basel
- Subjects
HISTAMINE receptors; CYCLIC adenylic acid; DRUG antagonism; DOSE-response relationship in biochemistry; BINDING sites; ANTIHISTAMINES
- Publication
Digestion, 2001, Vol 64, Issue 3, p155
- ISSN
0012-2823
- Publication type
Article
- DOI
10.1159/000048856