Desensitization of canine histamine H2 receptor expressed in Chinese hamster ovary cells

Yasushi Fukushima, Yoshitomo Oka, Hideki Katagiri, Toshihito Saitoh, Tomoichiro Asano, Hisamitsu Ishihara, Nobuyuki Matsuhashi, Tatsuhiko Kodama, Yoshio Yazaki, Kentaro Sugano

Research output: Contribution to journalArticlepeer-review

29 Citations (Scopus)


Canine histamine H2 receptor DNA was transfected into Chinese hamster ovary cells using an expression vector. Expression of H2 receptors was demonstrated by immunoblotting with specific antibodies and the binding of tiotidine, an H2 receptor antagonist. H2 receptor-specific cAMP production was observed only in the cells expressing canine H2 receptor with 10-9-10-4 M histamine in a dose-dependent manner. Preincubation of transfected cells with 10 μM histamine for 10 min or 60 min at 37°C decreased both the maximal response and the sensitivity of the subsequent histamine-stimulated cAMP production, showing desensitization. Under these circumstances, tiotidine binding was decreased by 25% in intact cells. A similar decrease in the tiotidine binding was observed also in the membrane without changes in the affinity, whereas no decrease in total H2 receptor number was observed. Thus, desensitization of histamine H2 receptor was associated with the sequestration of receptors.

Original languageEnglish
Pages (from-to)1149-1155
Number of pages7
JournalBiochemical and Biophysical Research Communications
Issue number3
Publication statusPublished - 1993 Feb 15


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