Dimaprit, a Histamine H2-Agonist, Inhibits Anaphylactic Histamine Release from Mast Cells and the Decreased Release Is Restored by Thioperamide (H3-Antagonist), but Not by Cimetidine (H2-Antagonist).
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概要
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Whether anaphylactic histamine release from rat peritoneal mast cells is influenced by betahistine, a histamine H<SUB>1</SUB>-receptor agonist/H<SUB>3</SUB>-antagonist, and dimaprit, an H<SUB>2</SUB>-agonist, was examined. Treatment with dimaprit at 6 and 60 μM for 20 min significantly inhibited the anaphylactic histamine release, whereas betahistine at up to 80 μM under the same conditions did not affect it. Treatment with dimaprit at 6 and 60 μM for 1 to 20 min and for 5 to 20 min, respectively, caused a time-dependent inhibition of the release, but up to 30 min treatment with 8 and 80 μM betahistine had no effect. The decreased histamine release induced by dimaprit was recovered by neither mepyramine nor cimetidine. However, thioperamide, an H<SUB>3</SUB>-selective antagonist, dose-dependently restored the diminished release. From these results, the inhibition of anaphylactic histamine release by dimaprit is not produced by the stimulation of H<SUB>2</SUB>-receptors, but involves the stimulation of H<SUB>3</SUB>-like receptors or H<SUB>3</SUB>-subtype receptors, which are distinct from the H<SUB>3</SUB>-receptors located in brain, and suggests that the receptor plays an important role in the negative feedback regulation of histamine release.
- 公益社団法人 日本薬理学会の論文
著者
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Ohata Katsuya
Department Of Pharmacology Kyoto Pharmaceutical University:department Of Pneumology Ogaki Municipal
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Ogawa Kohji
Department Of Chemistry Faculty Of Science Science University Of Tokyo
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Nabe Takeshi
Department Of Pharmacology Kyoto Pharmaceutical University
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Yamamura Hideki
Department Of Anatomy Hiroshima University School Of Medicine
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Kohno Shigekatsu
Department Of Pharmacology Division Of Pathological Sciences Kyoto Pharmaceutical University
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