The Affinity of Histamine for Gq Protein-Coupled Histamine H₁-Receptors Is Predominantly Regulated by Their Internalization in Human Astrocytoma Cells
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- Hishinuma Shigeru
- Department of Pharmacodynamics, Meiji Pharmaceutical University, Japan Department of Pharmacodynamics, Meiji Pharmaceutical University, Japan
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- Sato Yuko
- Department of Pharmacodynamics, Meiji Pharmaceutical University, Japan Department of Pharmacodynamics, Meiji Pharmaceutical University, Japan
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- Akatsu Chizuru
- Department of Pharmacodynamics, Meiji Pharmaceutical University, Japan Department of Pharmacodynamics, Meiji Pharmaceutical University, Japan
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- Shoji Masaru
- Department of Pharmacodynamics, Meiji Pharmaceutical University, Japan Department of Pharmacodynamics, Meiji Pharmaceutical University, Japan
書誌事項
- タイトル別名
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- The Affinity of Histamine for Gq Protein-Coupled Histamine H<SUB>1</SUB>-Receptors Is Predominantly Regulated by Their Internalization in Human Astrocytoma Cells
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We examined the regulatory mechanisms of the affinity of Gq protein-coupled histamine H1-receptors for histamine after histamine pretreatment in intact human U373 MG astrocytoma cells. In control cells, the displacement curves for histamine against the binding of 5 nM [3H]mepyramine, a radioligand for H1-receptors, showed the presence of two binding sites for histamine, that is, high and low affinity sites. Pretreatment with 0.1 mM histamine for 30 min at 37°C induced a significant reduction in the percentage of high affinity sites for histamine and a concomitant increase in the percentage of low affinity sites with no change in their pIC50 values. These histamine-induced changes were insensitive to 30 μM KN-62, an inhibitor of Ca2+/calmodulin-dependent protein kinase II, but they were completely inhibited either by 0.4 mM ZnCl2, an inhibitor of G protein-coupled receptor kinases (GRKs), or under hypertonic conditions, where clathrin-mediated endocytosis is known to be inhibited. These results suggest that histamine-induced conversion of high to low affinity sites for histamine is predominantly regulated by GRK/clathrin-mediated internalization of H1-receptors in human astrocytoma cells.
収録刊行物
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- Journal of Pharmacological Sciences
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Journal of Pharmacological Sciences 119 (3), 233-242, 2012
公益社団法人 日本薬理学会
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詳細情報 詳細情報について
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- CRID
- 1390001205179864576
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- NII論文ID
- 10030986893
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- NII書誌ID
- AA11806667
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- COI
- 1:CAS:528:DC%2BC38XhtFOnsbfE
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- ISSN
- 13478648
- 13478613
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- NDL書誌ID
- 023819142
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- PubMed
- 22786583
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- 本文言語コード
- en
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- データソース種別
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- JaLC
- NDL
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- PubMed
- CiNii Articles
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