Pharmacological properties of angiotensin II receptors in cultured rabbit gingival fibroblasts
Autor: | Yasuo Kizawa, Masakazu Sano, Hajime Murakami, Nozomi Ohuchi, Keishi Iwamoto, Masami Ohsawa, Kazuhiko Hayashi, Yumiko Taniguchi, Katsuo Koike, Tadashi Kusama |
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Rok vydání: | 2004 |
Předmět: |
medicine.medical_specialty
Angiotensin receptor Physiology Health Toxicology and Mutagenesis Blotting Western Population Gingiva Tetrazoles Biology Tritium Toxicology Binding Competitive Biochemistry Losartan Angiotensin Receptor Antagonists Radioligand Assay chemistry.chemical_compound Internal medicine medicine Animals Receptor education Cells Cultured education.field_of_study Receptors Angiotensin Angiotensin II receptor type 1 Dose-Response Relationship Drug Angiotensin II Ligand binding assay Biphenyl Compounds Cell Biology General Medicine Fibroblasts Kinetics Endocrinology chemistry cardiovascular system Benzimidazoles Rabbits Saralasin Angiotensin II Type 1 Receptor Blockers Cell Division hormones hormone substitutes and hormone antagonists circulatory and respiratory physiology |
Zdroj: | Comparative Biochemistry and Physiology Part C: Toxicology & Pharmacology. 137:281-289 |
ISSN: | 1532-0456 |
DOI: | 10.1016/j.cca.2004.02.003 |
Popis: | We demonstrated that angiotensin II (Ang II, 10-1000 nM) induced proliferation of cultured rabbit gingival fibroblasts in a concentration-dependent manner. The Ang II-induced proliferation was inhibited by CV-11974 (AT1 antagonist; 1 microM) and saralasin (AT1/AT2 antagonist; 1 microM), but not by PD123,319 (AT2 antagonist; 1 microM), suggesting that Ang II-induced proliferation was mediated via AT1 receptors present in and/or on gingival fibroblasts. The results of Western blot analysis indicated the presence of AT1 and AT2 receptors in/on the fibroblasts. In a subsequent radioligand binding assay, the binding of [3H]Ang II to the fibroblasts was specific and saturable with both high- and low-affinity sites. Competition binding experiments indicated that Ang II completely displaced [3H]Ang II binding, and CV-11974 and PD123,319 maximally displaced up to approximately 63% and 37% of the total binding, respectively. Ang II and CV-11974 completely displaced the [3H]DuP753 binding but PD123,319 did not, indicating a single population of binding site. These findings demonstrate that gingival fibroblasts contain both AT1 and AT2 receptor subtypes for Ang II, and support that Ang II stimulation of AT1 receptors results in proliferation of the fibroblasts. |
Databáze: | OpenAIRE |
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