The selective endothelin ETA receptor antagonist BQ123 antagonizes endothelin-1-mediated mitogenesis
| Autor: | John D. Elliott, Eliot H. Ohlstein, Anthony J. Arleth, Heidemarie Bryan, Cheng Po Sung |
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| Rok vydání: | 1992 |
| Předmět: |
Male
Agonist medicine.medical_specialty Vascular smooth muscle medicine.drug_class Mitosis Receptors Cell Surface Peptide Peptides Cyclic Muscle Smooth Vascular Internal medicine medicine Animals Cells Cultured Pharmacology chemistry.chemical_classification Dose-Response Relationship Drug biology Receptors Endothelin Endothelins Rats Inbred Strains DNA Endothelin 1 In vitro Rats medicine.anatomical_structure Endocrinology chemistry Mitogen-activated protein kinase cardiovascular system biology.protein Endothelin receptor Thymidine Blood vessel |
| Zdroj: | European Journal of Pharmacology: Molecular Pharmacology. 225:347-350 |
| ISSN: | 0922-4106 |
| DOI: | 10.1016/0922-4106(92)90109-9 |
| Popis: | The mitogenic effects of endothelin isopeptides and the selective ETA receptor antagonist BQ123 were evaluated in rat aortic vascular smooth muscle cells. Endothelin-1 (ET-1) and endothelin-3 (ET-3) produced concentration-dependent increases in [3H]thymidine incorporation (EC50 = 0.1 and 25 nM, respectively). The ETB-selective agonist sarafotoxin 6c did not produce significant effects on [3H]thymidine incorporation. BQ123 produced selective and concentration-dependent inhibition of ET-1-mediated [3H]thymidine incorporation. These data demonstrate that ET-1-mediated mitogenesis in vascular smooth muscle is mediated by ETA receptors. |
| Databáze: | OpenAIRE |
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