Abstract
In cardiovascular diseases, endothelin type B (ET(B)) receptors in arterial smooth muscle cells are upregulated. The present study revealed that organ culture of rat mesenteric artery segments enhanced endothelin ET(B) receptor-mediated contraction paralleled with increase in the receptor mRNA and protein expressions. The endothelin ET(B) receptor-mediated contraction was associated with increase in phosphorylation of extracellular regulation kinase 1 and 2 (ERK1/2) proteins and elevated levels of intracellular calcium. The elevation curve of intracellular calcium consisted of two phases: one rapid and one sustained. Inhibition of ERK1/2 phosphorylation by SB386023 or blockage of calcium channels by nifedipine significantly reduced the endothelin ET(B) receptor-mediated contraction (P<0.05) and decreased the sustained phase of intracellular calcium level, but not the rapid phase. Thus, phosphorylation of ERK1/2 proteins and elevation of intracellular calcium level are required for endothelin ET(B) receptor-mediated contraction in rat mesenteric artery.
| Original language | English |
|---|---|
| Journal | European Journal of Pharmacology |
| Volume | 538 |
| Issue number | 1-3 |
| Pages (from-to) | 124-31 |
| Number of pages | 8 |
| ISSN | 0014-2999 |
| DOIs | |
| Publication status | Published - 24 May 2006 |
Keywords
- Animals
- Blotting, Western
- Calcium
- Calcium Channel Blockers
- Dose-Response Relationship, Drug
- Enzyme Inhibitors
- In Vitro Techniques
- Intracellular Fluid
- Mesenteric Arteries
- Mitogen-Activated Protein Kinase 1
- Mitogen-Activated Protein Kinase 3
- Nifedipine
- Phosphorylation
- RNA, Messenger
- Rats
- Rats, Sprague-Dawley
- Receptor, Endothelin B
- Time Factors
- Up-Regulation
- Vasoconstriction
- Vasoconstrictor Agents
- Viper Venoms
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