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Functional coupling of ETA receptor with Ca(2+)-permeable nonselective cation channel in mouse fibroblasts and rabbit aortic smooth-muscle cells



Functional coupling of ETA receptor with Ca(2+)-permeable nonselective cation channel in mouse fibroblasts and rabbit aortic smooth-muscle cells



Journal of Cardiovascular Pharmacology 26(Suppl. 3): S258-S261



Endothelin-1 (ET-1) induces persistent vasoconstriction via a sustained increase in intracellular free Ca-2+ concentrations ((Ca-2+)-i). The mechanisms of the elevation of (Ca-2+)-i operating at physiologically low concentrations of ET-1 are controversial. Here we report that both native ET-A receptors in vascular smooth-muscle cells and recombinant ET-A receptors expressed in mouse fibroblasts (Ltk cells) are functionally coupled with a non-selective cation channel, which is permeable to Ca-2+ and is blocked by mefenamic acid. The channel is persistently activated by a low concentration of ET-1 (10-10 nM) without stimulation of inositol triphosphate (IP-3) formation and mediates sustained vasoconstriction.

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Accession: 008709174

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PMID: 8587381


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