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Z Fekete, XY Yang, M Kimura and A Aviv
Hypertension Research Center, University of Medicine and Dentistry of New Jersey, New Jersey Medical School, Newark, USA.
In this study we characterized the endothelin (ET) receptors of cultured L6 myotubes in order to gain a further insight into the mechanism of the ET effect on skeletal muscle cells. Displacements of 125I-ET-1 by unlabeled ET-1, ET-2 and ET-3 revealed receptors with a high affinity (Kd < 1 nmol/l) to ET-1 and ET-2 and a low affinity (Kd > 100 nmol/l) to ET-3, which suggested the presence of primarily ETA receptors on L6 myotubes. These findings were complemented by displacement binding kinetics, in which the ETA receptor antagonist JKC- 301 was used. More-over, the ET-1-evoked increase in the cytosolic free Ca was blocked by JKC-301 but not by the ETB receptor antagonist IRL- 1038. Collectively, these findings indicate that the ET-mediated response in cultured skeletal muscle cells is through the ETA receptor.
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