Biological activity of the endothelin family in cultured basilar arterial smooth muscle cells.
The effects of three forms of endothelin (ET), ET-1, -2 and -3, on intracellular free Ca2+ concentration ([Ca2+]i), their receptor binding activities, and DNA synthesis were investigated in cultured porcine basilar arterial smooth muscle cells. Endothelin-1 and ET-2 induced cytosolic free calcium elevations that did not return to the basal level. The maximum levels of [Ca2+]i induced by the three points were ET-1 approximately equal to ET-2 > ET-3. The cells display specific binding of 125I-labelled endothelin-1 which was displaced by three endothelins; ET-1, -2, and -3, in a concentration-dependent manner. The order of potency in inhibiting 125I-labeled endothelin-1 binding was ET-1 approximately equal to ET-2 > ET-3. Endothelin-1, ET-2, and ET-3 stimulated [3H]thymidine incorporation in a dose-dependent manner, the maximum order of potency (100 nM) was again ET-1 approximately equal to ET-2 > ET-3. These results indicate that ET-1 and ET-2 are more potent in their biological activities than ET-3 in cultured cerebral arterial smooth muscle cells.
Takenaka
K
K
Department of Neurosurgery, Gifu University School of Medicine, Japan.
Kishino
J
J
Arita
H
H
Okano
Y
Y
Sakai
N
N
Yamada
H
H
Nozawa
Y
Y
D000818:Animals; D001488:Basilar Artery / Q000166:cytology / Q000378:metabolism; D001667:Binding, Competitive / Q000502:physiology; D002118:Calcium / Q000378:metabolism; D002478:Cells, Cultured; D016232:Endothelins / Q000378:metabolism / Q000502:physiology*; D005260:Female; D008297:Male; D009131:Muscle, Smooth, Vascular / Q000166:cytology / Q000378:metabolism*; D013552:Swine; D013936:Thymidine / Q000378:metabolism
D016232:Endothelins; D002118:Calcium; D013936:Thymidine