Down-regulation of endothelin binding sites in rat vascular smooth muscle cells

Journal Article · Sat Mar 31 23:00:00 EST 1990 · American Journal of Hypertension; (USA)

DOI:https://doi.org/10.1093/ajh/3.4.310· OSTI ID:6709257

Roubert, P; Gillard, V; Plas, P; Chabrier, P E; Braquet, P ^[1]

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1. Institut Henri Beaufour, Les Ulis (France)

In cultured rat aortic smooth muscle cells, ({sup 125}I)endothelin (ET-1) bound to an apparent single class of high affinity recognition sites with a dissociation constant of 1.84 +/- 0.29 nmol/L and a maximum binding of 62 +/- 10.5 fmol/10(6) cells. The binding was not affected by calcium antagonists or vasoactive substances, including angiotensin II, arginine vasopressin, atrial natriuretic factor and bradykinin. Exposure of the cells to ET-1 (0.01 nmol/L to 10 nmol/L) resulted in an apparent dose-dependent reduction of the number of endothelin binding sites with no significant modification of its binding affinity. The time course of the down-regulation of ET-1 binding sites showed that this effect was present after 30 min incubation and persisted after 18 h. This indicates that down-regulation of ET-1 binding sites can modulate the activity of ET-1 and suggests a rapid internalization of ET-1 in vascular cells.

• OSTI ID: 6709257
• Journal Information: American Journal of Hypertension; (USA), Journal Name: American Journal of Hypertension; (USA) Vol. 3:4; ISSN AJHYE; ISSN 0895-7061
• Country of Publication: United States
• Language: English

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59 BASIC BIOLOGICAL SCIENCES
ANIMALS
BETA DECAY RADIOISOTOPES
BIOCHEMICAL REACTION KINETICS
CELL CULTURES
DAYS LIVING RADIOISOTOPES
DOSE-RESPONSE RELATIONSHIPS
ELECTRON CAPTURE RADIOISOTOPES
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IODINE 125
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KINETICS
MAMMALS
MEMBRANE PROTEINS
MUSCLES
NUCLEI
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PROTEINS
RADIOISOTOPES
RATS
REACTION KINETICS
RECEPTORS
RODENTS
TRACER TECHNIQUES
VERTEBRATES