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Cadmium directly acts on endothelin receptor and inhibits endothelin binding activity

Authors
Journal
FEBS Letters
0014-5793
Publisher
Wiley Blackwell (John Wiley & Sons)
Publication Date
Volume
285
Issue
1
Identifiers
DOI: 10.1016/0014-5793(91)80727-k
Keywords
  • Vaso Constriction
  • Hypertension
  • Hypotension
  • Human Placenta
  • Divalent Metals
  • Chelating Agent

Abstract

Abstract The binding of endothelin (ET) to human placenta ET receptor was strongly inhibited by cadmium ions (Cd 2+) (IC 50 = 2 × 10 −5 M). Experiments with affinity cross-linking showed that the major 40 kDa receptor was inhibited to form a [ 125I]ET-1/receptor complex. The mode of inhibition was noncompetitive with respect to ET-1. The inhibitory effect of Cd 2+ on solubilized ET receptor was partially reversed by the chelating agent, ethylenediaminetetraacetic acid (EDTA), whereas the effect was irreversible for the membrane-associated receptor. The rat aorta contractions by ET were prevented by pretreatment or addition of Cd 2+.

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