Why the study?
Does cadmium inhibit endothelin binding activity and endothelin-induced contractions in preclinical models?
Does cadmium inhibit endothelin binding activity and endothelin-induced contractions in preclinical models?
Cadmium acts directly on the endothelin receptor to noncompetitively inhibit endothelin binding and prevent endothelin-induced vascular contractions in vitro.
Cadmium may inhibit ET-mediated vasoconstriction in vitro; leaves open relevance to human toxicity or vascular disease.
The binding of endothelin (ET) to human placenta ET receptor was strongly inhibited by cadmium ions (Cd2+) (IC50 = 2 x 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 Cd2+ 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 Cd2+.
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Wada et al. (1991) studied this question.
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