Abstract
The binding of [ 3H]angiotensin II to AT 1 receptors on Chinese Hamster Ovary cells expressing the human AT 1 receptor (CHO-AT 1 cells) is potently inhibited by venoms of the marine snails Conus geographus and C. betulinus. On the other hand, the binding of the nonpeptide AT 1 receptor-selective antagonist [ 3H]candesartan is not affected but competition binding curves of angiotensin II and the peptide antagonist [Sar 1,Ile 8]angiotensin II (sarile) are shifted to the right. These effects resulted from the breakdown of angiotensin II into smaller fragments that do not bind to the AT 1 receptor. In this context, angiotensin-(1–7) is the most prominent fragment and angiotensin-(1–4) and angiotensin-(1–5) are also formed but to a lesser extent. The molecular weight of the involved peptidases exceeds 50 kDa, as determined by gel chromatography and ultrafitration.
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