valsartan is a potent, highly selective, and orally active antagonist at the angiotensin II (AII) AT1-receptor. Valsartan compets with [125I]-AII at its specific binding sites in rat aortic smooth muscle cell membranes (AT1-receptor subtype) with a Ki of 2.38 nM, but is about 30,000 times less active in human myometrial membranes (AT2-receptor subtype).
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