AT1-AT2-balanced angiotensin II antagonists

Three heterocyclic series of nonpeptide angiotensin II receptor antagonists (quinazolinones, imidazo[4,5-b]pyridines, and triazolinones) have been transformed in parallel from agents highly selective for the AT 1 receptor subtype into ligands with equal and high affinity for the AT 1 and AT 2 subtypes. These compounds are orally active with long duration of action in animal models of hypertension. They should be useful for investigating potential therapeutic advantages of dual AT 1 /AT 2 receptor blockade