Key result
Novel angiotensin II antagonist Compound 44 demonstrates subnanomolar AT1/AT2 potency and oral activity in rats.
Why the study?
Development of orally active non-peptide angiotensin II antagonists with potent and equal affinity for human AT1 and AT2 receptor subtypes was pursued to block effects induced by AII interactions with both receptors.
The study identifies Compound 44 as a potent, orally active dual AT1/AT2 receptor antagonist with equal affinity for both subtypes, providing a novel pharmacological tool.
No takes yet. Share an insight, caveat, or question.
Hypothesis-generating for dual AT1/AT2 blockade in animals; should not yet change clinical practice.
Chang et al. (1995) studied this question. Compound 44 (trisubstituted 1,2,4-triazolinone biphenyl-sulfonamide dual-acting AII antagonist) was evaluated on AT1 and AT2 receptor binding affinity and in vivo activity. Compound 44, a novel non-peptide angiotensin II antagonist, exhibited subnanomolar potency at both AT1 and AT2 receptors and demonstrated oral activity at 3 mg/kg in a conscious rat model.
Synapse has enriched 5 closely related papers on similar clinical questions. Consider them for comparative context: