A192621

A192621 is a potent, non-peptide, and highly selective endothelin B (ETB) receptor antagonist. Developed by Abbott Laboratories, it is primarily utilized as a pharmacological research tool to investigate the physiological and pathological roles of the ETB receptor subtype. The ETB receptor is known to mediate complex vascular effects, including vasodilation via endothelial nitric oxide release and vasoconstriction through receptors located on vascular smooth muscle cells. A192621 has been instrumental in preclinical studies exploring cerebrovascular remodeling, hypertension, and renal function, particularly in models of type 2 diabetes. Research indicates that while ETB receptor activation may be vasculoprotective in healthy states, its role can become maladaptive in diseased states, a distinction elucidated through the use of selective antagonists like A192621.

Other names

(2R,3R,4S)-4-(1,3-benzodioxol-5-yl)-1-[2-[(2,6-diethylphenyl)amino]-2-oxoethyl]-2-(4-propoxyphenyl)pyrrolidine-3-carboxylic acid