Pharmacological Characterization of a Novel Sulfonylureid-Pyrazole Derivative, SM-19712, a Potent Nonpeptidic Inhibitor of Endothelin Converting Enzyme

Preclinical models including rat lung microsomes, cultured porcine aortic endothelial cells, anesthetized rats, and rabbits subjected to coronary occlusion and reperfusion (acute myocardial infarction model).

SM-19712 (a novel sulfonylureid-pyrazole derivative) administered in vitro (1-100 microM) and in vivo (1-30 mg/kg IV or 10-30 mg/kg oral in rats).

Inhibition of endothelin converting enzyme (ECE) activity and reduction of infarct size.surrogate