Pharmacological characterization of a potent nonpeptide endothelin receptor antagonist, 97-139.

The endothelin (ET) receptor antagonist activity of 97-139 [27-O-3-[2-(3-carboxy-acryloylamino)-5-hydroxyphenyl]-acryloylo xy myricerone, sodium salt] was studied. In rat aortic smooth muscle A7r5 cells that express ETA receptors and human Girardi heart cells that express ETB receptors, 97-139 displaced specifically bound [125I]ET-1 with the Ki values of 1.0 +/- 0.