Discovery of a series of pyrrolidine-based endothelin receptor antagonists with enhanced ET A receptor selectivity

…, TW von Geldern, M Winn, JR Wu-Wong…

Index: Boyd, Steven A.; Mantei, Robert A.; Tasker, Andrew S.; Liu, Gang; Sorensen, Bryan K.; Henry Jr., Kenneth J.; Von Geldern, Thomas W.; Winn, Martin; Wu-Wong, Jinshyun R.; Chiou, William J.; Dixon, Douglas B.; Hutchins, Charles W.; Marsh, Kennan C.; Nguyen, Bach; Opgenorth, Terry J. Bioorganic and Medicinal Chemistry, 1999 , vol. 7, # 6 p. 991 - 1002

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Citation Number: 18

Abstract

Endothelins, ET-1, ET-2, and ET-3 are potent vasoconstricting and mitogenic 21-amino acid bicyclic peptides, which exert their effects upon binding to the ETA and ETB receptors. The ETA receptor mediates vasoconstriction and smooth muscle cell proliferation, and the ETB receptor mediates different effects in different tissues, including nitric oxide release from endothelial cells, and vasoconstriction in certain vascular cell types. Selective antagonists ...

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