O. Gresser et al., ET-1 AND ET-3 ACTIONS MEDIATED BY CLONED ETA ENDOTHELIN RECEPTORS EXHIBIT DIFFERENT SENSITIVITIES TO BQ-123, Biochemical and biophysical research communications, 224(1), 1996, pp. 169-171
Et-1 and Et-3 activate phospholipase C in fibroblasts expressing clone
d ETA receptors of bovine, rat and human origins. BQ-123 competitively
antagonizes both responses but Et-3 actions are 10 times more sensiti
ve to BQ-123 than Et-l actions. It is suggested that differential sens
itivity to BQ-123 is an intrinsic property of Et-l and Et-3 activated
ETA receptors and that there is no need to postulate the existence of
new ETA receptor isoforms to account for singular actions of BQ-123. (
C) 1996 Academic Press, Inc.