The inhibitory effect of [D-Arg1,D-Phe,D-Try7,9,Leu11] substance P on endothelin-1 binding sites in rat cardiac membranes.
The specific binding of [125I]ET-1 to rat cardiac membrane fragments was inhibited by [D-Arg1,D-Phe, D-Try7,9,Leu11] substance P [substance P(D)], a potent bombesin antagonist. This inhibitory effect required high concentrations (greater than 3X10(-6)M) of substance P(D) and was accompanied by a steep increase in non-specific binding, and not a decrease in total binding. Such results indicate that substance P(D) does not competitively inhibit the specific binding of [125I]ET-1 to rat cardiac membrane fragments.
Gu
X H
XH
Department of Medicine, University of Melbourne, Austin Hospital, Heidelberg VIC Australia.
Casley
D J
DJ
Nayler
W G
WG
D000818:Animals; D001665:Binding Sites; D001839:Bombesin / Q000037:antagonists & inhibitors; D002462:Cell Membrane / Q000378:metabolism; D016232:Endothelins / Q000378:metabolism*; D006352:Heart Ventricles; D007700:Kinetics; D009206:Myocardium / Q000378:metabolism*; D051381:Rats; D011919:Rats, Inbred Strains; D011956:Receptors, Cell Surface / Q000187:drug effects / Q000378:metabolism*; D017466:Receptors, Endothelin; D013373:Substance P / Q000031:analogs & derivatives* / Q000494:pharmacology
D016232:Endothelins; D011956:Receptors, Cell Surface; D017466:Receptors, Endothelin; D013373:Substance P; C045800:substance P, Phe(5)-Trp(7,9)-Leu(11)-; D001839:Bombesin