DesArg9-D-Arg[Hyp3,Thi5,D-Tic7,Oic8]bradykinin (desArg10-[Hoe140]) is a potent bradykinin B1 receptor antagonist.
DesArg9-D-Arg[Hyp3,Thi5,D-Tic7,Oic8]BK is a potent and stable B1 bradykinin (BK) receptor antagonist which was one order of magnitude more potent (IC50 1.2 x 10(-8) M) in the isolated rabbit aorta than the known selective B1 BK receptor antagonist, desArg9-[Leu8]BK (IC50 1.1 x 10(-7) M). DesArg9-D-Arg[Hyp3,Thi5,D-Tic7,Oic8]BK is the desArg10 derivative of Hoe140, a new, potent, stable, selective and long-acting B2 BK receptor antagonist. In B2 organ preparation it was three orders of magnitude less potent than Hoe140. Since it is potent and stable it could contribute to the investigation of B1 BK receptor function.
Wirth
K
K
Hoechst AG, Frankfurt/Main, F.R.G.
Breipohl
G
G
Stechl
J
J
Knolle
J
J
Henke
S
S
Schölkens
B
B
D000818:Animals; D001920:Bradykinin / Q000037:antagonists & inhibitors* / Q000031:analogs & derivatives; D005260:Female; D006168:Guinea Pigs; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects; D009131:Muscle, Smooth, Vascular / Q000187:drug effects; D009842:Oligopeptides / Q000494:pharmacology*; D011817:Rabbits; D018002:Receptors, Bradykinin; D017981:Receptors, Neurotransmitter / Q000187:drug effects*; D014661:Vasoconstriction / Q000187:drug effects
D009842:Oligopeptides; D018002:Receptors, Bradykinin; D017981:Receptors, Neurotransmitter; C065679:icatibant; D001920:Bradykinin