DesArg 9D-Arg[Hyp 3,Thi 5,D-Tic 7,Oic 8]bradykinin (desArg 10-[Hoe140]) is a bradykinin B 1 receptor antagonist

Abstract

DesArg 9-D-Arg[Hyp 3,Thi 5,D-Tic 7,Oic 8]BK is a potent and stable B 1 bradykinin (BK) receptor antagonist which was one order of magnitude more potent (IC 50 1.2 × 10 −8 M) in the isolated rabbit aorta than the known selective B 1 BK receptor antagonist, desArg 9-[Leu 8]BK (IC 50 1.1 × 10 −7 M). DesArg 9-D-Arg[Hyp 3,Thi 5,D-Tic 7,Oic 8]BK is the desArg 10 derivative of Hoe 140, a new, potent, stable, selective and long-acting B 2 BK receptor antagonist. In B 2 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 B 1 BK receptor function.