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DesArg9-D-Arg[Hyp3,Thi5,D-Tic7,Oic8]bradykinin (desArg10-[Hoe140]) is a potent bradykinin B1 receptor antagonist.

作者信息

Wirth K, Breipohl G, Stechl J, Knolle J, Henke S, Schölkens B

机构信息

Hoechst AG, Frankfurt/Main, F.R.G.

出版信息

Eur J Pharmacol. 1991 Nov 26;205(2):217-8. doi: 10.1016/0014-2999(91)90824-a.

Abstract

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.

摘要

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