PMID: 7712006Jan 1, 1995Paper

The kinin B1 receptor antagonist des-Arg9-[Leu8]bradykinin: an antagonist of the angiotensin AT1 receptor which also binds to the AT2 receptor

British Journal of Pharmacology
D PruneauJ C Bonnafous

Abstract

1. Agonists and antagonists of kinin B1 and B2 receptors were evaluated in vitro for their effects against angiotensin II (AII)-induced contractile responses in the rabbit aorta and for their binding properties to angiotensin AT1 and AT2 receptors from purified membrane of rat liver and lamb uterus respectively. 2. In aortic rings, the kinin B1 receptor antagonist, des-Arg9-[Leu8]bradykinin (BK) (3-100 microM) caused a concentration-dependent decrease in sensitivity and a depression of the maximum response to AII. Des-Arg10-[Leu9]kallidin (KD), des-Arg9-BK, des-Arg10-KD, BK or KD at 3 microM had no effect against AII-induced contractions. 3. Des-Arg9-[Leu8]BK (3 or 100 microM) did not affect contractions of aortic rings to histamine, potassium chloride, endothelin-1, 5-hydroxytryptamine, noradrenaline and the thromboxane A2-mimetic, U46619. 4. Des-Arg9-[Leu8]BK displaced [125I]-Sar1-AII binding to the AT1 subtype in rat liver membranes with a Ki value of 1.1 +/- 0.4 microM. Values of Ki for des-Arg9-BK and KD were 45 +/- 13 microM and 25 +/- 22 microM, respectively. The other kinin derivatives des-Arg10-KD, BK and des-Arg10-[Leu9]KD at concentrations up to 100 microM did not bind to the AT1 receptor. 5. All the kinin derivative...Continue Reading

References

Nov 1, 1992·Pharmacology & Therapeutics·J M Hall
Jan 1, 1990·Journal of Cardiovascular Pharmacology·D RegoliS Dion
Feb 1, 1991·Trends in Pharmacological Sciences·P B TimmermansW F Herblin
Aug 30, 1989·Biochemical and Biophysical Research Communications·S WhitebreadM de Gasparo

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Citations

Jun 1, 1995·Immunopharmacology·F Marceau
Jul 3, 1998·European Journal of Pharmacology·D RegoliF J Gobeil
Nov 9, 2002·Autonomic & Autacoid Pharmacology·K M Ellis, J R Fozard

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