Studies on the angiotensin-converting enzyme and the kinin B2 receptor in the rabbit jugular vein: modulation of contractile response to bradykinin

Canadian Journal of Physiology and Pharmacology
F GobeilD Regoli

Abstract

The rabbit jugular vein (rbJV) was used as a bioassay system to validate some early and new hypothetical interactions between the angiotensin-converting enzyme (ACE) and the B2 receptor, which may be influenced by ACE inhibitors (ACE-I). These involve the potentiation of the contractile effect of bradykinin (BK) and BK analogues, which are inactivated by ACE (e.g., [Hyp3, Tyr(Me8)]-BK (R556)), the prevention of BK-induced B2 receptor desensitisation, and the restoration of receptor sensitivity in tissues desensitised with B2 receptor agonists. Enzymatic degradation studies performed in vitro and in vivo revealed that BK and R556 are readily degraded by rabbit ACE whereas [Phe8psi(CH2-NH)Arg9]-BK (R379) is totally resistant. BK, R556, and R379 contracted endothelium-denuded veins with similar potencies (pEC50 range 8.10-8.50). Tissues pretreated with ACE-I showed an increase in pEC50 values for BK and R556 but not for R379. ACE-I (captopril, enalaprilat) were unable to prevent B2 receptor desensitisation induced by BK (1 microM). ACE-I partially restored B2 receptor-mediated contraction in tissues initially exposed to BK but not to R379. These effects were antagonised by HOE 140 (0.1 microM) but were unaffected by AcLys[Dbeta-Na...Continue Reading

References

Jan 1, 1979·Canadian Journal of Physiology and Pharmacology·J BarabéD Regoli
Jan 1, 1992·Journal of Cardiovascular Pharmacology·G BönnerC Toussaint
Mar 1, 1991·British Journal of Pharmacology·F J HockJ Knolle
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Jan 1, 1988·Methods in Enzymology·G Drapeau, D Regoli
Apr 1, 1981·Canadian Journal of Physiology and Pharmacology·P GaudreauD Regoli
Nov 1, 1994·The American Journal of Physiology·J F ArnalD G Harrison
Jan 1, 1994·Life Sciences·D RegoliD G Sawutz
Aug 1, 1993·Canadian Journal of Physiology and Pharmacology·D RegoliN E Rhaleb
Feb 1, 1996·Canadian Journal of Physiology and Pharmacology·F GobeilD Regoli
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Citations

Apr 5, 2003·The International Journal of Biochemistry & Cell Biology·Beril TomA H Jan Danser
Dec 20, 2002·International Immunopharmacology·Ervin G Erdös, Peter A Deddish
Sep 5, 2002·British Journal of Pharmacology·Beril TomA H Jan Danser
Apr 7, 2017·Canadian Journal of Physiology and Pharmacology·Domenico Regoli, Fernand Gobeil
Jan 24, 2003·British Journal of Pharmacology·Andreas DendorferPeter Dominiak
Feb 1, 2006·Signal Transduction·Sylvia MuellerSiegmund Reissmann
Apr 28, 2012·Pharmacology & Therapeutics·Domenico RegoliFernand Gobeil

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