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1 Research Center, Pavillon Hotel-Dieu, CHUQ, Quebec City, PQ, Canada
2 Institute of Pharmacology, University of Sherbrooke, Sherbrooke, PQ, Canada
3 Faculty of Pharmacy, University of Montreal, Montreal, PQ, Canada
4 Institute of Pharmacology, University of Ferrara, Ferrara, Italy
* To whom correspondence should be addressed. E-mail: francois.marceau{at}crhdq.ulaval.ca.
It has been recently claimed that the human B1 receptors for kinins bind angiotensin converting enzyme (ACE) inhibitors via a potential zinc binding domain and are pharmacologically stimulated by these drugs. We verified whether ACE inhibitors stimulate B1 receptors in vitro. The isolated rabbit aorta or mouse stomach responded by negligible contractions to the application of captopril, enalaprilat or zofenoprilat. The human isolated umbilical vein also failed to respond to enalaprilat. All these preparations were responsive to the B1 receptor agonists des-Arg9-BK or Lys-des-Arg9-BK. Further, enalaprilat applied continuously had no significant interaction with the effects of Lys-des-Arg9-BK on the rabbit aorta. Enalaprilat failed to stimulate [3H]arachidonate release, translocate the receptors (confocal microscopy) or stimulate ERK1/2 phosphorylation (immunoblot) in HEK 293 cells stably expressing the rabbit B1 receptor conjugated to yellow fluorescent protein. The phospho-ERK1/2 content of arterial smooth muscle cells of human or rabbit origin was increased by treatment with Lys-des-Arg,9-BK, but not with enalaprilat. ACE inhibitors do not act as bona fide agonists of the kinin B1 receptors.
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