[Kinin B1 and B2 receptor antagonists and therapeutic perspectives].
Physiological and pathological effects of kinins result from the activation of specific receptors which are present in various organs. Kinin receptors have been characterized through studies on isolated organs in vitro and have been classified as B1 and B2. A careful analysis of B2 receptors led to the identification of two subtypes, namely B2rb (in the rabbit) and B2gp (in the guinea-pig). The distinction between B2rb and B2gp receptors is primarily based on differences in the activities of selective agonists and particularly on differences in affinities of competitive antagonists, namely DArg[Hyp3,DPhe7,Leu8]BK and the non-peptide compound, WIN 64338. The non-competitive antagonist, HOE 140, has shown the same affinity on B2rb and B2gp. The potential role of B1 and B2 receptors in physiopathology is analysed on data obtained with specific and selective antagonists of the B1 (desArg9[Leu8]BK) and B2 (HOE140) receptors. The therapeutic potential of endogenous kinins as mediators of the therapeutic beneficial effects of the angiotensin-converting enzyme inhibitors or the potential of the use of exogenous kinins in the vascular permeability are discussed together with the therapeutic potential of B1 and B2 receptor antagonists.
Regoli
D
D
Département de pharmacologie, Faculté de médecine, Université de Sherbrooke, Québec, Canada.
Jukic
D
D
Gobeil
F
F
D000818:Animals; D004285:Dogs; D007705:Kinins / Q000502:physiology / Q000627:therapeutic use; D011817:Rabbits; D017981:Receptors, Neurotransmitter / Q000819:agonists / Q000037:antagonists & inhibitors* / Q000145:classification / Q000502:physiology
D007705:Kinins; D017981:Receptors, Neurotransmitter
Antagonistes de récepteurs B1 et B2 des kinines et perspectives thérapeutiques.