Characterization of bradykinin receptors in peripheral organs

1991 ◽  
Vol 69 (7) ◽  
pp. 938-943 ◽  
Author(s):  
Nour-Eddine Rhaleb ◽  
Noureddine Rouissi ◽  
Guy Drapeau ◽  
Daniela Jukic ◽  
Domenico Regoli
Keyword(s):  
Urinary Bladder ◽  
Guinea Pig ◽  
Jugular Vein ◽  
Smooth Muscles ◽  
Rabbit Aorta ◽  
Arachidonic Acid Cascade ◽  
Receptor System ◽  
Kinin Receptors ◽  
Concentration Levels

Bradykinin (BK) and related kinins are potent stimulants of the rabbit jugular vein, the hamster urinary bladder, and the guinea pig trachea. The characterization of kinin receptors in these tissues was made with agonists and antagonists. Results obtained with agonists indicate that bradykinin and kallidin are much more active than des-Arg9-BK and suggest the presence of B2 receptors in the three organs. Some new agonists were also tested and the BK analogue, [Hyp3,Tyr(Me)8]BK, was found to be a potent and selective stimulant of the three preparations, with pD2 values of 8.56, 8.00, and 8.39, respectively, but inactive on the rabbit aorta (a B1-receptor system). Contractile effects of kinins in the rabbit jugular vein and hamster urinary bladder were reduced or eliminated by B2-receptor antagonists but at different concentration levels; e.g., acetyl-D-Arg[Hyp3,D-Phe7]BK showed pA2 values of 7.78 on the rabbit jugular vein but only 5.72 on hamster urinary bladder. This compound contracted the guinea-pig trachea and was found to be inactive as an antagonist on this preparation. Contractions of the hamster urinary bladder and the guinea-pig trachea in response to bradykinin were markedly reduced or eliminated by indomethacin and by BW 755C, while those of the rabbit jugular vein were not modified. The present findings indicate that the myotropic effect of kinins on the rabbit jugular vein depends on the activation of B2 receptors and suggest that B2 receptors are largely responsible also for the response of the hamster urinary bladder. B2 receptors and (or) a nonreceptor mechanism appear to be involved in the stimulant effects of the kinin agonists and some antagonists in the guinea-pig trachea.Key words: bradykinin, B2 receptors, agonists, antagonists, smooth muscles, arachidonic acid cascade, indomethacin, BW 755C.

New agonist and antagonist analogues of bradykinin

1984 ◽  
Vol 62 (6) ◽  
pp. 627-629 ◽  
Author(s):  
J. Barabé ◽  
S. Caranikas ◽  
P. D'Orléans-Juste ◽  
D. Regoli
Keyword(s):  
Guinea Pig ◽  
Jugular Vein ◽  
Rabbit Aorta ◽  
Guinea Pig Ileum ◽  
Receptor System ◽  
Relative Affinity ◽  
Agonist And Antagonist

Three new analogues of bradykinin (BK) have been tested for their agonistic and antagonistic actions on the rabbit jugular vein and the guinea pig ileum (B2 receptors), and six were studied on rabbit aorta strips (B1 receptors). Substitution of Gly4, Phe5, and Phe8 in BK with D-Trp gives analogues with a relative affinity lower than 1.0% as compared with BK. These analogues have no antagonistic properties on the rabbit jugular vein and on guinea pig ileum (B2 receptors). Substitution of Pro7 in des-Arg9-BK by Gly and by D-Ala give compounds that antagonise the effects of kinins on the rabbit aorta strips (B1-receptor system). These new antagonists are fairly potent with a pA2 value of 6.03 to 7.29 and seem competitive because the pA2 – pA10 values approximate 0.95. These results suggest that the orientation of Phe8 is critical for the activation of B1 receptors by kinins.

Effects of kinins on isolated blood vessels. Role of endothelium

1982 ◽  
Vol 60 (12) ◽  
pp. 1580-1583 ◽  
Author(s):  
D. Regoli ◽  
J. Mizrahi ◽  
P. D'Orléans-Juste ◽  
S. Caranikas
Keyword(s):  
Arachidonic Acid ◽  
Carotid Artery ◽  
Common Carotid Artery ◽  
Smooth Muscles ◽  
Rabbit Aorta ◽  
Arachidonic Acid Metabolism ◽  
Arachidonic Acid Cascade ◽  
Vascular Smooth Muscles ◽  
Acid Metabolites

Bradykinin (BK) and des-Arg9-BK were used to determine whether the stimulatory and inhibitory actions of the kinins in various isolated vessels require the presence of endothelium and may be mediated by arachidonic acid metabolites. It was found that the presence of intact endothelium is required only for the relaxation of the dog common carotid artery in response to bradykinin. Stimulatory actions of both BK and des-Arg9-BK in arterial (rabbit aorta) and venous (rabbit jugular and mesenteric vein) smooth muscle do not require the presence of endothelium. Inhibition of the arachidonic acid cascade at various levels affects the relaxing action of acetylcholine (rabbit aorta and dog common carotid artery) while being inactive against both the relaxing (dog common carotid artery) and contractile actions (rabbit aorta, rabbit jugular and mesenteric veins) of bradykinin and des-Arg9-BK. Inhibitors of the arachidonic acid cascade also do not affect the inhibitory action of isopropylnoradrenaline on the rabbit aorta. The present results indicate that stimulant actions of kinins in isolated vascular smooth muscles do not require the presence of endothelium. Endothelium is required for the inhibitory actions of acetylcholine and bradykinin but not for that of isopropylnoradrenaline on the dog carotid artery. Moreover, the inhibition of arachidonic acid metabolism only affects the response of isolated vessels to acetylcholine. The present results suggest that several mechanisms may be involved in the inhibition of vascular tone by vasodilators.

Comparative immunohistochemical characterization of interstitial cells in the urinary bladder of human, guinea pig and pig

2018 ◽  
Vol 149 (5) ◽  
pp. 491-501 ◽  
Author(s):  
Clara Steiner ◽  
Thomas Gevaert ◽  
Roman Ganzer ◽  
Dirk De Ridder ◽  
Jochen Neuhaus
Keyword(s):  
Urinary Bladder ◽  
Guinea Pig ◽  
Interstitial Cells

Pharmacological studies of kinins in venous smooth muscles

1981 ◽  
Vol 59 (4) ◽  
pp. 371-379 ◽  
Author(s):  
P. Gaudreau ◽  
J. Barabé ◽  
S. St-Pierre ◽  
D. Regoli
Keyword(s):  
Guinea Pig ◽  
Jugular Vein ◽  
Biological Activities ◽  
Smooth Muscles ◽  
Response Curves ◽  
Kininase Ii ◽  
Structure Activity ◽  
Hexyl Ester ◽  
Pharmacological Studies ◽  
Specific Receptors

The myotropic effects of bradykinin (BK) and other kinins in two isolated veins, the rabbit jugular and the guinea pig anterior mesenteric, have been studied. The effects of degradation on the biological activities of these compounds and the receptor types mediating their myotropic effects have been determined.It has been found that contractions elicited by kinins in these veins result from direct actions on specific receptors. Both veins contain active kininase II (but not active carboxypeptidases A or B) which interferes with the measurement of the myotropic effects and can be blocked by 1-(D-3-mereapto-2-methyl-3-oxopropyl)-L-proline (SQ 14225). The slopes but not the maxima of the concentration–response curves of BK and other kinins measured in the presence of SQ 14225 are different from those recorded in its absence whereas no significant changes are observed in concentration–response curves obtained with the analogue [D-Phe8]-BK, which resists degradation by kininase II.BK is more potent than its fragment sequence des-Arg9-BK and the effects of kinins are antagonized by dihydrochlorprothixene and β-phenylalanine hexyl ester. These findings suggest that the rabbit jugular and the guinea pig anterior mesenteric veins contain receptors of the B2 type.The findings presented in this paper indicate that the rabbit jugular vein and the guinea pig anterior mesenteric vein are sensitive preparations for kinins and they can be useful for structure–activity studies of these peptides. A correct evaluation of the relative affinities of various kinins is, however, only possible by eliminating the interference of kininase II.

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