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Receptors for kinins in the human isolated umbilical vein
Author(s) -
Gobeil F.,
Pheng L.H.,
Badini I.,
NguyenLe X.K.,
Pizard A.,
Rizzi A.,
Blouin D.,
Regoli D.
Publication year - 1996
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.1996.tb15401.x
Subject(s) - receptor , bradykinin , kinin , receptor antagonist , antagonist , agonist , chemistry , kallidin , competitive antagonist , endocrinology , medicine , pharmacology , biology , biochemistry
1 The human umbilical vein has been found to contract in response to bradykinin (BK) and desArg 9 BK. 2 The rank order of potency of agonists, in the presence of the B 1 receptor antagonist Lys[Leu 8 ]desArg 9 BK, is as follows: [Hyp 3 , Tyr(Me) 8 ]BK (pD 2 8.88) = [Hyp 3 ]BK (pD 2 8.86) = LysBK (pD 2 8.81) ≥BK (pD 2 8.60) > >[Aib 7 ]BK (pD 2 6.38) > >desArg 9 BK and LysdesArg 9 BK (inactive). 3 Hoe 140 (pA 2 8.42) inhibits the effects of BK while other B 2 receptor peptide antagonists are very weak and WIN 64338 is practically inactive. 4 Venoconstrictor responses to desArg 9 BK of fresh tissues increase with time during the in vitro incubation and reach a maximum after 4–6 h. The activity of Hoe 140 (pA 2 5.48) is negligible against B 1 receptor agonists. 5 When measured in the presence of the selective B 2 receptor antagonist Hoe 140 (400 nM), the order of potency of kinin related peptides on the B 1 receptor is Lys[desArg 9 ]BK (pD 2 8.60)>desArg 9 BK (pD 2 6.69). BK, LysBK, [Hyp 3 ]BK and other B 2 receptor agonists are inactive. 6 The B 1 receptor antagonist, Lys[Leu 8 ]desArg 9 BK (pA 2 7.99), inhibits the response of the human vein to B 1 receptor agonists (LysdesArg 9 BK or desArg 9 BK), but do not alter the effect of BK. 7 The results summarized in this paper indicate that the human isolated umbilical vein is a sensitive preparation containing both B 1 and B 2 receptors. The human B 2 receptor shows some similarity with that of the rabbit (at least for agonist potencies) and differs from the B 2 receptor of the guinea‐pig. Compared to the rabbit B 1 receptor, the human B 1 receptor shows low sensitivity to peptides that lack the N‐terminal Lys.