Skip to main content
NCBI home page
British Journal of Pharmacology logoLink to British Journal of Pharmacology
. 1996 May;118(2):289–294. doi: 10.1111/j.1476-5381.1996.tb15401.x

Receptors for kinins in the human isolated umbilical vein.

F Gobeil 1, L H Pheng 1, I Badini 1, X K Nguyen-Le 1, A Pizard 1, A Rizzi 1, D Blouin 1, D Regoli 1
PMCID: PMC1909628  PMID: 8735629

Abstract

1. The human umbilical vein has been found to contract in response to bradykinin (BK) and desArg9BK. 2. The rank order of potency of agonists, in the presence of the B1 receptor antagonist Lys[Leu8]desArg9BK, is as follows: [Hyp3, Tyr(Me)8]BK (pD2 8.88) = [Hyp3]BK (pD2 8.86) = LysBK (pD2 8.81) > or = BK (pD2 8.60) >> [Aib7]BK (pD2 6.38) >> desArg9BK and LysdesArg9BK (inactive). 3. Hoe 140 (pA2 8.42) inhibits the effects of BK while other B2 receptor peptide antagonists are very weak and WIN 64338 is practically inactive. 4. Venoconstrictor responses to desArg9BK of fresh tissues increase with time during the in vitro incubation and reach a maximum after 4-6 h. The activity of Hoe 140 (pA2 5.48) is negligible against B1 receptor agonists. 5. When measured in the presence of the selective B2 receptor antagonist Hoe 140 (400 nM), the order of potency of kinin related peptides on the B1 receptor is Lys[desArg9]BK (pD2 8.60) > desArg9BK (pD2 6.69). BK, LysBK, [Hyp3]BK and other B2 receptor agonists are inactive. 6. The B1 receptor antagonist, Lys[Leu8]desArg9BK (pA2 7.99), inhibits the response of the human vein to B1 receptor agonists (LysdesArg9BK or desArg9BK), 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 B1 and B2 receptors. The human B2 receptor shows some similarity with that of the rabbit (at least for agonist potencies) and differs from the B2 receptor of the guinea-pig. Compared to the rabbit B1 receptor, the human B1 receptor shows low sensitivity to peptides that lack the N-terminal Lys.

Full text

PDF
289

Selected References

These references are in PubMed. This may not be the complete list of references from this article.

  1. Altura B. M., Malaviya D., Reich C. F., Orkin L. R. Effects of vasoactive agents on isolated human umbilical arteries and veins. Am J Physiol. 1972 Feb;222(2):345–355. doi: 10.1152/ajplegacy.1972.222.2.345. [DOI] [PubMed] [Google Scholar]
  2. Couture R., Mizrahi J., Regoli D., Devroede G. Peptides and the human colon: an in vitro pharmacological study. Can J Physiol Pharmacol. 1981 Sep;59(9):957–964. doi: 10.1139/y81-146. [DOI] [PubMed] [Google Scholar]
  3. Drapeau G., Regoli D. Synthesis of bradykinin analogs. Methods Enzymol. 1988;163:263–272. doi: 10.1016/0076-6879(88)63025-4. [DOI] [PubMed] [Google Scholar]
  4. Eggerickx D., Raspe E., Bertrand D., Vassart G., Parmentier M. Molecular cloning, functional expression and pharmacological characterization of a human bradykinin B2 receptor gene. Biochem Biophys Res Commun. 1992 Sep 30;187(3):1306–1313. doi: 10.1016/0006-291x(92)90445-q. [DOI] [PubMed] [Google Scholar]
  5. Félétou M., Martin C. A., Molimard M., Naline E., Germain M., Thurieau C., Fauchère J. L., Canet E., Advenier C. In vitro effects of HOE 140 in human bronchial and vascular tissue. Eur J Pharmacol. 1995 Feb 14;274(1-3):57–64. doi: 10.1016/0014-2999(94)00709-g. [DOI] [PubMed] [Google Scholar]
  6. Gobeil F., Regoli D. Characterization of kinin receptors by bioassays. Braz J Med Biol Res. 1994 Aug;27(8):1781–1791. [PubMed] [Google Scholar]
  7. Goldstein R. H., Wall M. Activation of protein formation and cell division by bradykinin and des-Arg9-bradykinin. J Biol Chem. 1984 Jul 25;259(14):9263–9268. [PubMed] [Google Scholar]
  8. Hess J. F., Borkowski J. A., Macneil T., Stonesifer G. Y., Fraher J., Strader C. D., Ransom R. W. Differential pharmacology of cloned human and mouse B2 bradykinin receptors. Mol Pharmacol. 1994 Jan;45(1):1–8. [PubMed] [Google Scholar]
  9. Hess J. F., Borkowski J. A., Young G. S., Strader C. D., Ransom R. W. Cloning and pharmacological characterization of a human bradykinin (BK-2) receptor. Biochem Biophys Res Commun. 1992 Apr 15;184(1):260–268. doi: 10.1016/0006-291x(92)91187-u. [DOI] [PubMed] [Google Scholar]
  10. Hock F. J., Wirth K., Albus U., Linz W., Gerhards H. J., Wiemer G., Henke S., Breipohl G., König W., Knolle J. Hoe 140 a new potent and long acting bradykinin-antagonist: in vitro studies. Br J Pharmacol. 1991 Mar;102(3):769–773. doi: 10.1111/j.1476-5381.1991.tb12248.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  11. MacNeil T., Bierilo K. K., Menke J. G., Hess J. F. Cloning and pharmacological characterization of a rabbit bradykinin B1 receptor. Biochim Biophys Acta. 1995 Nov 7;1264(2):223–228. doi: 10.1016/0167-4781(95)00152-7. [DOI] [PubMed] [Google Scholar]
  12. Marceau F. Kinin B1 receptors: a review. Immunopharmacology. 1995 Jun;30(1):1–26. doi: 10.1016/0162-3109(95)00011-h. [DOI] [PubMed] [Google Scholar]
  13. Marceau F., Levesque L., Drapeau G., Rioux F., Salvino J. M., Wolfe H. R., Seoane P. R., Sawutz D. G. Effects of peptide and nonpeptide antagonists of bradykinin B2 receptors on the venoconstrictor action of bradykinin. J Pharmacol Exp Ther. 1994 Jun;269(3):1136–1143. [PubMed] [Google Scholar]
  14. McEachern A. E., Shelton E. R., Bhakta S., Obernolte R., Bach C., Zuppan P., Fujisaki J., Aldrich R. W., Jarnagin K. Expression cloning of a rat B2 bradykinin receptor. Proc Natl Acad Sci U S A. 1991 Sep 1;88(17):7724–7728. doi: 10.1073/pnas.88.17.7724. [DOI] [PMC free article] [PubMed] [Google Scholar]
  15. Menke J. G., Borkowski J. A., Bierilo K. K., MacNeil T., Derrick A. W., Schneck K. A., Ransom R. W., Strader C. D., Linemeyer D. L., Hess J. F. Expression cloning of a human B1 bradykinin receptor. J Biol Chem. 1994 Aug 26;269(34):21583–21586. [PubMed] [Google Scholar]
  16. Regoli D., Barabé J., Park W. K. Receptors for bradykinin in rabbit aortae. Can J Physiol Pharmacol. 1977 Aug;55(4):855–867. doi: 10.1139/y77-115. [DOI] [PubMed] [Google Scholar]
  17. Regoli D., Barabé J. Pharmacology of bradykinin and related kinins. Pharmacol Rev. 1980 Mar;32(1):1–46. [PubMed] [Google Scholar]
  18. Regoli D., Boudon A., Fauchére J. L. Receptors and antagonists for substance P and related peptides. Pharmacol Rev. 1994 Dec;46(4):551–599. [PubMed] [Google Scholar]
  19. Regoli D., Gobeil F., Nguyen Q. T., Jukic D., Seoane P. R., Salvino J. M., Sawutz D. G. Bradykinin receptor types and B2 subtypes. Life Sci. 1994;55(10):735–749. doi: 10.1016/0024-3205(94)00557-5. [DOI] [PubMed] [Google Scholar]
  20. Regoli D., Jukic D., Gobeil F., Rhaleb N. E. Receptors for bradykinin and related kinins: a critical analysis. Can J Physiol Pharmacol. 1993 Aug;71(8):556–567. doi: 10.1139/y93-079. [DOI] [PubMed] [Google Scholar]
  21. Regoli D., Rhaleb N. E., Dion S., Drapeau G. New selective bradykinin receptor antagonists and bradykinin B2 receptor characterization. Trends Pharmacol Sci. 1990 Apr;11(4):156–161. doi: 10.1016/0165-6147(90)90067-I. [DOI] [PubMed] [Google Scholar]
  22. Rhaleb N. E., Drapeau G., Dion S., Jukic D., Rouissi N., Regoli D. Structure-activity studies on bradykinin and related peptides: agonists. Br J Pharmacol. 1990 Mar;99(3):445–448. doi: 10.1111/j.1476-5381.1990.tb12947.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  23. Rhaleb N. E., Télémaque S., Rouissi N., Dion S., Jukic D., Drapeau G., Regoli D. Structure-activity studies of bradykinin and related peptides. B2-receptor antagonists. Hypertension. 1991 Jan;17(1):107–115. doi: 10.1161/01.hyp.17.1.107. [DOI] [PubMed] [Google Scholar]
  24. Salvino J. M., Seoane P. R., Douty B. D., Awad M. M., Dolle R. E., Houck W. T., Faunce D. M., Sawutz D. G. Design of potent non-peptide competitive antagonists of the human bradykinin B2 receptor. J Med Chem. 1993 Aug 20;36(17):2583–2584. doi: 10.1021/jm00069a021. [DOI] [PubMed] [Google Scholar]
  25. Wirth K., Hock F. J., Albus U., Linz W., Alpermann H. G., Anagnostopoulos H., Henk S., Breipohl G., König W., Knolle J. Hoe 140 a new potent and long acting bradykinin-antagonist: in vivo studies. Br J Pharmacol. 1991 Mar;102(3):774–777. doi: 10.1111/j.1476-5381.1991.tb12249.x. [DOI] [PMC free article] [PubMed] [Google Scholar]

Articles from British Journal of Pharmacology are provided here courtesy of The British Pharmacological Society

RESOURCES