Abstract
We investigated the effect of the nonpeptide bradykinin receptor antagonist, [[4-[[2-[[bis(cyclohexylamino)methylene] amino]-3-(2-naphthalenyl) 1-oxopropyl]amino]-phenyl]-tributyl, chloride, monohydrochloride (WIN 64338), on [3H]-bradykinin binding and on bradykinin-induced contraction of the guinea-pig trachea. This non peptide bradykinin receptor antagonist inhibited [3H]-bradykinin binding with a nanomolar range of affinity, Ki = 50.9 +/- 19 nM and inhibited bradykinin-induced contraction in a non-competitive manner with a KB value of 6.43 10(-8) +/- 2.34 10(-8) M.
Full text
PDF
Selected References
These references are in PubMed. This may not be the complete list of references from this article.
- Farmer S. G., DeSiato M. A. Effects of a novel nonpeptide bradykinin B2 receptor antagonist on intestinal and airway smooth muscle: further evidence for the tracheal B3 receptor. Br J Pharmacol. 1994 Jun;112(2):461–464. doi: 10.1111/j.1476-5381.1994.tb13095.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Kyle D. J., Martin J. A., Burch R. M., Carter J. P., Lu S. F., Meeker S., Prosser J. C., Sullivan J. P., Togo J., Noronha-Blob L. Probing the bradykinin receptor: mapping the geometric topography using ethers of hydroxyproline in novel peptides. J Med Chem. 1991 Aug;34(8):2649–2653. doi: 10.1021/jm00112a047. [DOI] [PubMed] [Google Scholar]
- 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]
- Trifilieff A., Amrani Y., Landry Y., Gies J. P. Comparative action of new highly potent bradykinin receptor antagonists in the guinea-pig trachea. Eur J Pharmacol. 1993 Aug 3;239(1-3):227–229. doi: 10.1016/0014-2999(93)91000-d. [DOI] [PubMed] [Google Scholar]
- Trifilieff A., Da Silva A., Landry Y., Gies J. P. Effect of Hoe 140, a new B2 noncompetitive antagonist, on guinea pig tracheal bradykinin receptors. J Pharmacol Exp Ther. 1992 Dec;263(3):1377–1382. [PubMed] [Google Scholar]
- Vavrek R. J., Stewart J. M. Competitive antagonists of bradykinin. Peptides. 1985 Mar-Apr;6(2):161–164. doi: 10.1016/0196-9781(85)90033-6. [DOI] [PubMed] [Google Scholar]
- 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]