Dual antagonists of the bradykinin B1 and B2 receptors based on a postulated common pharmacophore from existing non-peptide antagonists

Biological Chemistry

Volumn 387, Issue 2, 2006, Pages 189-194

  Morissette, Guillaume ^a   Bouthillier, Johanne ^a   Marceau, François ^a  

^a LAVAL UNIVERSITY   (Canada)

Author keywords

Bradyzide; LF16 0687; Rabbit aorta; Radioligand binding assay; Smooth muscle cells

Indexed keywords

2 [3 OXO 1 (BENZENE 4 SULFONYL) 1,2,3,4 4H QUINOXALIN 2 YL] N [4 (METHYLOXYFORMYL)PHENYL]ACETAMIDE; 2 [3 OXO 1 (TOLUENE 4 SULFONYL) 1,2,3,4 4H QUINOXALIN 2 YL] N PHENYLACETAMIDE; 3 (TOLUENE 4 SULFONYLAMINO)PROPIONIC ACID ETHYL ESTER; [1 [[2,4 DICHLORO 3 [(2,4 DIMETHYLQUINOLIN 8 YL)OXY]METHYL]PHENYL]SULFONYL] N [3 [[4 (AMINOIMINOMETHYL)PHENYL]CARBONYLAMINO]PROPYL]PYRROLIDINECARBOXAMIDE; ANATIBANT; BRADYKININ B1 RECEPTOR; BRADYKININ B1 RECEPTOR ANTAGONIST; BRADYKININ B2 RECEPTOR; BRADYKININ B2 RECEPTOR ANTAGONIST; BRADYZIDE; ETHYL 2 [3 [(1 PHENYLSULFONYL 1H INDOL 2 YL)CARBONYL] 1,4,5,6 TETRAHYDROPYRIDIN 1 YL]ETHANOATE; N (4 ETHOXYPHENYL) 3 (TOLUENE 4 SULFONYLAMINO)PROPIONAMIDE; N [2 [4 (4,5 DIHYDRO 1H IMIDAZOL 2 YL)PHENYL]ETHYL] 2 [1 (2 NAPHTHYLSULFONYL) 3 OXO 1,2,3,4 TETRAHYDROQUINOXALIN 2 YL]ACETAMIDE; UNCLASSIFIED DRUG;

AORTA; CONFERENCE PAPER; DATA BASE; IC 50; MOLECULE; MUSCLE CONTRACTILITY; NONHUMAN; PHARMACOPHORE; PRIORITY JOURNAL; RABBIT; RADIOASSAY; RECEPTOR BINDING; SMOOTH MUSCLE FIBER;

ACETANILIDES; ANIMALS; AORTA; BINDING SITES; BINDING, COMPETITIVE; CELLS, CULTURED; MOLECULAR STRUCTURE; MUSCLE, SMOOTH; PYRROLIDINES; QUINOLINES; QUINOXALINES; RABBITS; RECEPTOR, BRADYKININ B1; RECEPTOR, BRADYKININ B2; STRUCTURE-ACTIVITY RELATIONSHIP; SULFONES; THIOSEMICARBAZONES; TOSYL COMPOUNDS;

ORYCTOLAGUS CUNICULUS;

EID: 32344433548     PISSN: 14316730     EISSN: None     Source Type: Journal    
DOI: 10.1515/BC.2006.025     Document Type: Conference Paper

References (21)

1. Dziadulewicz, E.K. (2005). Non-peptide ligands for bradykinin receptors 1995-2004. Expert Opin. Ther. Patents 15, 829-859.
2. 1 receptors in cultured cells. Am. J. Physiol. Heart Circ. Physiol. 284, H1647-H1654.
3. 1 receptors in the rabbit aorta. J. Pharmacol. Exp. Ther. 314, 1169-1174.
4. Ha, S.N., Hey, P.J., Ransom, R.W., Harrell, C.M. Jr., Murphy, K.L., Chang, R., Chen, T.B., Su, D.S., Markowitz, M.K., Bock, M.G., et al. (2005). Binding modes of dihydroquinoxalinones in a homology model of bradykinin receptor 1. Biochem. Biophys. Res. Commun. 331, 159-166.
5. 2 receptor. Hypertension 35, 1319-1325.
6. 1 antagonists: SAR studies in the 2,3-diaminopyridine series. Bioorg. Med. Chem. Lett. 15, 3925-3929.
7. Leeb-Lundberg, L.M.F., Marceau, F., Müller-Esterl, W., Pettibone, D.J., and Zuraw, B.L. (2005). International Union of Pharmacology. XLV. Classification of the kinin receptor family: from molecular mechanisms to pathophysiological consequences. Pharmacol. Rev. 57, 27-77.
8. 1 receptor. Trends Pharmacol. Sci. 26, 116-118.
9. Marceau, F. and Regoli, D. (2004). Bradykinin receptor ligands: therapeutic perspectives. Nat. Rev. Drug Discov. 3, 845-852.
10. 2 receptor. Peptides 22, 1397-1402.
11. 2 receptor. Int. Immunopharmacol. 3, 1529-1536.
12. 2 bradykinin receptor. Modeling of non-peptidic ligand action and comparison to the rhodopsin structure. J. Biol. Chem. 276, 41100-41111.
13. 2+ signaling in single vascular smooth muscle cells. Mol. Pharmacol. 50, 128-139.
14. 1 receptor: effects at the rabbit receptor. J. Pharmacol. Exp. Ther. 311, 1121-1130.
15. 2 receptor antagonist. Immunopharmacology 43, 187-194.
16. 1 receptor antagonist. Eur. J. Pharmacol. 499, 77-84.
17. 1 receptor based on a 2-alkylamino-5- sulfamoylbenza-mide core. J. Med. Chem. 47, 4642-4644.
18. 1 receptor in fresh or cultured rabbit aortic smooth muscle: role of NF-κB. Am. J. Physiol. Heart Circ. Physiol. 283, H227-H237.
19. 1 receptor antagonist. J. Am. Chem. Soc. 125, 7516-7517.
20. 1 receptor occupancy studies. Bioorg. Med. Chem. Lett. 14, 6045-6048.
21. 9-bradykinin and bradykinin. J. Pharmacol. Exp. Ther. 264, 930-937.