The neuromedin B receptor antagonist, BIM-23127, is a potent antagonist at human and rat urotensin-II receptors

British Journal of Pharmacology

Volumn 139, Issue 2, 2003, Pages 203-207

  Herold, Christopher L ^a   Behm, David J ^a   Buckley, Peter T ^a   Foley, James J ^a   Wixted, William E ^a   Sarau, Henry M ^a   Douglas, Stephen A ^a  

^a GLAXOSMITHKLINE   (United States)

Author keywords

BIM 23127; GPR14; Neuromedin B; Urotensin II; UT receptor

Indexed keywords

BIM 23127; CALCIUM; NEUROMEDIN B; PD 168368; RECEPTOR BLOCKING AGENT; RECEPTOR PROTEIN; RECOMBINANT RECEPTOR; SOMATOSTATIN 14; SOMATOSTATIN DERIVATIVE; UNCLASSIFIED DRUG; UROTENSIN II; UROTENSIN II RECEPTOR;

ANIMAL TISSUE; AORTA CONSTRICTION; ARTICLE; BINDING ASSAY; CALCIUM CELL LEVEL; CALCIUM MOBILIZATION; COMPETITIVE INHIBITION; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG ACTIVITY; DRUG EFFECT; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG SELECTIVITY; EMBRYO; HUMAN; HUMAN CELL; HUMAN CELL CULTURE; IC 50; MALE; NONHUMAN; PRIORITY JOURNAL; PROTEIN EXPRESSION; RAT;

ANIMALS; AORTA, THORACIC; BINDING, COMPETITIVE; CALCIUM; CELL LINE; DOSE-RESPONSE RELATIONSHIP, DRUG; HUMANS; MALE; PEPTIDES, CYCLIC; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, BOMBESIN; RECEPTORS, G-PROTEIN-COUPLED; UROTENSINS;

EID: 0038606902     PISSN: 00071188     EISSN: None     Source Type: Journal    
DOI: 10.1038/sj.bjp.0705251     Document Type: Article

References (21)

1. AMES, R.S., SARAU, H.M., CHAMBERS, J.K., WILLETTE, R.N., AIYAR, N.V., ROMANIC, A.M., LOUDEN, C.S., FOLEY, J.J., SAUERMELCH, C.F., COATNEY, R.W., AO, Z., DISA, J., HOLMES, S.D., STADEL, J.M., MARTIN, J.D., LIU, W.S., GLOVER, G.I., WILSON, S., McNULTY, D.E., ELLIS, C.E., ELSHOURBAGY, N.A., SHABON, U., TRILL, J.J., HAY, D.W.P., OHLSTEIN, E.H., BERGSMA, D.J. & DOUGLAS, S.A. (1999). Human urotensin-II is a potent vasoconstrictor and agonist for the orphan receptor GPR14. Nature, 401, 282-286.
2. BEHM, D.J., HEROLD, C.L., OHLSTEIN, E.H., KNIGHT, S.D., DHANAK, D. & DOUGLAS, S.A. (2002). Pharmacological characterization of SB-710411 (Cpa-c[D-Cys-Pal-D-Trp- Lys- Val-Cys]-Cpa-amide), a novel peptidic urotensin-II receptor antagonist. Br. J. Pharmacol., 137, 449-458.
3. CAMARDA, V., GUERRINI, R., KOSTENIS, E., RIZZI, A., CALO, G., HATTENBERGER, A., ZUCCHINI, M., SALVADORI, S. & REGOLI, D. (2002). A new ligand for the urotensin II receptor. Br. J. Pharmacol., 137, 311-314.
4. COULOUARN, Y., LIHRMANN, I., JEGOU, S., ANOUAR, Y., TOSTIVINT, H., BEAUVILLAIN, J.C., CONLON, J.M., BERN, H.A. & VAUDRY, H. (1998). Cloning of the cDNA encoding the urotensin II precursor in frog and human reveals intense expression of the urotensin II gene in motoneurons of the spinal cord. Proc. Natl. Acad. Sci. USA, 95, 15803-15808.
5. DOUGLAS, S.A. & OHLSTEIN, E.H. (2000a). Human urotensin-II, the most potent mammalian vasoconstrictor identified to date, as a therapeutic target for the management of cardiovascular disease. Trends Cardiovasc Med., 10, 229-237.
6. DOUGLAS, S.A. & OHLSTEIN, E.H. (2000b). Urotensin receptors. In: The IUPHAR Compendium of Receptor Characterization and Classification. ed. Girdlestone, D. pp. 365-372. London: IUPHAR Media.
7. DOUGLAS, S.A., SULPIZIO, A.C., PIERCY, V., SARAU, H.M., AMES, R.S., AIYAR, N.V., OHLSTEIN, E.H. & WILLETTE, R.N. (2000c). Differential vasoconstrictor activity of human urotensin-II in vascular tissue isolated from the rat, mouse, dog, pig, marmoset and cynomolgus monkey. Br. J. Pharmacol., 131, 1262-1274.
8. DOUGLAS, S.A., TAYARA, L., OHLSTEIN, E.H., HALAWA, N. & GIAID, A. (2002). Congestive heart failure and expression of myocardial urotensin II. Lancet., 359, 1990-1997.
9. FLOHR, S., KURZ, M., KOSTENIS, E., BRKOVICH, A., FOURNIER, A. & KLABUNDE, T. (2002). Identification of nonpeptidic urotensin II receptor antagonists by virtual screening based on a pharmacophore model derived from structure - activity relationships and nuclear magnetic resonance studies on urotensin II. J. Med. Chem., 45, 1799-1805.
10. HEROLD, C.L., BEHM, D.J., AIYAR, N.V., NASELSKY, D.P., KNIGHT, S.D., DHANAK, D. & DOUGLAS, S.A. (2001). The somatostatin derivative, Cpa-c-[D-Cys-Pal-D-Trp-Lys-Val-Cys]-Cpa-amide, is an agonist at the human UT receptor but not the rat UT receptor in transfected HEK293 cells. Pharmacologist, 43, 189.
11. KINNEY, W.A., ALMOND, H.R., QI, J., SMITH, C.E., SANTULLI, R.J., DE GARAVILLA, L., ANDRADE-GORDON, P., CHO, D.S., EVERSON, A.M., FEINSTEIN, M.A., LEUNG, P.A. & MARYANOFF, B.E. (2002). Structure - function analysis of urotensin II and its use in the construction of a ligand-receptor working model. Angew. Chem. Int. Ed., 41, 2940-2944.
12. LACH, E.B., BROAD, S. & ROZENGURT, E. (1995). Mitogenic signaling by transfected neuromedin B receptors in Rat-1 cells. Cell Growth Differ., 6, 1427-1435.
13. MATSUSHITA, M., SHICHIRI, M., IMAI, T., IWASHINA, M., TANAKA, H., TAKASU, N. & HIRATA, Y. (2001). Co-expression of urotensin II and its receptor (GPR14) in human cardiovascular and renal tissues. J. Hypertens., 19, 2185-2190.
14. OHSAKO, S., ISHIDA, I., ICHIKAWA, T. & DEGUCHI, T. (1986). Cloning and sequence analysis of cDNAs encoding precursors of urotensin II-alpha and -gamma. J. Neurosci., 6, 2730-2735.
15. ORBUCH, M., TAYLOR, J.E., COY, D.H., MROZINSKI, J.E., JR., MANTEY, S.A., BATTEY, J.F., MOREAU, J.P. & JENSEN, R.T. (1993). Discovery of a novel class of neuromedin B receptor antagonists, substituted somatostatin analogues. Mol. Pharmacol., 44, 841-850.
16. PAYSANT, J., RUPIN, A., SIMONET, S., FABIANI, J.N. & VERBEUREN, T.J. (2001). Comparison of the contractile responses of human coronary bypass grafts and monkey arteries to human urotensin-II. Fundam. Clin. Pharmacol., 15, 227-231.
17. PEARSON, D., SHIVELY, J.E., CLARK, B.R., GESCHWIND, II., BARKLEY, M., NISHIOKA, R.S. & BERN, H.A. (1980). Urotensin II: a somatostatin-like peptide in the caudal neurosecretory system of fishes. Proc. Natl. Acad. Sci. U.S.A., 77, 5021-5024.
18. ROSSOWSKI, W.J., CHENG, B.L., TAYLOR, J.E., DATTA, R. & COY, D.H. (2002). Human urotensin II-induced aorta ring contractions are mediated by protein kinase C, tyrosine kinases and Rho-kinase: inhibition by somatostatin receptor antagonists. Eur. J. Pharmacol., 438, 159-170.
19. RUSSELL, F.D., MOLENAAR, P. & O'BRIEN, D.M. (2001). Cardiostimulant effects of urotensin-II in human heart in vitro. Br. J. Pharmacol., 132, 5-9.
20. WATANABE, T., PAKALA, R., KATAGIRI, T. & BENEDICT, C.R. (2001). Synergistic effect of urotensin II with mildly oxidized LDL on DNA synthesis in vascular smooth muscle cells. Circulation, 104, 16-18.
21. ZOU, Y., NAGAI, R. & YAMAZAKI, T. (2001). Urotensin II induces hypertrophic responses in cultured cardiomyocytes from neonatal rats. FEBS Lett., 508, 57-60.