Long term orexigenic effect of a novel melanocortin 4 receptor selective antagonist

British Journal of Pharmacology

Volumn 126, Issue 1, 1999, Pages 27-34

  Skuladottir, Gudrun V ^a   Jonsson, Logi ^b   Skarphedinsson, Jon O ^c   Mutulis, Fciikss ^d   Muceniece, Ruta ^d   Rainc, Amanda ^a   Mutule, Izc ^b   Helgason, Johannes ^c   Prusis, Peteris ^d   Wikberg, Jari E S ^d   Schiöth, Heigi B ^a  

^a UNIVERSITY OF ICELAND   (Iceland)

^b Department of Medicinal Chemistry ^*

^c LATVIAN INSTITUTE OF ORGANIC SYNTHESIS   (Latvia)

^d UPPSALA UNIVERSITY   (Sweden)

Author keywords

Chronic i.c.v. administration; Cyclic AMP; Food intake; HS028; Ligand binding; Melanocortin (MC) receptor subtypes; MSH (melanocyte stimulating hormone)

Indexed keywords

ALPHA INTERMEDIN; APPETITE STIMULANT; BETA INTERMEDIN[11-22][11 (N ACETYLCYSTEINE) 14 (3,4 DICHLORO DEXTRO PHENYLALANINE) 18 CYSTEINE 22 ASPARTIC ACID AMIDE] 11,18 CYCLIC DISULFIDE; BETA INTERMEDIN[11-22][11 (N ACETYLCYSTEINE) 14 [3 (2 NAPHTHYL) DEXTRO ALANINE] 18 CYSTEINE 22 ASPARTIC ACID AMIDE] 11,18 CYCLIC DISULFIDE; CYCLIC AMP; HORMONE RECEPTOR BLOCKING AGENT; INTERMEDIN DERIVATIVE; MELANOCORTIN RECEPTOR; RECEPTOR SUBTYPE; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL TISSUE; APPETITE; ARTICLE; BODY WEIGHT; CONTROLLED STUDY; DOSE RESPONSE; FOOD INTAKE; INTRACEREBROVENTRICULAR DRUG ADMINISTRATION; MALE; NONHUMAN; OSMOTIC MINIPUMP; PRIORITY JOURNAL; RAT; RECEPTOR AFFINITY; TACHYPHYLAXIS;

ALPHA-MSH; ANIMALS; APPETITE STIMULANTS; BINDING, COMPETITIVE; BODY WEIGHT; COS CELLS; CYCLIC AMP; EATING; HUMANS; INFUSIONS, PARENTERAL; INJECTIONS, SUBCUTANEOUS; MALE; MELANOCYTE-STIMULATING HORMONES; PEPTIDE FRAGMENTS; RATS; RATS, WISTAR; RECEPTOR, MELANOCORTIN, TYPE 3; RECEPTOR, MELANOCORTIN, TYPE 4; RECEPTORS, CORTICOTROPIN; RECEPTORS, PITUITARY HORMONE; RECOMBINANT FUSION PROTEINS; WEIGHT GAIN;

EID: 0032892326     PISSN: 00071188     EISSN: None     Source Type: Journal    
DOI: 10.1038/sj.bjp.0702264     Document Type: Article

References (29)

1. ADAN, R.A.H., OOSTEROM, J., LUDVIGSDOTTIR, G., BRAKKEE, J.H., BURBACH, J.P.H. & GISPEN, W.U. (1994). Identification of antagonists for melanocortin MC3, MC4 and MC5 receptors. Ear. J. Pharmacol., 269, 331-337.
2. AL-OBEIDI, F., CASTRUCCI, A.L., HADLEV, M.E. & HRUBY, V.J. (1989). Potent and prolonged acting cyclic lactam analogues of xmclanotropin: Design based on molecular dynamics. J. Mecl. Cliem.. 32, 2555-2561.
3. CHEN W, KELLY MA, OPITZ-ARAYA X, THOMAS RE, LOW MJ, CONE, RD. (1997). Exocrine gland dysfunction in MC5-Rdeficient mice: evidence for coordinated regulation of exocrine gland function by melanocortin peptides. Cell, 91: 789-798.
4. CHHAJLANI, V., MUCEN1ECE, R. & WIKBERG, J.E.S. (1993). Molecular cloning of a novel human melanocortin receptor. Biochem. Biophys. Res. Commun., 195, 866-873.
5. CHHAJLANI, V. & WIKBERG, J.E.S. (1992). Molecular cloning and expression of the human melanocyte stimulating hormone receptor cDNA. FEES Lett., 309, 417-420.
6. CONE, R.D., LU, D., KOPPULA, S., VAGE, D.I., KLUNGLAND, H., BOSTON, B., CHEN, W., ORTII, D.N., POUTON, C. & KESTERSON, R.A. (1996). The melanocortin receptors: agonists, antagonists, and the hormonal control of picmentation. Recent. Prog. Harm. Res., 51,287-317.
7. FAN, W., BOSTON, B.A., KESTERSON, R.A., HRUBY, V.J. & CONE, R.D. (1997). Role of melanocortinergic neurons in feeding and the agouti obesity syndrome. Nature, 385, 165- 168.
8. GANTZ, I., KONDA, Y., TASHIRO, T., SHIMOTO, Y., MIWA, H., MUNZERT, G., WATSON, S.J., DEL VALLE, J. & YAMADA, T. (1993a). Molecular cloning of a novel melanocortin receptor. J. Biol. Cliem.. 268, 8246-8250.
9. GANTZ, I., MIWA, H., KONDA, Y., SHIMOTO, Y., TASHIRO, T., WATSON, S.J., DEL VALLE, V. & YAMADA, T. ( 1993b). Molecular cloning, expression, and gene localization of a fourth melanocortin receptor. J. Biol. Chcm., 268, 15174-15179.
10. HUSZAR, D., LYNCH, C.A., FAIRCHILD-HUNTRESS, V., DUNMORE, J.H., FANG, Q., BERKEMEYER, L.R., GU, W., KESTERSON, R.A., BOSTON, B.A., CONE, R.D., SMITH, F.J., CAMPFIELD, L.A. BURN, P. & LEE, F. (1997). Targeted disruption of the melanocortin-4 receptor results in obesity in mice. Cell, 88, 131-141.
11. HRUBY, V.J., LU, D., SHARMA, S.D., CASTRUCCI, A.L., KESTERSON, R.A., AL-OBEIDI, F.A., HADLEY, M.E. & CONE, R.D. (1995). Cyclic lactam a-melanotropin analogues of Ac-Nle4-cyclo(Asp5, D-Phe7, Lys')a-melanocyte-stimulating hormone-(4-10)-NH2 with bulky aromatic amino acids at position 7 show high antagonist potency and selectivity at specific melanocortin receptors. J. Med. Cheir... 38, 3454-3461.
12. HRUBY, V.J., SHARMA, S.D., TOTH, K., JAW, J.Y., AL-OBEIDI, F., SAWYER, T.K. & HADLEY, M.E. (1993). Design, synthesis, and conformation of superpotent and prolonged acting melanotropins. Ann. N.Y. Acad. Sei., 680, 51-63.
13. KASK, A., RÄGO, L. KORROV1TS, P., WIKBERG, J.E.S. & SCHIoTH, H.B. (1998a). Evidence that the orexigenic eflects of melanocortin 4 receptor antagonist are mediated by NPY. Biochem. Biophys. Res. Commun., 248, 245-249.
14. KASK, A., RAGO, L., MUTULIS, F., WIKBERG, J.E.S. & SCH1ÖTH, H.B. (1998b). Selective melanocortin 4 receptor antagonist (HS014) increases food intake in free-feeding rats. Biochem. Biophys. Res. Commun., 245, 90-93.
15. LEVINE, R.L., MCINTOSH, T.K, LOTHROP, D.A. & JACKSON, B.T. (1980). Orcadian periodicity of plasma corticosterone levels in rats subjected to hemorrhagic shock and surgical trauma. Harm. AM., 13, 385-395.
16. LIPTON, J.M. & CATANIA A. (1997). Anti-inflammatory actions of the neuroimmunomodulator alpha-MSH. Immunol. Toilav, 18, 140-145.
17. MARTI, O., GAVALDA, A., JOLIN, T. & ARMARIO, A. (1996). Acute stress attenuates but does not abolish circadian rhythmicity of serum thyrotrophin and growth hormone in the rat. Enr. J. Emlocrinol., 135, 703-708.
18. MOUNTJOY, K.G., MORTRUD, M.T., LOW, M.J., SIMERLY, R.B. & CONE, R.D. (1994). Localization of the melanocortin-4 receptor (MC4-R) in endocrine and autonomie control circuits in the brain. Molecular Endocrinology, 8, 1298-1308.
19. MOUNTJOY, K.G., ROBBINS, L.S., MORTRUD, M.T. & CONE, R.D. (1992). The cloning of a family of genes that encode the melanocortin receptors. Science, 257, 1248- 1251.
20. NORDSTEDT, C. &. FREDHOLM, B.B. (1990). A modification of a protein-binding method for rapid quantification of cAMP in cellculture supernatants and body fluid. Analytical Chemistry, 189, 231-234.
21. ROSELLI-REHFUSS, L., MOUNTJOY, K.G., ROBBINS, L.S., MORTRUD, M.T., LOW, M.J., TARTO, J.B., ENTWISTLE, M.L., SIMERLY, R.B. & CONE, R.D. (1993). Identification of a receptor for y melanotropin and other proopiomelanocortin peptides in the hypothalamus and limbic system. Proc. Nail. Acail. Sei. U.S.A., 90, 8856-8860.
22. SCHIÖTH, H.B., CHHAJLANI, V., MUCENIECE, R., KLUSA, V. & WIKBERG, J.E.S. (1996a). Major pharmacological distinction of the ACTH receptor from the other melanocortic receptors. Life Sciences, 59, 797-801.
23. SCHIÖTH, H.B., MUCENIECE, R., LARSSON, M., MUTULIS, F., SZARDENINGS, M., PRUS1S, P., LINDEBERG, G. & WIKBERG, J.E.S. (1997b). Selectively of cyclic [D-Phe7] and [D-Nal7] substituted MSH analogues for the melanocortin receptors. Peplicles, 18, 1009-1013.
24. SCHIÖTH, H.B., MUCENIECE, R., WIKBERG, J.E.S. & CHHAJLANI, V. (1995). Characterisation of melanocortin receptor subtypes by radioligand binding analysis. Eur. J. Phannacol., Mot. Pharm. Sect., 288, 311-317.
25. SCHIÖTH, H.B., MUCENIECE, R. & WIKBERG, J.E.S. (1996b). Characterisation of melanocortin 4 receptor by radioligand binding analysis. Pharmacology & Toxicology, 79, 161 -165.
26. SCHIÖTH, H.B., MUCENIECE, R. & WIKBERG, J.E.S. (1997a). Selectively of [Phe-I7], [Ala6] and [D-Ala4, Gln5,Tyr6] substiluled ACTH(4-10) analogues for ihe melanocorlin receplors. Peptides, 18, 761-763.
27. SCHIÖTH, H.B., MUTULIS, F., MUCENIECE, R., PRUSIS, P. & WIKBERG, J.E.S. (1998a). Discovery of novel melanocorlin 4 receptor selective MSH analogues. Br. J. Phannacol., 124, 75-82.
28. SCHIÖTH, H.B., MUTULIS, F., MUCENIECE, R., PRUSIS, P. & WIKBERG, J.E.S. (1998b). Seleclive properties of C- and Nterminals and core residues in the MSH peptide for Ihe melanocorlin receplor sublypes. Eur. J. Phannacol., 349, 359-366.
29. SEELEY RJ, YAGALOFF KA, FISHER SL, BURN P, THIELE TE, VAN DIJK G, BASKIN DG, SCHWARTZ MW. (1997). Melanocorlin receptors in leptin effects. Nature, 390: 349.