Discovery of a novel superpotent and selective melanocortin-4 receptor antagonist (HS024): Evaluation in vitro and in vivo

Endocrinology

Volumn 139, Issue 12, 1998, Pages 5006-5014

  Kask, Ants ^a   Mutulis, Felikss ^b,c   Muceniece, Ruta ^b,c   Pähkla, Rein ^a   Mutule, Ilze ^b,c   Wikberg, Jarl E S ^c   Rägo, Lembit ^a   Schiöth, Helgi B ^c,d  

^a UNIVERSITY OF TARTU   (Estonia)

^b LATVIAN INSTITUTE OF ORGANIC SYNTHESIS   (Latvia)

^c UPPSALA UNIVERSITY   (Sweden)

^d UPPSALA UNIVERSITY   (Sweden)

Author keywords

[No Author keywords available]

Indexed keywords

HS 024; INTERMEDIN DERIVATIVE; MELANOCORTIN RECEPTOR; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL TISSUE; ANOREXIA; ANXIETY; ARTICLE; DOSE RESPONSE; DRUG MECHANISM; DRUG POTENCY; DRUG SELECTIVITY; EMOTION; INTRACEREBROVENTRICULAR DRUG ADMINISTRATION; LOCOMOTION; MALE; NONHUMAN; PRIORITY JOURNAL; RAT; RECEPTOR AFFINITY;

EID: 0031786114     PISSN: 00137227     EISSN: None     Source Type: Journal    
DOI: 10.1210/endo.139.12.6352     Document Type: Article

References (49)

1. Chhajlani V, Wikberg JES 1992 Molecular cloning and expression of the human melanocyte stimulating hormone receptor cDNA FEBS Lett 309:417-420
2. Mountjoy KG, Rabbins LS, Mortrud MT, Cone RD 1992 The cloning of a family of genes that encode the melanocortin receptors. Science 257:1248-1251
3. Gantz I, Y, Tashiro T, Shimoto Y, Miwa H, Munzert G, Watson SJ, Del Valle J, Yamada T 1993 Molecular cloning of a novel melanocortin receptor. J Biol Chem 268:8246-8250
4. Gantz I, Miwa H, Konda Y, Shimoto Y, Tashiro T, Watson SJ, DelValle J, Yamada T 1993 Molecular cloning, expression, and gene localization of a fourth melanocortin receptor. J Biol Chem 268:15174-15179
5. Chhajlani V, Muceniece R, Wikberg, JES 1993 Molecular cloning of a novel human melanocortin receptor. Biochem Biophys Res Commun 195:866-873
6. Cone RD, Lu D, Koppula S, Vage DI, Klungland H, Boston B, Chen W, Orth DN, Pouton C, Kesterson RA 1996 The melanocortin receptors: agonists, antagonists, and the hormonal control of pigmentation. Recent Prog Horm Res 51:287-317
7. Roselli-Rehfuss L, Mountjoy KG, Robbins LS, Mortrud MT, Low MJ, Tatro JB, Entwistle ML, Simerly RB, Cone RD 1993 Identification of a receptor for melanotropin and other proopiomelanocortin peptides in the hypothalamus and limbic system. Proc Natl Acad Sci USA 90:8856-8860
8. Mountjoy KG, Mortrud MT, Low MJ, Simerly RB, Cone RD 1994 Localization of the melanocortin-4 receptor (MC4-R) in endocrine and autonomic control circuits in the brain. Mol Endocrinol 8:1298-1308
9. Huszar D, Lynch CA, Fairchild-Huntress V, Dunmore JH, Fang Q, Berkemeier LR, Gu W, Kesterson RA, Boston BA, Cone RD, Smith FJ, Campfield LA, Burn P, Lee F 1997 Targeted disruption of the melanocortin-4 receptor results in obesity in mice. Cell 88:131-141
10. Chen W, Kelly MA, Opitz-Araya X, Thomas RE, Low MJ, Cone RD 1997 Exocrine gland dysfunction in MC5-R-deficient mice: evidence for coordinated regulation of exocrine gland function by melanocortin peptides. Cell 91:789-798
11. Schiöth HB, Muceniece R, Wikberg JES, Chhajlani V 1995 Characterisation of melanocortin receptor subtypes by radioligand binding analysis. Eur J Pharmacol 288:311-317
12. Schiöth HB, Muceniece R, Wikberg JES 1996 Characterisation of melanocortin 4 receptor by radioligand binding analysis. Pharmacol Toxicol 79:161-165
13. Schiöth HB, Chhajlani V, Muceniece R, Klusa V, Wikberg JES 1996 Major pharmacological distinction of the ACTH receptor from the other melanocortic receptors. Life Sci 59:797-801
14. 2 with bulky aromatic amino acids at position 7 show high antagonist potency and selectivity at specific melanocortin receptors. J Med Chem 38:3454-3461
15. Schiöth HB, Mutulis F, Muceniece R, Prusis P, Wikberg JES 1998 Discovery of novel melanocortin 4 receptor selective MSH analogues. Br J Pharmacol 124:75-82
16. Li SJ, Varga K, Archer P, Hruby VJ, Sharma SD, Kesterson RA, Cone RD, Kunos G 1996 Melanocortin antagonists define two distinct pathways of cardiovascular control by α- and γ-melanocyte-stimulating hormones. J Neurosci 16:5182-5188
17. Fan W, Boston BA, Kesterson RA, Hruby VJ, Cone RD 1997 Role of melanocortinergic neurons in feeding and the agouti obesity syndrome. Nature 385:165-168
18. Seeley RJ, Yagaloff KA, Fisher SL, Burn P, Thiele TE, van Dijk G, Baskin DG, Schwartz MW 1997 Melanocortin receptors in leptin effects. Nature 390:349
19. Kask A, Rägo L, Mutulis F, Pähkla R, Wikberg JES, Schiöth HB 1998 Selective antagonist for the melanocortin 4 receptor (HS014) increases food intake in free-feeding rats. Biochem Biophys Res Commun 245:90-93
20. Kask A, Rägo L, Korrovits P, Wikberg JES, Schiöth HB 1998 Evidence that orexigenic effects of melanocortin 4 receptor antagonist HS014 are mediated by neuropeptide Y. Biochem Biophys Res Commun 248:245-249
21. Tagliaferro AR, Levitsky DA 1982 Spillage behavior and thiamin deficiency in the rat. Physiol Behav 28:933-937
22. Gonzales MI, Vaziri S, Wilson, CA 1996 Behavioral effects of α-MSH and MCH after central administration in the female rat. Peptides 17:171-177
23. Panksepp J, Abbott BB 1990 Modulation of separation distress by α-MSH. Peptides 11:647-653
24. Panksepp J, Normansell L 1990 Effects of ACTH(1-24) and ACTH/MSH-(4-10) on isolation-induced distress vocalization in domestic chicks. Peptides 11:915-919
25. 1-24: interaction with benzodiazepines. Pharmacol Biochem Behav 36:631-634
26. 7]a-melanocyte stimulating hormone: a highly potent α-melanotropin with ultralong biological activity. Proc Natl Acad Sci USA 77:5754-5758
27. Nordstedt C, Fredholm BB 1990 A modification of a protein-binding method for rapid quantification of cAMP in cell-culture supernatants and body fluid. Anal Chem 189:231-234
28. Pellow S, Chopin P, File SE, Briley, M 1985 Validation of open:closed arm entries in an elevated plus-maze as a measure of anxiety in the rat. J Neurosci Methods 14:144-167
29. 7] substituted MSH analogues for the melanocortin receptors. Peptides 18:1009-1013
30. 1 receptor antagonist BIBP3226 in rats. Neuroreport 8:3645-3647
31. 13-36 microinjected into vicinity of locus coeruleus in rats. Brain Res 788:345-348
32. Broadhurst PL 1975 The Maudsley reactive and nonreactive strains of rats: a survey. Behav Genet 5:299-319
33. 10]melanotropin analogues. J Med Chem 28:125-129
34. 10]-α-melanocyte stimulating hormone; a cyclic α-melanotropin exibiting super-agonist biological activity. Proc Natl Acad Sci USA 79:1751-1755
35. Eberle AN 1988 The Melanotropins: Chemistry, Physiology and Mechanisms of Action. Karger, Basel
36. Al-Obeidi F, Castrucci AL, Hadley ME, Hruby VJ 1989 Potent and prolonged acting cyclic lactam analogues of α-melanotropin: design based on molecular dynamics. J Med Chem 32:2555-2561
37. Schiöth HB, Mutulis F, Muceniece R, Prusis P, Wikberg JES 1998 Selective properties of C- and N-terminals and core residues in the melanocortin stimulating hormone peptide for the melanocortin receptor subtypes. Eur J Pharmacol 349:359-366
38. Jayawickreme CK, Quillan JM, Graminski GF, Lerner MR 1994 Discovery and structure-function analysis of a-melanocyte-stimulating hormone antagonists. J Biol Chem 269:29846-29854
39. Quillan JM, Sadee W 1996 Structure-based search for peptide ligands that cross-react with melanocortin receptors. Pharm Res 13:1624-1630
40. 1-selective antagonist BIBP3226. Br J Pharmacol 124:1507-1515
41. Morley JE, Levine AS, Gosnell BA, Kneip J, Grace M 1987 Effect of neuropeptide Y on ingestive behaviors in the rat. Am J Physiol 252:R599-R609
42. Sakurai T, Amemiya A, Ishii M, Matsuzaki H, Chemelli R, Tanaka H, Williams SC, Richardson JA, Kozlowski GP, Wilson S, Arch JRS, Buckingham RE, Haynes AC, Carr SA, Annan RS, McNulty DE, Liu W-S, Terrett JA, Elshourbagy NA, Bergsma DJ 1998 Orexins and orexin receptors: a family of hypothalamic neuropeptides and G protein-coupled receptors that regulate feeding behaviour. Cell 92:573-585
43. de Lecea L, Kilduff TS, Peyron C, Gao X-B, Foye PE, Danielson PE, Fukuhara C, Battenberg ELF, Gautvik VT, Bartlett II FS, Frankel WN, van den Pol AN, Bloom FE, Gautvik KM, Sutcliffe JG 1998 The hypocretins: hypothalamus-specific peptides with neuroexcitatory activity. Proc Natl Acad Sci USA 95:322-327
44. Dunn AJ, Berridge CW 1990 Physiological and behavioral responses to corticotropin-releasing factor administration: is CRF a mediator of anxiety or stress responses? Brain Res Rev 15:71-100
45. Heinrichs SC, Menzaghi F, Pich EM, Baldwin HA, Rassnick S, Britton KT, Koob GF 1994 Anti-stress action of a corticotropin-releasing factor antagonist on behavioral reactivity to stressors of varying type and intensity. Neuropsychopharmacology 11:179-186
46. Biro E, Sarnyai Z, Penke B, Szabo G, Telegdy, G 1993 Role of endogenous corticotropin-releasing factor in mediation of neuroendocrine and behavioral responses to cholecystokinin octapeptide sulfate ester in rats. Neuroendocrinology 57:340-345
47. Heilig M, Wahlestedt C, Widerlöv E 1988 Neuropeptide Y (NPY)-induced suppression of activity in the rat: evidence for NPY receptor heterogeneity and for interaction with α-adrenoceptors. Eur J Pharmacol 157:205-213
48. Kim JH, Kiefer LL, Woychik RP, Wilkinson WO, Ittoop O, Willard D, Nichols J, Zemel MB 1997 Agouti regulation of intracellular calcium: role of melanocortin receptors. Am J Physiol 272:E379-E384
49. Gross PM, Weaver DF 1993 A new experimental model of epilepsy based on the intraventricular injection of endothelin. J Cardiovasc Pharmacol 22:S282-S287