T-226296: a novel, orally active and selective melanin-concentrating hormone receptor antagonist

An, 2001, Identification and characterization of a melanin-concentrating hormone receptor, Proc. Natl. Acad. Sci. U. S. A., 98, 7576, 10.1073/pnas.131200698 Audinot, 2001, Structure-activity relationship studies of melanin-concentrating hormone (MCH)-related peptide ligands at SLC-1, the human MCH receptor, J. Biol. Chem., 276, 13554, 10.1074/jbc.M010727200 Bächner, 1999, Identification of melanin concentrating hormone (MCH) as the natural ligand for the orphan somatostatin-like receptor 1 (SLC-1), FEBS Lett., 457, 522, 10.1016/S0014-5793(99)01092-3 Beck, 2001, KO's and organization of peptidergic feeding behavior mechanisms, Neurosci. Biobehav. Rev., 25, 143, 10.1016/S0149-7634(01)00003-3 Bittencourt, 1992, The melanin-concentrating hormone system of the rat brain: an immuno- and hybridization histochemical characterization, J. Comp. Neurol., 319, 218, 10.1002/cne.903190204 Bradley, 2000, Melanin-concentrating hormone regulates leptin synthesis and secretion in rat adipocytes, Diabetes, 49, 1073, 10.2337/diabetes.49.7.1073 Chambers, 1999, Melanin-concentrating hormone is the cognate ligand for the orphan G-protein-coupled receptor SLC-1, Nature, 400, 261, 10.1038/22313 Civelli, 2001, Novel neurotransmitters as natural ligands of orphan G-protein-coupled receptors, Trends Neurosci., 24, 230, 10.1016/S0166-2236(00)01763-X Drozdz, 1995, Melanin-concentrating hormone binding to mouse melanoma cells in vitro, FEBS Lett., 359, 199, 10.1016/0014-5793(95)00043-9 Hanada, 2000, Differential regulation of melanin-concentrating hormone and orexin genes in the Agouti-related protein/melanocortin-4 receptor system, Biochem. Biophys. Res. Commun., 268, 88, 10.1006/bbrc.1999.2081 Hawes, 2000, The melanin-concentrating hormone receptor couples to multiple G proteins to activate diverse intracellular signaling pathways, Endocrinology, 141, 4524, 10.1210/en.141.12.4524 Hervieu, 1995, Pro-melanin concentrating hormone messenger ribonucleic acid and peptides expression in peripheral tissues of the rat, Neuroendocrinology, 61, 348, 10.1159/000126857 Hervieu, 2000, The distribution of the mRNA and protein products of the melanin-concentrating hormone (MCH) receptor gene, slc-1, in the central nervous system of the rat, Eur. J. Neurosci., 12, 1194, 10.1046/j.1460-9568.2000.00008.x Hill, 2001, Molecular cloning and functional characterization of MCH2, a novel human MCH receptor, J. Biol. Chem., 276, 20125, 10.1074/jbc.M102068200 Kawauchi, 1983, Characterization of melanin-concentrating hormone in chum salmon pituitaries, Nature, 305, 321, 10.1038/305321a0 Kokkotou, 2001, Melanin-concentrating hormone receptor is a target of leptin action in the mouse brain, Endocrinology, 142, 680, 10.1210/en.142.2.680 Kolakowski, 1996, Characterization of a human gene related to genes encoding somatostatin receptors, FEBS Lett., 398, 253, 10.1016/S0014-5793(96)01160-X Lakaye, 1998, Cloning of the rat brain cDNA encoding for the SLC-1 G protein-coupled receptor reveals the presence of an intron in the gene, Biochim. Biophys. Acta, 1401, 216, 10.1016/S0167-4889(97)00135-3 Lembo, 1999, The receptor for the orexigenic peptide melanin-concentrating hormone is a G-protein-coupled receptor, Nat. Cell Biol., 1, 267, 10.1038/12978 Ludwig, 2001, Melanin-concentrating hormone overexpression in transgenic mice leads to obesity and insulin resistance, J. Clin. Invest., 107, 379, 10.1172/JCI10660 Mori, 2001, Cloning of a novel G protein-coupled receptor, slt, a subtype of the melanin-concentrating hormone receptor, Biochem. Biophys. Res. Commun., 283, 1013, 10.1006/bbrc.2001.4893 Presse, 1990, Structure of the human melanin concentrating hormone mRNA, Mol. Endocrinol., 4, 632, 10.1210/mend-4-4-632 Qu, 1996, A role for melanin-concentrating hormone in the central regulation of feeding behaviour, Nature, 380, 243, 10.1038/380243a0 Rossi, 1997, Melanin-concentrating hormone acutely stimulates feeding, but chronic administration has no effect on body weight, Endocrinology, 138, 351, 10.1210/en.138.1.351 Sailer, 2001, Identification and characterization of a second melanin-concentrating hormone receptor, MCH-2R, Proc. Natl. Acad. Sci. U. S. A., 98, 7564, 10.1073/pnas.121170598 Saito, 1999, Molecular characterization of the melanin-concentrating hormone receptor, Nature, 400, 265, 10.1038/22321 Shimada, 1998, Mice lacking melanin-concentrating hormone are hypophagic and lean, Nature, 396, 670, 10.1038/25341 Shimomura, 1999, Isolation and identification of melanin-concentrating hormone as the endogenous ligand of the SLC-1 receptor, Biochem. Biophys. Res. Commun., 261, 622, 10.1006/bbrc.1999.1104 Tadayyon, 2000, Expression of melanin-concentrating hormone receptors in insulin-producing cells: MCH stimulates insulin release in RINm5F and CRI-G1 cell-lines, Biochem. Biophys. Res. Commun., 275, 709, 10.1006/bbrc.2000.3357 Vaughan, 1989, Characterization of melanin-concentrating hormone from rat hypothalamus, Endocrinology, 125, 1660, 10.1210/endo-125-3-1660