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Items: 1 to 50 of 206

1.

Evaluation of a melanocortin-4 receptor (MC4R) agonist (Setmelanotide) in MC4R deficiency.

Collet TH, Dubern B, Mokrosinski J, Connors H, Keogh JM, Mendes de Oliveira E, Henning E, Poitou-Bernert C, Oppert JM, Tounian P, Marchelli F, Alili R, Le Beyec J, Pépin D, Lacorte JM, Gottesdiener A, Bounds R, Sharma S, Folster C, Henderson B, O'Rahilly S, Stoner E, Gottesdiener K, Panaro BL, Cone RD, Clément K, Farooqi IS, Van der Ploeg LHT.

Mol Metab. 2017 Oct;6(10):1321-1329. doi: 10.1016/j.molmet.2017.06.015. Epub 2017 Jul 8.

2.

Deuterium-reinforced polyunsaturated fatty acids protect against atherosclerosis by lowering lipid peroxidation and hypercholesterolemia.

Berbée JFP, Mol IM, Milne GL, Pollock E, Hoeke G, Lütjohann D, Monaco C, Rensen PCN, van der Ploeg LHT, Shchepinov MS.

Atherosclerosis. 2017 Sep;264:100-107. doi: 10.1016/j.atherosclerosis.2017.06.916. Epub 2017 Jun 21.

PMID:
28655430
3.

Magel2-null mice are hyper-responsive to setmelanotide, a melanocortin 4 receptor agonist.

Bischof JM, Van Der Ploeg LH, Colmers WF, Wevrick R.

Br J Pharmacol. 2016 Sep;173(17):2614-21. doi: 10.1111/bph.13540. Epub 2016 Jul 27.

4.

Temporal cAMP Signaling Selectivity by Natural and Synthetic MC4R Agonists.

Molden BM, Cooney KA, West K, Van Der Ploeg LH, Baldini G.

Mol Endocrinol. 2015 Nov;29(11):1619-33. doi: 10.1210/me.2015-1071. Epub 2015 Sep 29.

5.

Ghrelin.

Müller TD, Nogueiras R, Andermann ML, Andrews ZB, Anker SD, Argente J, Batterham RL, Benoit SC, Bowers CY, Broglio F, Casanueva FF, D'Alessio D, Depoortere I, Geliebter A, Ghigo E, Cole PA, Cowley M, Cummings DE, Dagher A, Diano S, Dickson SL, Diéguez C, Granata R, Grill HJ, Grove K, Habegger KM, Heppner K, Heiman ML, Holsen L, Holst B, Inui A, Jansson JO, Kirchner H, Korbonits M, Laferrère B, LeRoux CW, Lopez M, Morin S, Nakazato M, Nass R, Perez-Tilve D, Pfluger PT, Schwartz TW, Seeley RJ, Sleeman M, Sun Y, Sussel L, Tong J, Thorner MO, van der Lely AJ, van der Ploeg LH, Zigman JM, Kojima M, Kangawa K, Smith RG, Horvath T, Tschöp MH.

Mol Metab. 2015 Mar 21;4(6):437-60. doi: 10.1016/j.molmet.2015.03.005. eCollection 2015 Jun. Review.

6.

Differentiation of antiinflammatory and antitumorigenic properties of stabilized enantiomers of thalidomide analogs.

Jacques V, Czarnik AW, Judge TM, Van der Ploeg LH, DeWitt SH.

Proc Natl Acad Sci U S A. 2015 Mar 24;112(12):E1471-9. doi: 10.1073/pnas.1417832112. Epub 2015 Mar 9. Erratum in: Proc Natl Acad Sci U S A. 2015 May 12;112(19):E2553.

7.

RM-493, a melanocortin-4 receptor (MC4R) agonist, increases resting energy expenditure in obese individuals.

Chen KY, Muniyappa R, Abel BS, Mullins KP, Staker P, Brychta RJ, Zhao X, Ring M, Psota TL, Cone RD, Panaro BL, Gottesdiener KM, Van der Ploeg LH, Reitman ML, Skarulis MC.

J Clin Endocrinol Metab. 2015 Apr;100(4):1639-45. doi: 10.1210/jc.2014-4024. Epub 2015 Feb 12.

8.

Dual melanocortin-4 receptor and GLP-1 receptor agonism amplifies metabolic benefits in diet-induced obese mice.

Clemmensen C, Finan B, Fischer K, Tom RZ, Legutko B, Sehrer L, Heine D, Grassl N, Meyer CW, Henderson B, Hofmann SM, Tschöp MH, Van der Ploeg LH, Müller TD.

EMBO Mol Med. 2015 Mar;7(3):288-98. doi: 10.15252/emmm.201404508.

9.

The Pentapeptide RM-131 Promotes Food Intake and Adiposity in Wildtype Mice but Not in Mice Lacking the Ghrelin Receptor.

Fischer K, Finan B, Clemmensen C, van der Ploeg LH, Tschöp MH, Müller TD.

Front Nutr. 2015 Jan 12;1:31. doi: 10.3389/fnut.2014.00031. eCollection 2014.

10.

Optimization of privileged structures for selective and potent melanocortin subtype-4 receptor ligands.

Hong Q, Bakshi RK, Dellureficio J, He S, Ye Z, Dobbelaar PH, Sebhat IK, Guo L, Liu J, Jian T, Tang R, Kalyani RN, Macneil T, Vongs A, Rosenblum CI, Weinberg DH, Peng Q, Tamvakopoulos C, Miller RR, Stearns RA, Cashen D, Martin WJ, Chen AS, Metzger JM, Chen HY, Strack AM, Fong TM, Maclntyre E, Van der Ploeg LH, Wyvratt MJ, Nargund RP.

Bioorg Med Chem Lett. 2010 Aug 1;20(15):4483-6. doi: 10.1016/j.bmcl.2010.06.038. Epub 2010 Jun 10.

PMID:
20598533
11.

Inhibition of NOTCH signaling by gamma secretase inhibitor engages the RB pathway and elicits cell cycle exit in T-cell acute lymphoblastic leukemia cells.

Rao SS, O'Neil J, Liberator CD, Hardwick JS, Dai X, Zhang T, Tyminski E, Yuan J, Kohl NE, Richon VM, Van der Ploeg LH, Carroll PM, Draetta GF, Look AT, Strack PR, Winter CG.

Cancer Res. 2009 Apr 1;69(7):3060-8. doi: 10.1158/0008-5472.CAN-08-4295. Epub 2009 Mar 24.

12.

Synthesis and SAR of potent and orally bioavailable tert-butylpyrrolidine archetype derived melanocortin subtype-4 receptor modulators.

Guo L, Ye Z, Ujjainwalla F, Sings HL, Sebhat IK, Huber J, Weinberg DH, Tang R, MacNeil T, Tamvakopoulos C, Peng Q, MacIntyre E, van der Ploeg LH, Goulet MT, Wyvratt MJ, Nargund RP.

Bioorg Med Chem Lett. 2008 Jun 1;18(11):3242-7. doi: 10.1016/j.bmcl.2008.04.049. Epub 2008 Apr 25.

PMID:
18479920
13.

Effects of a novel Y5 antagonist in obese mice: combination with food restriction or sibutramine.

Mashiko S, Ishihara A, Iwaasa H, Moriya R, Kitazawa H, Mitobe Y, Ito J, Gomori A, Matsushita H, Takahashi T, MacNeil DJ, Van der Ploeg LH, Fukami T, Kanatani A.

Obesity (Silver Spring). 2008 Jul;16(7):1510-5. doi: 10.1038/oby.2008.223. Epub 2008 Apr 10.

14.

Characterization of a novel and selective cannabinoid CB1 receptor inverse agonist, Imidazole 24b, in rodents.

Shearman LP, Stribling DS, Camacho RE, Rosko KM, Wang J, Tong S, Feng Y, Marsh DJ, Yu H, Guan X, Spann SK, Macneil DJ, Fong TM, Metzger JM, Goulet MT, Hagmann WK, Plummer CW, Finke PE, Mills SG, Shah SK, Truong Q, Van der Ploeg LH, Macintyre DE, Strack AM.

Eur J Pharmacol. 2008 Jan 28;579(1-3):215-24. Epub 2007 Oct 25.

PMID:
18021763
15.

Melanocortin subtype 4 receptor agonists: structure-activity relationships about the 4-alkyl piperidine core.

Sebhat IK, Lai Y, Barakat K, Ye Z, Tang R, Kalyani RN, Vongs A, Macneil T, Weinberg DH, Cabello MA, Maroto M, Teran A, Fong TM, Van der Ploeg LH, Patchett AA, Nargund RP.

Bioorg Med Chem Lett. 2007 Oct 15;17(20):5720-3. Epub 2006 Dec 3.

PMID:
17768046
16.

Antiobesity efficacy of a novel cannabinoid-1 receptor inverse agonist, N-[(1S,2S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl]-2-methyl-2-[[5-(trifluoromethyl)pyridin-2-yl]oxy]propanamide (MK-0364), in rodents.

Fong TM, Guan XM, Marsh DJ, Shen CP, Stribling DS, Rosko KM, Lao J, Yu H, Feng Y, Xiao JC, Van der Ploeg LH, Goulet MT, Hagmann WK, Lin LS, Lanza TJ Jr, Jewell JP, Liu P, Shah SK, Qi H, Tong X, Wang J, Xu SS, Francis B, Strack AM, MacIntyre DE, Shearman LP.

J Pharmacol Exp Ther. 2007 Jun;321(3):1013-22. Epub 2007 Feb 27.

17.

Lead optimization of 5,6-diarylpyridines as CB1 receptor inverse agonists.

Madsen-Duggan CB, Debenham JS, Walsh TF, Toupence RB, Huang SX, Wang J, Tong X, Lao J, Fong TM, Schaeffer MT, Xiao JC, Huang CR, Shen CP, Stribling DS, Shearman LP, Strack AM, MacIntyre DE, Van der Ploeg LH, Goulet MT.

Bioorg Med Chem Lett. 2007 Apr 1;17(7):2031-5. Epub 2007 Jan 13.

PMID:
17270441
18.

Discovery of N-[(1S,2S)-3-(4-Chlorophenyl)-2- (3-cyanophenyl)-1-methylpropyl]-2-methyl-2- {[5-(trifluoromethyl)pyridin-2-yl]oxy}propanamide (MK-0364), a novel, acyclic cannabinoid-1 receptor inverse agonist for the treatment of obesity.

Lin LS, Lanza TJ Jr, Jewell JP, Liu P, Shah SK, Qi H, Tong X, Wang J, Xu SS, Fong TM, Shen CP, Lao J, Xiao JC, Shearman LP, Stribling DS, Rosko K, Strack A, Marsh DJ, Feng Y, Kumar S, Samuel K, Yin W, Van der Ploeg LH, Goulet MT, Hagmann WK.

J Med Chem. 2006 Dec 28;49(26):7584-7.

PMID:
17181138
19.

A pair-feeding study reveals that a Y5 antagonist causes weight loss in diet-induced obese mice by modulating food intake and energy expenditure.

Mashiko S, Ishihara A, Iwaasa H, Sano H, Ito J, Gomori A, Oda Z, Moriya R, Matsushita H, Jitsuoka M, Okamoto O, MacNeil DJ, Van der Ploeg LH, Fukami T, Kanatani A.

Mol Pharmacol. 2007 Feb;71(2):602-8. Epub 2006 Nov 14. Erratum in: Mol Pharmacol. 2007 May;71(5):1444.

20.

2-Aminoquinoline melanin-concentrating hormone (MCH)1R antagonists.

Jiang J, Hoang M, Young JR, Chaung D, Eid R, Turner C, Lin P, Tong X, Wang J, Tan C, Feighner S, Palyha O, Hreniuk DL, Pan J, Sailer AW, MacNeil DJ, Howard A, Shearman L, Stribling S, Camacho R, Strack A, Van der Ploeg LH, Goulet MT, DeVita RJ.

Bioorg Med Chem Lett. 2006 Oct 15;16(20):5270-4. Epub 2006 Aug 17.

PMID:
16919456
21.

4-Aminoquinoline melanin-concentrating hormone 1-receptor (MCH1R) antagonists.

Jiang J, Lin P, Hoang M, Chang L, Tan C, Feighner S, Palyha OC, Hreniuk DL, Pan J, Sailer AW, Morin NR, MacNeil DJ, Howard AD, Van der Ploeg LH, Goulet MT, DeVita RJ.

Bioorg Med Chem Lett. 2006 Oct 15;16(20):5275-9. Epub 2006 Aug 17.

PMID:
16919453
22.

Design and synthesis of (ant)-agonists that alter appetite and adiposity.

Van der Ploeg LH, Kanatani A, MacNeil D, Ming Fong T, Strack A, Nargund R, Guan XM.

Prog Brain Res. 2006;153:107-18. Review.

PMID:
16876570
23.

A neuropeptide Y Y5 antagonist selectively ameliorates body weight gain and associated parameters in diet-induced obese mice.

Ishihara A, Kanatani A, Mashiko S, Tanaka T, Hidaka M, Gomori A, Iwaasa H, Murai N, Egashira S, Murai T, Mitobe Y, Matsushita H, Okamoto O, Sato N, Jitsuoka M, Fukuroda T, Ohe T, Guan X, MacNeil DJ, Van der Ploeg LH, Nishikibe M, Ishii Y, Ihara M, Fukami T.

Proc Natl Acad Sci U S A. 2006 May 2;103(18):7154-8. Epub 2006 Apr 24.

24.

Optimization of a privileged structure leading to potent and selective human melanocortin subtype-4 receptor ligands.

Bakshi RK, Hong Q, Tang R, Kalyani RN, Macneil T, Weinberg DH, Van der Ploeg LH, Patchett AA, Nargund RP.

Bioorg Med Chem Lett. 2006 Mar 1;16(5):1130-3. Epub 2005 Dec 20.

PMID:
16364639
25.

Synthesis of functionalized 1,8-naphthyridinones and their evaluation as novel, orally active CB1 receptor inverse agonists.

Debenham JS, Madsen-Duggan CB, Walsh TF, Wang J, Tong X, Doss GA, Lao J, Fong TM, Schaeffer MT, Xiao JC, Huang CR, Shen CP, Feng Y, Marsh DJ, Stribling DS, Shearman LP, Strack AM, MacIntyre DE, Van der Ploeg LH, Goulet MT.

Bioorg Med Chem Lett. 2006 Feb;16(3):681-5. Epub 2005 Nov 2.

PMID:
16263284
26.

Structure-activity relationship of linear tetrapeptides Tic-DPhe-Arg-Trp-NH2 at the human melanocortin-4 receptor and effects on feeding behaviors in rat.

Ye Z, MacNeil T, Weinberg DH, Kalyani RN, Tang R, Strack AM, Murphy BA, Mosley RT, Euan MacIntyre D, Van der Ploeg LH, Patchett AA, Wyvratt MJ, Nargund RP.

Peptides. 2005 Oct;26(10):2017-25.

PMID:
15993513
27.

Discovery and activity of (1R,4S,6R)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-2-methyl-2-azabicyclo[2.2.2]octane-6-carboxamide (3, RY764), a potent and selective melanocortin subtype-4 receptor agonist.

Ye Z, Guo L, Barakat KJ, Pollard PG, Palucki BL, Sebhat IK, Bakshi RK, Tang R, Kalyani RN, Vongs A, Chen AS, Chen HY, Rosenblum CI, MacNeil T, Weinberg DH, Peng Q, Tamvakopoulos C, Miller RR, Stearns RA, Cashen DE, Martin WJ, Metzger JM, Strack AM, MacIntyre DE, Van der Ploeg LH, Patchett AA, Wyvratt MJ, Nargund RP.

Bioorg Med Chem Lett. 2005 Aug 1;15(15):3501-5.

PMID:
15982875
28.

1-Amino-1,2,3,4-tetrahydronaphthalene-2-carboxylic acid as a Tic mimetic: application in the synthesis of potent human melanocortin-4 receptor selective agonists.

Bakshi RK, Hong Q, Olson JT, Ye Z, Sebhat IK, Weinberg DH, MacNeil T, Kalyani RN, Tang R, Martin WJ, Strack A, McGowan E, Tamvakopoulos C, Miller RR, Stearns RA, Tang W, Maclntyre DE, van der Ploeg LH, Patchett AA, Nargund RP.

Bioorg Med Chem Lett. 2005 Jul 15;15(14):3430-3.

PMID:
15951175
29.

2-Piperazinecarboxamides as potent and selective melanocortin subtype-4 receptor agonists.

Palucki BL, Park MK, Nargund RP, Tang R, MacNeil T, Weinberg DH, Vongs A, Rosenblum CI, Doss GA, Miller RR, Stearns RA, Peng Q, Tamvakopoulos C, Van der Ploeg LH, Patchett AA.

Bioorg Med Chem Lett. 2005 Apr 15;15(8):1993-6.

PMID:
15808454
30.

Synthesis and activity of 4,5-diarylimidazoles as human CB1 receptor inverse agonists.

Plummer CW, Finke PE, Mills SG, Wang J, Tong X, Doss GA, Fong TM, Lao JZ, Schaeffer MT, Chen J, Shen CP, Stribling DS, Shearman LP, Strack AM, Van der Ploeg LH.

Bioorg Med Chem Lett. 2005 Mar 1;15(5):1441-6.

PMID:
15713403
31.

Increased melanin concentrating hormone receptor type I in the human hypothalamic infundibular nucleus in cachexia.

Unmehopa UA, van Heerikhuize JJ, Spijkstra W, Woods JW, Howard AD, Zycband E, Feighner SD, Hreniuk DL, Palyha OC, Guan XM, Macneil DJ, Van der Ploeg LH, Swaab DF.

J Clin Endocrinol Metab. 2005 Apr;90(4):2412-9. Epub 2005 Jan 25.

PMID:
15671106
32.

Synthesis and SAR of 5,6-diarylpyridines as human CB1 inverse agonists.

Meurer LC, Finke PE, Mills SG, Walsh TF, Toupence RB, Debenham JS, Goulet MT, Wang J, Tong X, Fong TM, Lao J, Schaeffer MT, Chen J, Shen CP, Sloan Stribling D, Shearman LP, Strack AM, Van der Ploeg LH.

Bioorg Med Chem Lett. 2005 Feb 1;15(3):645-51. Erratum in: Bioorg Med Chem Lett. 2005 Mar 15;15(6):1755. Debenham, John S [added].

PMID:
15664830
33.

Discovery of (2S)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-4-methyl-2-piperazinecarboxamide (MB243), a potent and selective melanocortin subtype-4 receptor agonist.

Palucki BL, Park MK, Nargund RP, Ye Z, Sebhat IK, Pollard PG, Kalyani RN, Tang R, Macneil T, Weinberg DH, Vongs A, Rosenblum CI, Doss GA, Miller RR, Stearns RA, Peng Q, Tamvakopoulos C, McGowan E, Martin WJ, Metzger JM, Shepherd CA, Strack AM, Macintyre DE, Van der Ploeg LH, Patchett AA.

Bioorg Med Chem Lett. 2005 Jan 3;15(1):171-5.

PMID:
15582434
34.

Novel aspects of accumulation dynamics and A beta composition in transgenic models of AD.

Lewis HD, Beher D, Smith D, Hewson L, Cookson N, Reynolds DS, Dawson GR, Jiang M, Van der Ploeg LH, Qian S, Rosahl TW, Kalaria RN, Shearman MS.

Neurobiol Aging. 2004 Oct;25(9):1175-85.

PMID:
15312963
35.

Crystal structure of human phosphodiesterase 3B: atomic basis for substrate and inhibitor specificity.

Scapin G, Patel SB, Chung C, Varnerin JP, Edmondson SD, Mastracchio A, Parmee ER, Singh SB, Becker JW, Van der Ploeg LH, Tota MR.

Biochemistry. 2004 May 25;43(20):6091-100.

PMID:
15147193
36.

Expression, refolding, and purification of recombinant human phosphodiesterase 3B: definition of the N-terminus of the catalytic core.

Varnerin JP, Chung CC, Patel SB, Scapin G, Parmee ER, Morin NR, MacNeil DJ, Cully DF, Van der Ploeg LH, Tota MR.

Protein Expr Purif. 2004 Jun;35(2):225-36.

PMID:
15135397
37.

Distribution of neuromedin U receptor subtype 2 mRNA in the rat brain.

Guan XM, Yu H, Jiang Q, Van Der Ploeg LH, Liu Q.

Brain Res Gene Expr Patterns. 2001 Aug;1(1):1-4.

PMID:
15018811
38.

Orexigenic action of peripheral ghrelin is mediated by neuropeptide Y and agouti-related protein.

Chen HY, Trumbauer ME, Chen AS, Weingarth DT, Adams JR, Frazier EG, Shen Z, Marsh DJ, Feighner SD, Guan XM, Ye Z, Nargund RP, Smith RG, Van der Ploeg LH, Howard AD, MacNeil DJ, Qian S.

Endocrinology. 2004 Jun;145(6):2607-12. Epub 2004 Feb 12.

PMID:
14962995
39.

Design and syntheses of melanocortin subtype-4 receptor agonists: evolution of the pyridazinone archetype.

Ujjainwalla F, Warner D, Walsh TF, Wyvratt MJ, Zhou C, Yang L, Kalyani RN, MacNeil T, Van der Ploeg LH, Rosenblum CI, Tang R, Vongs A, Weinberg DH, Goulet MT.

Bioorg Med Chem Lett. 2003 Dec 15;13(24):4431-5.

PMID:
14643340
40.

Benzyl vinylogous amide substituted aryldihydropyridazinones and aryldimethylpyrazolones as potent and selective PDE3B inhibitors.

Edmondson SD, Mastracchio A, He J, Chung CC, Forrest MJ, Hofsess S, MacIntyre E, Metzger J, O'Connor N, Patel K, Tong X, Tota MR, Van der Ploeg LH, Varnerin JP, Fisher MH, Wyvratt MJ, Weber AE, Parmee ER.

Bioorg Med Chem Lett. 2003 Nov 17;13(22):3983-7.

PMID:
14592490
41.

Extensive structure-activity studies of lactam derivatives of MT-II and SHU-9119: their activity and selectivity at human melanocortin receptors 3, 4, and 5.

Grieco P, Balse-Srinivasan P, Han G, Weinberg D, MacNeil T, Van der Ploeg LH, Hruby VJ.

J Pept Res. 2003 Nov;62(5):199-206.

PMID:
14531843
42.

Chronic MCH-1 receptor modulation alters appetite, body weight and adiposity in rats.

Shearman LP, Camacho RE, Sloan Stribling D, Zhou D, Bednarek MA, Hreniuk DL, Feighner SD, Tan CP, Howard AD, Van der Ploeg LH, MacIntyre DE, Hickey GJ, Strack AM.

Eur J Pharmacol. 2003 Aug 15;475(1-3):37-47.

PMID:
12954357
43.

The role of tryptophan 1072 in human PDE3B inhibitor binding.

Chung C, Varnerin JP, Morin NR, MacNeil DJ, Singh SB, Patel S, Scapin G, Van der Ploeg LH, Tota MR.

Biochem Biophys Res Commun. 2003 Aug 8;307(4):1045-50.

PMID:
12878217
44.

Exploring the site of anorectic action of peripherally administered synthetic melanocortin peptide MT-II in rats.

Trivedi P, Jiang M, Tamvakopoulos CC, Shen X, Yu H, Mock S, Fenyk-Melody J, Van der Ploeg LH, Guan XM.

Brain Res. 2003 Jul 11;977(2):221-30.

PMID:
12834882
45.

Characterization of neuropeptide Y (NPY) Y5 receptor-mediated obesity in mice: chronic intracerebroventricular infusion of D-Trp(34)NPY.

Mashiko S, Ishihara A, Iwaasa H, Sano H, Oda Z, Ito J, Yumoto M, Okawa M, Suzuki J, Fukuroda T, Jitsuoka M, Morin NR, MacNeil DJ, Van der Ploeg LH, Ihara M, Fukami T, Kanatani A.

Endocrinology. 2003 May;144(5):1793-801.

PMID:
12697685
46.

Structure-activity studies of the melanocortin peptides: discovery of potent and selective affinity antagonists for the hMC3 and hMC4 receptors.

Grieco P, Lavecchia A, Cai M, Trivedi D, Weinberg D, MacNeil T, Van der Ploeg LH, Hruby VJ.

J Med Chem. 2002 Nov 21;45(24):5287-94.

PMID:
12431055
47.

Activation of melanocortin MC(4) receptors increases erectile activity in rats ex copula.

Martin WJ, McGowan E, Cashen DE, Gantert LT, Drisko JE, Hom GJ, Nargund R, Sebhat I, Howard AD, Van der Ploeg LH, MacIntyre DE.

Eur J Pharmacol. 2002 Nov 1;454(1):71-9.

PMID:
12409007
48.

Design and pharmacology of N-[(3R)-1,2,3,4-tetrahydroisoquinolinium- 3-ylcarbonyl]-(1R)-1-(4-chlorobenzyl)- 2-[4-cyclohexyl-4-(1H-1,2,4-triazol- 1-ylmethyl)piperidin-1-yl]-2-oxoethylamine (1), a potent, selective, melanocortin subtype-4 receptor agonist.

Sebhat IK, Martin WJ, Ye Z, Barakat K, Mosley RT, Johnston DB, Bakshi R, Palucki B, Weinberg DH, MacNeil T, Kalyani RN, Tang R, Stearns RA, Miller RR, Tamvakopoulos C, Strack AM, McGowan E, Cashen DE, Drisko JE, Hom GJ, Howard AD, MacIntyre DE, van der Ploeg LH, Patchett AA, Nargund RP.

J Med Chem. 2002 Oct 10;45(21):4589-93.

PMID:
12361385
49.

The role of melanocortins in body weight regulation: opportunities for the treatment of obesity.

MacNeil DJ, Howard AD, Guan X, Fong TM, Nargund RP, Bednarek MA, Goulet MT, Weinberg DH, Strack AM, Marsh DJ, Chen HY, Shen CP, Chen AS, Rosenblum CI, MacNeil T, Tota M, MacIntyre ED, Van der Ploeg LH.

Eur J Pharmacol. 2002 Aug 16;450(1):93-109. Review.

PMID:
12176114
50.

A role for the melanocortin 4 receptor in sexual function.

Van der Ploeg LH, Martin WJ, Howard AD, Nargund RP, Austin CP, Guan X, Drisko J, Cashen D, Sebhat I, Patchett AA, Figueroa DJ, DiLella AG, Connolly BM, Weinberg DH, Tan CP, Palyha OC, Pong SS, MacNeil T, Rosenblum C, Vongs A, Tang R, Yu H, Sailer AW, Fong TM, Huang C, Tota MR, Chang RS, Stearns R, Tamvakopoulos C, Christ G, Drazen DL, Spar BD, Nelson RJ, MacIntyre DE.

Proc Natl Acad Sci U S A. 2002 Aug 20;99(17):11381-6. Epub 2002 Aug 9.

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