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Items: 43

1.

Antiobesity effect of MK-5046, a novel bombesin receptor subtype-3 agonist.

Guan XM, Metzger JM, Yang L, Raustad KA, Wang SP, Spann SK, Kosinski JA, Yu H, Shearman LP, Faidley TD, Palyha O, Kan Y, Kelly TM, Sebhat I, Lin LS, Dragovic J, Lyons KA, Craw S, Nargund RP, Marsh DJ, Strack AM, Reitman ML.

J Pharmacol Exp Ther. 2011 Feb;336(2):356-64. doi: 10.1124/jpet.110.174763. Epub 2010 Oct 29.

PMID:
21036912
2.

Dihydro-pyrano[2,3-b]pyridines and tetrahydro-1,8-naphthyridines as CB1 receptor inverse agonists: synthesis, SAR and biological evaluation.

Madsen-Duggan CB, Debenham JS, Walsh TF, Yan L, Huo P, Wang J, Tong X, Lao J, Fong TM, Xiao JC, Huang CR, Shen CP, Stribling DS, Shearman LP, Strack AM, Goulet MT, Hale JJ.

Bioorg Med Chem Lett. 2010 Jun 15;20(12):3750-4. doi: 10.1016/j.bmcl.2010.04.071. Epub 2010 Apr 21.

PMID:
20483606
3.

Discovery of N-[(4R)-6-(4-chlorophenyl)-7-(2,4-dichlorophenyl)-2,2-dimethyl-3,4-dihydro-2H-pyrano[2,3-b]pyridin-4-yl]-5-methyl-1H-pyrazole-3-carboxamide (MK-5596) as a novel cannabinoid-1 receptor (CB1R) inverse agonist for the treatment of obesity.

Yan L, Huo P, Debenham JS, Madsen-Duggan CB, Lao J, Chen RZ, Xiao JC, Shen CP, Stribling DS, Shearman LP, Strack AM, Tsou N, Ball RG, Wang J, Tong X, Bateman TJ, Reddy VB, Fong TM, Hale JJ.

J Med Chem. 2010 May 27;53(10):4028-37. doi: 10.1021/jm100023j.

PMID:
20423086
4.

Discovery of substituted biphenyl imidazoles as potent, bioavailable bombesin receptor subtype-3 agonists.

He S, Dobbelaar PH, Liu J, Jian T, Sebhat IK, Lin LS, Goodman A, Guo C, Guzzo PR, Hadden M, Henderson AJ, Ruenz M, Sargent BJ, Yet L, Kelly TM, Palyha O, Kan Y, Pan J, Chen H, Marsh DJ, Shearman LP, Strack AM, Metzger JM, Feighner SD, Tan C, Howard AD, Tamvakopoulos C, Peng Q, Guan XM, Reitman ML, Patchett AA, Wyvratt MJ Jr, Nargund RP.

Bioorg Med Chem Lett. 2010 Mar 15;20(6):1913-7. doi: 10.1016/j.bmcl.2010.01.154. Epub 2010 Feb 4.

PMID:
20167483
5.

Furo[2,3-b]pyridine-based cannabinoid-1 receptor inverse agonists: synthesis and biological evaluation. Part 1.

Debenham JS, Madsen-Duggan CB, Toupence RB, Walsh TF, Wang J, Tong X, Kumar S, Lao J, Fong TM, Xiao JC, Huang CR, Shen CP, Feng Y, Marsh DJ, Stribling DS, Shearman LP, Strack AM, Goulet MT.

Bioorg Med Chem Lett. 2010 Feb 15;20(4):1448-52. doi: 10.1016/j.bmcl.2009.12.065. Epub 2010 Jan 4.

PMID:
20096577
6.

Pyridopyrimidine based cannabinoid-1 receptor inverse agonists: Synthesis and biological evaluation.

Debenham JS, Madsen-Duggan CB, Wang J, Tong X, Lao J, Fong TM, Schaeffer MT, Xiao JC, Huang CC, Shen CP, Sloan Stribling D, Shearman LP, Strack AM, Euan Macintyre D, Hale JJ, Walsh TF.

Bioorg Med Chem Lett. 2009 May 1;19(9):2591-4. doi: 10.1016/j.bmcl.2009.03.005. Epub 2009 Mar 9.

PMID:
19328684
7.

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
8.

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.

PMID:
17327489
9.

Substituted acyclic sulfonamides as human cannabinoid-1 receptor inverse agonists.

Armstrong HE, Galka A, Lin LS, Lanza TJ Jr, Jewell JP, Shah SK, Guthikonda R, Truong Q, Chang LL, Quaker G, Colandrea VJ, Tong X, Wang J, Xu S, Fong TM, Shen CP, Lao J, Chen J, Shearman LP, Stribling DS, Rosko K, Strack A, Ha S, Van der Ploeg L, Goulet MT, Hagmann WK.

Bioorg Med Chem Lett. 2007 Apr 15;17(8):2184-7. Epub 2007 Feb 2.

PMID:
17293109
10.

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
11.

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
12.

Ghrelin neutralization by a ribonucleic acid-SPM ameliorates obesity in diet-induced obese mice.

Shearman LP, Wang SP, Helmling S, Stribling DS, Mazur P, Ge L, Wang L, Klussmann S, Macintyre DE, Howard AD, Strack AM.

Endocrinology. 2006 Mar;147(3):1517-26. Epub 2005 Dec 8.

PMID:
16339202
13.

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
14.

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
15.

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
16.

Enhanced running wheel activity of both Mch1r- and Pmch-deficient mice.

Zhou D, Shen Z, Strack AM, Marsh DJ, Shearman LP.

Regul Pept. 2005 Jan 15;124(1-3):53-63.

PMID:
15544841
17.
18.

Antidepressant-like and anorectic effects of the cannabinoid CB1 receptor inverse agonist AM251 in mice.

Shearman LP, Rosko KM, Fleischer R, Wang J, Xu S, Tong XS, Rocha BA.

Behav Pharmacol. 2003 Dec;14(8):573-82.

PMID:
14665974
19.

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
20.

Plasma agouti-related protein level: a possible correlation with fasted and fed states in humans and rats.

Shen CP, Wu KK, Shearman LP, Camacho R, Tota MR, Fong TM, Van der Ploeg LH.

J Neuroendocrinol. 2002 Aug;14(8):607-10.

PMID:
12153462
21.

Neither agouti-related protein nor neuropeptide Y is critically required for the regulation of energy homeostasis in mice.

Qian S, Chen H, Weingarth D, Trumbauer ME, Novi DE, Guan X, Yu H, Shen Z, Feng Y, Frazier E, Chen A, Camacho RE, Shearman LP, Gopal-Truter S, MacNeil DJ, Van der Ploeg LH, Marsh DJ.

Mol Cell Biol. 2002 Jul;22(14):5027-35.

22.

Melanin-concentrating hormone 1 receptor-deficient mice are lean, hyperactive, and hyperphagic and have altered metabolism.

Marsh DJ, Weingarth DT, Novi DE, Chen HY, Trumbauer ME, Chen AS, Guan XM, Jiang MM, Feng Y, Camacho RE, Shen Z, Frazier EG, Yu H, Metzger JM, Kuca SJ, Shearman LP, Gopal-Truter S, MacNeil DJ, Strack AM, MacIntyre DE, Van der Ploeg LH, Qian S.

Proc Natl Acad Sci U S A. 2002 Mar 5;99(5):3240-5. Epub 2002 Feb 26.

23.
24.

Targeted disruption of the mPer3 gene: subtle effects on circadian clock function.

Shearman LP, Jin X, Lee C, Reppert SM, Weaver DR.

Mol Cell Biol. 2000 Sep;20(17):6269-75.

25.

Interacting molecular loops in the mammalian circadian clock.

Shearman LP, Sriram S, Weaver DR, Maywood ES, Chaves I, Zheng B, Kume K, Lee CC, van der Horst GT, Hastings MH, Reppert SM.

Science. 2000 May 12;288(5468):1013-9.

26.

CLOCK, an essential pacemaker component, controls expression of the circadian transcription factor DBP.

Ripperger JA, Shearman LP, Reppert SM, Schibler U.

Genes Dev. 2000 Mar 15;14(6):679-89.

27.

Cocaine up-regulates norepinephrine transporter binding in the rat placenta.

Shearman LP, Meyer JS.

Eur J Pharmacol. 1999 Dec 10;386(1):1-6.

PMID:
10611457
28.

mCRY1 and mCRY2 are essential components of the negative limb of the circadian clock feedback loop.

Kume K, Zylka MJ, Sriram S, Shearman LP, Weaver DR, Jin X, Maywood ES, Hastings MH, Reppert SM.

Cell. 1999 Jul 23;98(2):193-205.

29.

Photic induction of Period gene expression is reduced in Clock mutant mice.

Shearman LP, Weaver DR.

Neuroreport. 1999 Feb 25;10(3):613-8.

PMID:
10208599
30.

Expression of basic helix-loop-helix/PAS genes in the mouse suprachiasmatic nucleus.

Shearman LP, Zylka MJ, Reppert SM, Weaver DR.

Neuroscience. 1999 Mar;89(2):387-97.

PMID:
10077321
31.

A molecular mechanism regulating rhythmic output from the suprachiasmatic circadian clock.

Jin X, Shearman LP, Weaver DR, Zylka MJ, de Vries GJ, Reppert SM.

Cell. 1999 Jan 8;96(1):57-68.

32.

Molecular analysis of mammalian timeless.

Zylka MJ, Shearman LP, Levine JD, Jin X, Weaver DR, Reppert SM.

Neuron. 1998 Nov;21(5):1115-22.

33.

Relationship between [125I]RTI-55-labeled cocaine binding sites and the serotonin transporter in rat placenta.

Shearman LP, McReynolds AM, Zhou FC, Meyer JS.

Am J Physiol. 1998 Dec;275(6):C1621-9. doi: 10.1152/ajpcell.1998.275.6.C1621.

PMID:
9843724
35.

Norepinephrine transporters in rat placenta labeled with [3H]nisoxetine.

Shearman LP, Meyer JS.

J Pharmacol Exp Ther. 1998 Feb;284(2):736-43.

PMID:
9454822
36.

Two period homologs: circadian expression and photic regulation in the suprachiasmatic nuclei.

Shearman LP, Zylka MJ, Weaver DR, Kolakowski LF Jr, Reppert SM.

Neuron. 1997 Dec;19(6):1261-9.

37.

Widespread expression of functional D1-dopamine receptors in fetal rat brain.

Shearman LP, Zeitzer J, Weaver DR.

Brain Res Dev Brain Res. 1997 Aug 18;102(1):105-15.

PMID:
9298239
38.

Molecular dissection of two distinct actions of melatonin on the suprachiasmatic circadian clock.

Liu C, Weaver DR, Jin X, Shearman LP, Pieschl RL, Gribkoff VK, Reppert SM.

Neuron. 1997 Jul;19(1):91-102.

39.

Haloperidol regulates neurotensin gene expression in striatum of c-fos-deficient mice.

Shearman LP, Weaver DR.

Brain Res Mol Brain Res. 1997 Jul;47(1-2):275-85.

PMID:
9221926
40.
41.

Monoamine transporters and the neurobehavioral teratology of cocaine.

Meyer JS, Shearman LP, Collins LM.

Pharmacol Biochem Behav. 1996 Dec;55(4):585-93. Review.

PMID:
8981589
42.

Characterization and localization of [125I]RTI-55-labeled cocaine binding sites in fetal and adult rat brain.

Shearman LP, Collins LM, Meyer JS.

J Pharmacol Exp Ther. 1996 Jun;277(3):1770-83.

PMID:
8667249
43.

Cocaine binding sites in fetal rat brain: implications for prenatal cocaine action.

Meyer JS, Shearman LP, Collins LM, Maguire RL.

Psychopharmacology (Berl). 1993;112(4):445-51.

PMID:
7871055

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