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Page 1
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. Fong TM, et al. Among authors: strack am. J Pharmacol Exp Ther. 2007 Jun;321(3):1013-22. doi: 10.1124/jpet.106.118737. Epub 2007 Feb 27. J Pharmacol Exp Ther. 2007. PMID: 17327489
1-Sulfonyl-4-acylpiperazines as selective cannabinoid-1 receptor (CB1R) inverse agonists for the treatment of obesity.
Vachal P, Fletcher JM, Fong TM, Huang CC, Lao J, Xiao JC, Shen CP, Strack AM, Shearman L, Stribling S, Chen RZ, Frassetto A, Tong X, Wang J, Ball RG, Tsou NN, Hickey GJ, Thompson DF, Faidley TD, Nicolich S, Achanfuo-Yeboah J, Hora DF, Hale JJ, Hagmann WK. Vachal P, et al. Among authors: strack am. J Med Chem. 2009 Apr 23;52(8):2550-8. doi: 10.1021/jm900063x. J Med Chem. 2009. PMID: 19320488
Regulation of energy homeostasis by bombesin receptor subtype-3: selective receptor agonists for the treatment of obesity.
Guan XM, Chen H, Dobbelaar PH, Dong Y, Fong TM, Gagen K, Gorski J, He S, Howard AD, Jian T, Jiang M, Kan Y, Kelly TM, Kosinski J, Lin LS, Liu J, Marsh DJ, Metzger JM, Miller R, Nargund RP, Palyha O, Shearman L, Shen Z, Stearns R, Strack AM, Stribling S, Tang YS, Wang SP, White A, Yu H, Reitman ML. Guan XM, et al. Among authors: strack am. Cell Metab. 2010 Feb 3;11(2):101-12. doi: 10.1016/j.cmet.2009.12.008. Epub 2010 Jan 21. Cell Metab. 2010. PMID: 20096642 Free article.
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. Lin LS, et al. J Med Chem. 2006 Dec 28;49(26):7584-7. doi: 10.1021/jm060996+. J Med Chem. 2006. PMID: 17181138
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. Armstrong HE, et al. Bioorg Med Chem Lett. 2007 Apr 15;17(8):2184-7. doi: 10.1016/j.bmcl.2007.01.087. Epub 2007 Feb 2. Bioorg Med Chem Lett. 2007. PMID: 17293109
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. Plummer CW, et al. Among authors: strack am. Bioorg Med Chem Lett. 2005 Mar 1;15(5):1441-6. doi: 10.1016/j.bmcl.2004.12.078. Bioorg Med Chem Lett. 2005. PMID: 15713403
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. Debenham JS, et al. Among authors: strack am. Bioorg Med Chem Lett. 2006 Feb;16(3):681-5. doi: 10.1016/j.bmcl.2005.10.028. Epub 2005 Nov 2. Bioorg Med Chem Lett. 2006. PMID: 16263284
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. Shearman LP, et al. Among authors: strack am. Eur J Pharmacol. 2008 Jan 28;579(1-3):215-24. doi: 10.1016/j.ejphar.2007.10.033. Epub 2007 Oct 25. Eur J Pharmacol. 2008. PMID: 18021763
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. Debenham JS, et al. Among authors: strack am. Bioorg Med Chem Lett. 2009 May 1;19(9):2591-4. doi: 10.1016/j.bmcl.2009.03.005. Epub 2009 Mar 9. Bioorg Med Chem Lett. 2009. PMID: 19328684
102 results