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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: rosko km. 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
The acyclic CB1R inverse agonist taranabant mediates weight loss by increasing energy expenditure and decreasing caloric intake.
Addy C, Wright H, Van Laere K, Gantz I, Erondu N, Musser BJ, Lu K, Yuan J, Sanabria-Bohórquez SM, Stoch A, Stevens C, Fong TM, De Lepeleire I, Cilissen C, Cote J, Rosko K, Gendrano IN 3rd, Nguyen AM, Gumbiner B, Rothenberg P, de Hoon J, Bormans G, Depré M, Eng WS, Ravussin E, Klein S, Blundell J, Herman GA, Burns HD, Hargreaves RJ, Wagner J, Gottesdiener K, Amatruda JM, Heymsfield SB. Addy C, et al. Cell Metab. 2008 Jan;7(1):68-78. doi: 10.1016/j.cmet.2007.11.012. Cell Metab. 2008. PMID: 18177726 Free article. Clinical Trial.
Multiple-dose pharmacokinetics, pharmacodynamics, and safety of taranabant, a novel selective cannabinoid-1 receptor inverse agonist, in healthy male volunteers.
Addy C, Rothenberg P, Li S, Majumdar A, Agrawal N, Li H, Zhong L, Yuan J, Maes A, Dunbar S, Cote J, Rosko K, Van Dyck K, De Lepeleire I, de Hoon J, Van Hecken A, Depré M, Knops A, Gottesdiener K, Stoch A, Wagner J. Addy C, et al. J Clin Pharmacol. 2008 Jun;48(6):734-44. doi: 10.1177/0091270008317591. J Clin Pharmacol. 2008. PMID: 18508950 Clinical Trial.
Safety, tolerability, pharmacokinetics, and pharmacodynamic properties of taranabant, a novel selective cannabinoid-1 receptor inverse agonist, for the treatment of obesity: results from a double-blind, placebo-controlled, single oral dose study in healthy volunteers.
Addy C, Li S, Agrawal N, Stone J, Majumdar A, Zhong L, Li H, Yuan J, Maes A, Rothenberg P, Cote J, Rosko K, Cummings C, Warrington S, Boyce M, Gottesdiener K, Stoch A, Wagner J. Addy C, et al. J Clin Pharmacol. 2008 Apr;48(4):418-27. doi: 10.1177/0091270008314467. Epub 2008 Feb 7. J Clin Pharmacol. 2008. PMID: 18258750 Clinical Trial.
Synthesis of 7-benzyl-5-(piperidin-1-yl)-6,7,8,9-tetrahydro-3H-pyrazolo[3,4-c][2,7]naphthyridin-1-ylamine and its analogs as bombesin receptor subtype-3 agonists.
Guo C, Guzzo PR, Hadden M, Sargent BJ, Yet L, Kan Y, Palyha O, Kelly TM, Guan X, Rosko K, Gagen K, Metzger JM, Dragovic J, Lyons K, Lin LS, Nargund RP. Guo C, et al. Bioorg Med Chem Lett. 2010 May 1;20(9):2785-9. doi: 10.1016/j.bmcl.2010.03.065. Epub 2010 Mar 17. Bioorg Med Chem Lett. 2010. PMID: 20371178
Effect of the cholesteryl ester transfer protein inhibitor, anacetrapib, on lipoproteins in patients with dyslipidaemia and on 24-h ambulatory blood pressure in healthy individuals: two double-blind, randomised placebo-controlled phase I studies.
Krishna R, Anderson MS, Bergman AJ, Jin B, Fallon M, Cote J, Rosko K, Chavez-Eng C, Lutz R, Bloomfield DM, Gutierrez M, Doherty J, Bieberdorf F, Chodakewitz J, Gottesdiener KM, Wagner JA. Krishna R, et al. Among authors: rosko k. Lancet. 2007 Dec 8;370(9603):1907-14. doi: 10.1016/S0140-6736(07)61813-3. Lancet. 2007. PMID: 18068514 Clinical Trial.
Human abuse potential and cognitive effects of taranabant, a cannabinoid 1 receptor inverse agonist: a randomized, double-blind, placebo- and active-controlled, crossover study in recreational polydrug users.
Schoedel KA, Addy C, Chakraborty B, Rosko K, Dunbar S, Maes A, Chen N, Stoch SA, Wagner J, Chodakewitz J, Sellers EM. Schoedel KA, et al. J Clin Psychopharmacol. 2012 Aug;32(4):492-502. doi: 10.1097/JCP.0b013e31825d380d. J Clin Psychopharmacol. 2012. PMID: 22722508 Clinical Trial.
11 results