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

  title={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},
  author={T. Fong and Xiao-ming Guan and D. Marsh and Chun-Pyn Shen and D. Stribling and Kim Rosko and Julie Lao and H. Yu and Y. Feng and J. Xiao and Lex H T van der Ploeg and M. Goulet and Williams K. Hagmann and Linus S. Lin and T. Lanza and James P. Jewell and P. Liu and S. Shah and Hongbo Qi and X. Tong and J. Wang and S. Xu and B. Francis and A. Strack and D. Macintyre and L. Shearman},
  journal={Journal of Pharmacology and Experimental Therapeutics},
  pages={1013 - 1022}
  • T. Fong, Xiao-ming Guan, +23 authors L. Shearman
  • Published 2007
  • Chemistry, Medicine
  • Journal of Pharmacology and Experimental Therapeutics
  • The cannabinoid-1 receptor (CB1R) has been implicated in the control of energy balance. To explore the pharmacological utility of CB1R inhibition for the treatment of obesity, we evaluated the efficacy of N-[(1S,2S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl]-2-methyl-2-{[5-(trifluoromethyl)pyridin-2-yl]oxy}propanamide (MK-0364) and determined the relationship between efficacy and brain CB1R occupancy in rodents. MK-0364 was shown to be a highly potent CB1R inverse agonist that… CONTINUE READING
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