Synthesis and Characterization of NESS 0327: A Novel Putative Antagonist of the CB1 Cannabinoid Receptor

@article{Ruiu2003SynthesisAC,
  title={Synthesis and Characterization of NESS 0327: A Novel Putative Antagonist of the CB1 Cannabinoid Receptor},
  author={Stefania Ruiu and G. Pinna and G. Marchese and Jean-Mario Mussinu and P. Saba and S. Tambaro and P. Casti and R. Vargiu and L. Pani},
  journal={Journal of Pharmacology and Experimental Therapeutics},
  year={2003},
  volume={306},
  pages={363 - 370}
}
  • Stefania Ruiu, G. Pinna, +6 authors L. Pani
  • Published 2003
  • Medicine, Chemistry
  • Journal of Pharmacology and Experimental Therapeutics
  • The compound N-piperidinyl-[8-chloro-1-(2,4-dichlorophenyl)-1,4,5,6-tetrahydrobenzo [6,7]cyclohepta[1,2-c]pyrazole-3-carboxamide] (NESS 0327) was synthesized and evaluated for binding affinity toward cannabinoid CB1 and CB2 receptor. NESS 0327 exhibited a stronger selectivity for CB1 receptor compared with N-piperidinyl-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide (SR 141716A), showing a much higher affinity for CB1 receptor (Ki = 350 ± 5 fM and 1.8 ± 0.075 nM… CONTINUE READING
    Pharmacological actions of cannabinoids.
    • 502
    • PDF
    Signal transduction of the CB1 cannabinoid receptor.
    • 225
    • PDF

    References

    Publications referenced by this paper.
    SHOWING 1-10 OF 36 REFERENCES
    Molecular characterization of a peripheral receptor for cannabinoids
    • 4,127
    Cannabinoid receptor localization in brain.
    • 1,932
    Isolation and structure of a brain constituent that binds to the cannabinoid receptor.
    • 4,676