BML‐190 and AM251 act as inverse agonists at the human cannabinoid CB2 receptor: signalling via cAMP and inositol phosphates

@article{New2003BML190AA,
  title={BML‐190 and AM251 act as inverse agonists at the human cannabinoid CB2 receptor: signalling via cAMP and inositol phosphates},
  author={D. C. New and Y. Wong},
  journal={FEBS Letters},
  year={2003},
  volume={536}
}
  • D. C. New, Y. Wong
  • Published 2003
  • Medicine, Chemistry
  • FEBS Letters
  • The aminoalkylindole BML‐190 and diarylpyrazole AM251 ligands have previously been shown to bind to cannabinoid CB2 and CB1 receptors, respectively. In HEK‐293 cells stably expressing the human CB2 receptor, BML‐190 and AM251 potentiated the forskolin‐stimulated accumulation of cAMP. Moreover, the CB2 receptor can interact productively with 16z44, a promiscuous Gα16/z chimera. BML‐190 and AM251 reduce the basal levels of inositol phosphate production in cells expressing the CB2 receptor and… CONTINUE READING
    28 Citations
    Pharmacological actions of cannabinoids.
    • R. Pertwee
    • Medicine, Chemistry
    • Handbook of experimental pharmacology
    • 2005
    • 514
    • Highly Influenced
    • PDF
    In vitro metabolism of indomethacin morpholinylamide (BML-190), an inverse agonist for the peripheral cannabinoid receptor (CB(2)) in rat liver microsomes.
    • Qiang Zhang, P. Ma, R. Cole, G. Wang
    • Chemistry, Medicine
    • European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences
    • 2010
    Functional CB2 type cannabinoid receptors at CNS synapses
    • 113
    • PDF
    Role for Cannabinoid Receptors in Human Proximal Tubular Hypertrophy
    • 47
    Characterization of human cannabinoid CB2 receptor coupled to chimeric Galpha(qi5) and Galpha(qo5) proteins.
    • 13

    References

    SHOWING 1-10 OF 26 REFERENCES
    Agonist‐inverse agonist characterization at CB1 and CB2 cannabinoid receptors of L759633, L759656 and AM630
    • 356
    SR 144528, an antagonist for the peripheral cannabinoid receptor that behaves as an inverse agonist.
    • 98
    • PDF
    Pharmacology of cannabinoid CB1 and CB2 receptors.
    • R. Pertwee
    • Biology, Medicine
    • Pharmacology & therapeutics
    • 1997
    • 1,323
    Autocrine and paracrine regulation of lymphocyte CB2 receptor expression by TGF-beta.
    • 51
    In vitro and in vivo pharmacological characterization of JTE-907, a novel selective ligand for cannabinoid CB2 receptor.
    • 162
    • PDF
    Pharmacology of cannabinoid receptor ligands.
    • R. Pertwee
    • Biology, Chemistry
    • Current medicinal chemistry
    • 1999
    • 495
    International Union of Pharmacology. XXVII. Classification of Cannabinoid Receptors
    • 2,246
    • PDF