Cannabidiol is an allosteric modulator at mu- and delta-opioid receptors

@article{Kathmann2006CannabidiolIA,
  title={Cannabidiol is an allosteric modulator at mu- and delta-opioid receptors},
  author={M. Kathmann and K. Flau and A. Redmer and C. Tr{\"a}nkle and E. Schlicker},
  journal={Naunyn-Schmiedeberg's Archives of Pharmacology},
  year={2006},
  volume={372},
  pages={354-361}
}
  • M. Kathmann, K. Flau, +2 authors E. Schlicker
  • Published 2006
  • Chemistry, Medicine
  • Naunyn-Schmiedeberg's Archives of Pharmacology
  • The mechanism of action of cannabidiol, one of the major constituents of cannabis, is not well understood but a noncompetitive interaction with mu opioid receptors has been suggested on the basis of saturation binding experiments. The aim of the present study was to examine whether cannabidiol is an allosteric modulator at this receptor, using kinetic binding studies, which are particularly sensitive for the measurement of allosteric interactions at G protein-coupled receptors. In addition, we… CONTINUE READING
    192 Citations

    Paper Mentions

    Observational Clinical Trial
    The aim of this study is to evaluate the efficacy of oral administration of nabilone or THC/CBD administration in combination with spinal cord stimulation (SCS) in FBSS patients… Expand
    ConditionsFBSS
    InterventionDrug
    The cannabinoid receptor agonists, anandamide and WIN 55,212-2, do not directly affect mu opioid receptors expressed in Xenopus oocytes
    • 4
    • Highly Influenced
    Binding and Signaling Studies Disclose a Potential Allosteric Site for Cannabidiol in Cannabinoid CB2 Receptors
    • 59
    • PDF
    Effects of cannabidiol on the function of α7-nicotinic acetylcholine receptors.
    • 42
    CB1 receptors modulate the intake of a sweetened-fat diet in response to mu-opioid receptor stimulation of the nucleus accumbens
    • 31
    Exploring the first Rimonabant analog-opioid peptide hybrid compound, as bivalent ligand for CB1 and opioid receptors
    • 17
    • PDF

    References

    SHOWING 1-10 OF 44 REFERENCES
    Modulation of rat brain opioid receptors by cannabinoids.
    • 77
    Pharmacology of cannabinoid receptor ligands.
    • R. Pertwee
    • Chemistry, Medicine
    • Current medicinal chemistry
    • 1999
    • 495
    The effects of cannabinoids on the brain
    • A. Ameri
    • Chemistry, Medicine
    • Progress in Neurobiology
    • 1999
    • 736
    Inverse agonism and neutral antagonism at cannabinoid CB1 receptors.
    • 413
    International Union of Pharmacology. XXVII. Classification of Cannabinoid Receptors
    • 2,273
    • PDF
    Modulation of transmitter release via presynaptic cannabinoid receptors.
    • 606
    [3H]naltrindole: a potent and selective ligand for labeling delta-opioid receptors.
    • 1
    (-)-Cannabidiol antagonizes cannabinoid receptor agonists and noradrenaline in the mouse vas deferens.
    • 117