TABLE 5

Effects of cannabinoid CB1 and/or CB2 receptor agonists on ligand-gated ion channels

See Section III.D for references and further details.

Gated Channel and EffectEndocannabinoid(s)?Effective Concentration RangeNonendogenous Cannabinoid Agonist(s)?Effective Concentration Range
Enhancement of activation
    Glycine (native)YesNanomolarYesNanomolar
    Glycine α1, α1β1YesNanomolarYesNanomolar
    Glycine α1βYesNanomolarYesMicromolar
    NMDAYesaNanomolar or micromolarYesbMicromolar
Inhibition of activation
    5-HT3YescNanomolarYescNanomolar
    Acetylcholine (nicotinic)YescNanomolarYescNanomolar or micromolar
    Glycine (native)YesNanomolar or micromolarNoNanomolar
    Glycine α1, α1βNoNanomolarYesMicromolar
    Glycine α2, α3NoMicromolarYesNanomolar or micromolar
Radioligand binding (↓)
    BenzodiazepineNoMicromolarYesMicromolar

  • ↵a Also R-(+)-methanandamide.

  • ↵b Only R-(+)-methanandamide.

  • ↵c May target an allosteric site on this receptor.