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 Effect | Endocannabinoid(s)? | Effective Concentration Range | Nonendogenous Cannabinoid Agonist(s)? | Effective Concentration Range |
|---|---|---|---|---|
| Enhancement of activation | ||||
| Glycine (native) | Yes | Nanomolar | Yes | Nanomolar |
| Glycine α1, α1β1 | Yes | Nanomolar | Yes | Nanomolar |
| Glycine α1β | Yes | Nanomolar | Yes | Micromolar |
| NMDA | Yesa | Nanomolar or micromolar | Yesb | Micromolar |
| Inhibition of activation | ||||
| 5-HT3 | Yesc | Nanomolar | Yesc | Nanomolar |
| Acetylcholine (nicotinic) | Yesc | Nanomolar | Yesc | Nanomolar or micromolar |
| Glycine (native) | Yes | Nanomolar or micromolar | No | Nanomolar |
| Glycine α1, α1β | No | Nanomolar | Yes | Micromolar |
| Glycine α2, α3 | No | Micromolar | Yes | Nanomolar or micromolar |
| Radioligand binding (↓) | ||||
| Benzodiazepine | No | Micromolar | Yes | Micromolar |
a
Also R-(+)-methanandamide.
b
Only R-(+)-methanandamide.
c
May target an allosteric site on this receptor.