CB1 NAM
CB1 cannabinoid receptor negative allosteric modulator
- Dampens cannabinoid agonist responses without occupying the orthosteric site
- ↓ effects of CB1 agonists; may temper THC-type intoxication
- Possible antipsychotic effect
- Mechanism likely multifactorial
- ↑ endocannabinoid tone — anandamide rises by displacement from its carrier proteins, not by blocking human FAAH
Drugs with this mechanism (1)
- Cannabidiol — Purified, nonintoxicating cannabinoid for severe developmental epilepsies.
Self-check
- Does CB1 negative allosteric modulation occupy the orthosteric site?
No. - How does the anandamide increase described here occur?
Displacement from carrier proteins, not human FAAH blockade.