Summary
A-834,735 is a drug developed by Abbott Laboratories that acts as a potent cannabinoid receptor full agonist at both the CB1 and CB2 receptors, with a Ki of 12 nM at CB1 and 0.21 nM at CB2. Replacing the aromatic 3-benzoyl or 3-naphthoyl group found in most indole derived cannabinoids with the 3-tetramethylcyclopropylmethanone group of A-834,735 and related compounds imparts significant selectivity for CB2, with most compounds from this group found to be highly selective CB2 agonists with little affinity for CB1. However, low nanomolar CB1 binding affinity is retained with certain heterocyclic 1-position substituents such as (N-methylpiperidin-2-yl)methyl (cf. AM-1220, AM-1248), or the (tetrahydropyran-4-yl)methyl substituent of A-834,735, resulting in compounds that still show significant affinity and efficacy at both receptors despite being CB2 selective overall.
Tolerance
Effects
- Muscle relaxation
- Anxiolytic
- Muscle Relaxant
- Physical euphoria
- Motor impairment
- Respiratory depression
- Sedation
- Sedative
- Dystaxia
- Hypnotic
- Anxiety suppression
- Reduced anxiety
- Amnesia
- Motor control loss
- Thought deceleration
- Emotion suppression
- Dizziness
- Delusions of sobriety
- Compulsive redosing
- Memory suppression
- Increased libido
- Increased music appreciation
- Appetite enhancement
- Tactile enhancement
- Disinhibition
- Visual acuity suppression
- Acuity suppression
- Dulled perception
- Perception of bodily heaviness
- External hallucinations