Summary
A-796,260 is a drug developed by Abbott Laboratories that acts as a potent and selective cannabinoid CB2 receptor agonist. Replacing the aromatic 3-benzoyl or 3-naphthoyl group found in most indole derived cannabinoids with the 3-tetramethylcyclopropylmethanone group, imparts significant selectivity for CB2, and A-796,260 was found to be a highly selective CB2 agonist with little affinity for CB1, having a CB2 Ki of 4.6 nM vs 945 nM at CB1. It has potent analgesic and anti-inflammatory actions in animal models, being especially effective in models of neuropathic pain, but without producing cannabis-like behavioral effects.
Tolerance
Build-up
develops over 1–4 weeks of daily use; hypnotic tolerance faster than anxiolytic tolerance
Reset
weeks to months depending on half-life and duration of use; taper recommended
Effects
Positive
- Muscle relaxation
- Anxiolytic
- Muscle Relaxant
- Physical euphoria
Negative
- Motor impairment
- Respiratory depression
- Sedation
- Sedative
- Dystaxia
- Hypnotic
Positive
- Anxiety suppression
- Reduced anxiety
Negative
- Amnesia
- Motor control loss
- Thought deceleration
- Emotion suppression
- Dizziness
- Delusions of sobriety
- Compulsive redosing
- Memory suppression
Positive
- Increased libido
- Increased music appreciation
- Appetite enhancement
- Tactile enhancement
Negative
- Disinhibition
- Visual acuity suppression
- Acuity suppression
- Dulled perception
- Perception of bodily heaviness
- External hallucinations