Synonyms: AM-1710 | analog 4b [PMID: 18038967]

Compound class: Synthetic organic

Comment: AM1710 is a cannabilactone class, selective cannabinoid CB₂ receptor agonist [5]. The cannabilactones produce peripheral analgesic activity without the the psychoactive central nervous system side-effects of other CB₂ receptor agonists [3]. As expected from its pharmacological profile, AM1710 shows limited blood brain barrier penetration [5]. It has potent agonist activity at rat and mouse CB₂ receptors but much reduced activity at human receptors, so is an excellent tool for rodent studies, but it is less useful for translation-to-human studies. In vitro experiments have identified low-potency CB₁ inverse agonist activity, but the in vivo relevance of this discovery is undetermined [2].It is important to note that the sequence heterogeneity in CB₂ across species leads to different pharmacologic responses to identical drugs [1], so extrapolating results from rodent models to humans should be approached with caution.
A 2019 publication of work by Li et al. describes rodent experiments that they undertook to resolve the mechanism(s) by which AM1710 suppresses allodynia caused by distinct pathological processes [4]. Their investigations show that AM1710 is not a broad-spectrum analgesic. In rodent models it is effective in paclitaxel-induced mechanical and cold allodynia but not in mechanically-induced allodynia.