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A-834,735

A-834,735 is a drug developed by Abbott Laboratories that acts as a potent cannabinoid receptor full agonist at both the CB<sub>1</sub> and CB<sub>2</sub> receptors, with a K<sub>i</sub> of 12&nbsp;nM at CB<sub>1</sub> and 0.21&nbsp;nM at CB<sub>2</sub>. 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 CB<sub>2</sub>, with most compounds from this group found to be highly selective CB<sub>2</sub> agonists with little affinity for CB<sub>1</sub>. However, low nanomolar CB<sub>1</sub> 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 CB<sub>2</sub> selective overall.

Legal status

As of October 2015 A-834,735 is a controlled substance in China.

See also

References