A-834,735
Encyclopedia
A-834,735 is a drug developed by Abbott Laboratories
which acts as a potent cannabinoid receptor
full agonist at both the CB1 and CB2 receptors, with a Ki of 12nM at CB1 and 0.21nM 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 which still show significant affinity and efficacy at both receptors despite being CB2 selective overall.
Abbott Laboratories
Abbott Laboratories is an American-based global, diversified pharmaceuticals and health care products company. It has 90,000 employees and operates in over 130 countries. The company headquarters are in Abbott Park, North Chicago, Illinois. The company was founded by Chicago physician, Dr....
which acts as a potent cannabinoid receptor
Receptor (biochemistry)
In biochemistry, a receptor is a molecule found on the surface of a cell, which receives specific chemical signals from neighbouring cells or the wider environment within an organism...
full agonist at both the CB1 and CB2 receptors, with a Ki of 12nM at CB1 and 0.21nM at CB2. Replacing the aromatic 3-benzoyl or 3-naphthoyl group found in most indole
Indole
Indole is an aromatic heterocyclic organic compound. It has a bicyclic structure, consisting of a six-membered benzene ring fused to a five-membered nitrogen-containing pyrrole ring. Indole is a popular component of fragrances and the precursor to many pharmaceuticals. Compounds that contain an...
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-1220
AM-1220 is a drug which acts as a potent and moderately selective agonist for the cannabinoid receptor CB1, with around 19x selectivity for CB1 over the related CB2 receptor...
, AM-1248
AM-1248
AM-1248 is a drug which acts as a moderately potent agonist for both the cannabinoid receptors CB1 and CB2, but with some dispute between sources over its exact potency and selectivity...
), or the (tetrahydropyran-4-yl)methyl substituent of A-834,735, resulting in compounds which still show significant affinity and efficacy at both receptors despite being CB2 selective overall.
See also
- A-796,260A-796,260A-796,260 is a drug developed by Abbott Laboratories which 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...
- AB-001AB-001AB-001 or 1-pentyl-3-indole is a designer drug which was found as an ingredient in synthetic cannabis smoking blends in Ireland in 2010 and Hungary in 2011...
- JTE 7-31JTE 7-31JTE 7-31 is a selective cannabinoid receptor agonist invented by Japan Tobacco. It is a reasonably highly selective CB2 agonist, but still retains appreciable affinity at CB1, with a Ki of 0.088nM at CB2 vs 11nM at CB1.-See also:* A-834,735* JTE-907...
- (1-Pentylindol-3-yl)-(2,2,3,3-tetramethylcyclopropyl)methanone(1-Pentylindol-3-yl)-(2,2,3,3-tetramethylcyclopropyl)methanone-methanone is a drug invented by Abbott Laboratories, that acts as a selective full agonist of the peripheral cannabinoid receptor CB2, but with much lower affinity for the psychoactive CB1 receptor. It has high affinity for the CB2 receptor with a Ki of 1.8nM but 83x lower affinity for the CB1...