AM-630
Encyclopedia
AM-630 is a drug which acts as a potent and selective inverse agonist
for the cannabinoid receptor
CB2, with a Ki of 32.1nM at CB2 and 165x selectivity over CB1, at which it acted as a weak partial agonist
. It is used in the study of CB2 mediated responses and has been used to investigate the possible role of CB2 receptors in the brain. AM-630 is significant as one of the first indole derived cannabinoid ligands substituted on the 6-position of the indole ring, a position which has subsequently been found to be important in determining affinity and efficacy at both the CB1 and CB2 receptors, and has led to the development of a large number of related derivatives.
Inverse agonist
In the field of pharmacology, an inverse agonist is an agent that binds to the same receptor as an agonist but induces a pharmacological response opposite to that agonist....
for the cannabinoid receptor
Cannabinoid receptor
The cannabinoid receptors are a class of cell membrane receptors under the G protein-coupled receptor superfamily. As is typical of G protein-coupled receptors, the cannabinoid receptors contain seven transmembrane spanning domains...
CB2, with a Ki of 32.1nM at CB2 and 165x selectivity over CB1, at which it acted as a weak partial agonist
Partial agonist
Partial agonists bind and activate a given receptor, but have only partial efficacy at the receptor relative to a full agonist...
. It is used in the study of CB2 mediated responses and has been used to investigate the possible role of CB2 receptors in the brain. AM-630 is significant as one of the first indole derived cannabinoid ligands substituted on the 6-position of the indole ring, a position which has subsequently been found to be important in determining affinity and efficacy at both the CB1 and CB2 receptors, and has led to the development of a large number of related derivatives.