AM-679 (cannabinoid)
Encyclopedia
AM-679 is a drug which acts as a moderately potent agonist
for the cannabinoid receptor
s, with a Ki
of 13.5nM at CB1 and 49.5nM at CB2. AM-679 was one of the first 3-(2-iodobenzoyl)indole derivatives that was found to have significant cannabinoid receptor affinity, and while AM-679 itself has only modest affinity for these receptors, it was subsequently used as a base to develop several more specialised cannabinoid ligands which are now widely used in research, including the potent CB1 agonists AM-694
and AM-2233
, and the selective CB2 agonist AM-1241
. AM-679 was first identified as having been sold as a cannabinoid designer drug
in Hungary in 2011, along with another novel compound 1-pentyl-3-(1-adamantoyl)indole.
Agonist
An agonist is a chemical that binds to a receptor of a cell and triggers a response by that cell. Agonists often mimic the action of a naturally occurring substance...
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...
s, with a Ki
Dissociation constant
In chemistry, biochemistry, and pharmacology, a dissociation constant is a specific type of equilibrium constant that measures the propensity of a larger object to separate reversibly into smaller components, as when a complex falls apart into its component molecules, or when a salt splits up into...
of 13.5nM at CB1 and 49.5nM at CB2. AM-679 was one of the first 3-(2-iodobenzoyl)indole derivatives that was found to have significant cannabinoid receptor affinity, and while AM-679 itself has only modest affinity for these receptors, it was subsequently used as a base to develop several more specialised cannabinoid ligands which are now widely used in research, including the potent CB1 agonists AM-694
AM-694
AM-694 is a drug which acts as a potent and selective agonist for the cannabinoid receptor CB1, with a Ki of 0.08nM at CB1 and 18x selectivity over the related CB2 receptor....
and AM-2233
AM-2233
AM-2233 is a drug which acts as a highly potent full agonist for the cannabinoid receptors, with a Ki of 1.8nM at CB1 and 2.2nM at CB2 as the active enantiomer. It was developed as a selective radioligand for the cannabinoid receptors and has been used as its 131I derivative for mapping the...
, and the selective CB2 agonist AM-1241
AM-1241
AM-1241 is a chemical from the aminoalkylindole family, which acts as a potent and selective agonist for the cannabinoid receptor CB2, with a Ki of 3.4nM at CB2 and 80x selectivity over the related CB1 receptor...
. AM-679 was first identified as having been sold as a cannabinoid designer drug
Designer drug
Designer drug is a term used to describe drugs that are created to get around existing drug laws, usually by preparing analogs or derivatives of existing drugs by modifying their chemical structure to varying degrees, or less commonly by finding drugs with entirely different chemical structures...
in Hungary in 2011, along with another novel compound 1-pentyl-3-(1-adamantoyl)indole.