AM-1221 is a drug that acts as a potent and selective

agonist An agonist is a chemical that activates a Receptor (biochemistry), receptor to produce a biological response. Receptors are Cell (biology), cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an R ...

for the

cannabinoid receptor Cannabinoid receptors, located throughout the body, are part of the endocannabinoid system of vertebrates a class of cell membrane receptors in the G protein-coupled receptor superfamily. As is typical of G protein-coupled receptors, the cann ...

CB₂, with a ''K''_i of 0.28 nM at CB₂ and 52.3 nM at the CB₁ receptor, giving it around 180 times selectivity for CB₂. The 2-

methyl In organic chemistry, a methyl group is an alkyl derived from methane, containing one carbon atom bonded to three hydrogen atoms, having chemical formula (whereas normal methane has the formula ). In formulas, the group is often abbreviated as ...

and 6-

nitro Nitro may refer to: Chemistry *Nitrogen, a chemical element and a gas except at very low temperatures, with which many compounds are formed: **Nitro compound, an organic compound containing one or more nitro functional groups, -NO2 **Nitro ligand ...

groups on the

indole Indole is an organic compound with the formula . Indole is classified as an aromatic heterocycle. It has a bicyclic structure, consisting of a six-membered benzene ring fused to a five-membered pyrrole ring. Indoles are derivatives of indole ...

ring both tend to increase CB₂ affinity while generally reducing affinity at CB₁, explaining the high CB₂ selectivity of AM-1221. However, despite this relatively high selectivity for CB₂, its CB₁ affinity is still too strong to make it useful as a truly selective CB₂ agonist, so the related compound AM-1241 is generally preferred for research purposes. In the United States, all CB₁ receptor agonists of the 3-(1-naphthoyl)indole class such as AM-1221 are

Schedule I Controlled Substance The Controlled Substances Act (CSA) is the statute establishing federal U.S. drug policy under which the manufacture, importation, possession, use, and distribution of certain substances is regulated. It was passed by the 91st United State ...

Legal status

It is illegal to supply, trade, sell, distribute, import or transport the pharmaceutical drug in the UK under the Psychoactive Substances Act 2016 which was in force on May 26, 2016.

References

Naphthoylindoles AM cannabinoids Aminoalkylindoles Nitroarenes Piperidines Designer drugs CB1 receptor agonists CB2 receptor agonists {{cannabinoid-stub

Legal status

See also

References