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

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

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 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 **Nitroalkene, ...

groups on the

indole Indole is an aromatic heterocyclic organic compound In chemistry, organic compounds are generally any chemical compounds that contain carbon-hydrogen or carbon-carbon bonds. Due to carbon's ability to catenate (form chains with other c ...

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 AM-1241 (1-(methylpiperidin-2-ylmethyl)-3-(2-iodo-5-nitrobenzoyl)indole) is a chemical from the aminoalkylindole family that acts as a potent and selective agonist for the cannabinoid receptor CB2, with a Ki of 3.4 nM at CB2 and 80 times s ...

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 This is the list of Schedule I drugs as defined by the United States Controlled Substances Act. 21 CFRbr>1308.11(CSA Sched I) with changes through (Oct 18, 2012). Retrieved September 6, 2013. The following findings are required for drugs to be pla ...

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 The Psychoactive Substances Act 2016 (c. 2) is an Act of the Parliament of the United Kingdom intended to restrict the production, sale and supply of a new class of psychoactive substances often referred to as "legal highs". The bill was given R ...

which was inforce on May 26th 2016.

References

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

Legal status

See also

References