AM-1221
Encyclopedia
AM-1221 is a drug which acts as a potent and selective agonist
for the cannabinoid receptor
CB2, with a Ki
of 0.28nM at CB2 and 52.3nM at the CB1 receptor, giving it around 180x selectivity for CB2. The 2-methyl and 6-nitro
groups on the 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.
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...
CB2, 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 0.28nM at CB2 and 52.3nM at the CB1 receptor, giving it around 180x selectivity for CB2. The 2-methyl and 6-nitro
Nitro compound
Nitro compounds are organic compounds that contain one or more nitro functional groups . They are often highly explosive, especially when the compound contains more than one nitro group and is impure. The nitro group is one of the most common explosophores used globally...
groups on the 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...
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
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...
is generally preferred for research purposes.
See also
- AM-630AM-630AM-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...
- AM-1220AM-1220AM-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-1235AM-1235AM-1235 is a drug which acts as a potent and reasonably selective agonist for the cannabinoid receptor CB1, with a Ki of 1.5nM at CB1 compared to 20.4nM at CB2...
- AM-2233AM-2233AM-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...
- N-(S)-Fenchyl-1-(2-morpholinoethyl)-7-methoxyindole-3-carboxamideN-(S)-Fenchyl-1-(2-morpholinoethyl)-7-methoxyindole-3-carboxamide7-methoxy-1--N--1H-indole-3-carboxamide is a drug invented by Bristol-Myers Squibb, that acts as a reasonably selective agonist of peripheral cannabinoid receptors...