AM-630 (6-Iodopravadoline) is a drug that acts as a potent and selective

inverse agonist In pharmacology, an inverse agonist is a drug that binds to the same receptor as an agonist but induces a pharmacological response opposite to that of the agonist. A neutral antagonist has no activity in the absence of an agonist or inverse agon ...

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 recepto ...

CB₂, with a ''K''_i of 32.1 nM at CB₂ and 165x selectivity over CB₁, at which it acted as a weak

partial agonist In pharmacology, partial agonists are drugs that bind to and activate a given receptor, but have only partial efficacy at the receptor relative to a full agonist. They may also be considered ligands which display both agonistic and antagonistic e ...

. 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 that 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 many related derivatives.

References

Benzoylindoles AM cannabinoids Morpholines Aminoalkylindoles Iodoarenes Designer drugs {{cannabinoid-stub

See also

References