AM-411 explained
AM-411 (part of the AM cannabinoid series) is an analgesic drug that is a cannabinoid agonist. It is a derivative of Δ8-THC substituted with an adamantyl group at the 3-position, demonstrating that the binding pocket for the alkyl chain at this position can accommodate significant bulk.
AM-411 is a potent and fairly selective CB1 full agonist with a Ki of 6.80 nM, but is still also a moderately potent CB2 agonist with a Ki of 52.0 nM.[1] It produces similar effects to other cannabinoid agonists such as analgesia, sedation, and anxiolysis.[2] [3]
See also
Notes and References
- Lu D, Meng Z, Thakur GA, Fan P, Steed J, Tartal CL, Hurst DP, Reggio PH, Deschamps JR, Parrish DA, George C, Järbe TU, Lamb RJ, Makriyannis A . 6 . Adamantyl cannabinoids: a novel class of cannabinergic ligands . Journal of Medicinal Chemistry . 48 . 14 . 4576–85 . July 2005 . 15999995 . 10.1021/jm058175c .
- Järbe TU, DiPatrizio NV, Lu D, Makriyannis A . (−)-Adamantyl-delta8-tetrahydrocannabinol (AM-411), a selective cannabinoid CB1 receptor agonist: effects on open-field behaviors and antagonism by SR-141716 in rats . Behavioural Pharmacology . 15 . 7 . 517–21 . November 2004 . 15472574 . 10.1097/00008877-200411000-00008 . 23889056 .
- McLaughlin PJ, Lu D, Winston KM, Thakur G, Swezey LA, Makriyannis A, Salamone JD . Behavioral effects of the novel cannabinoid full agonist AM 411 . Pharmacology, Biochemistry, and Behavior . 81 . 1 . 78–88 . May 2005 . 15894067 . 10.1016/j.pbb.2005.02.005 . 806517 .