|Chemical and physical data|
|Molar mass||556.463 g/mol|
|3D model (Jmol)|
|(what is this?)|
AM-6545 is a drug which acts as a peripherally selective silent antagonist for the CB1 receptor, and was developed for the treatment of obesity. Other cannabinoid antagonists such as rimonabant have been marketed for this application, but have subsequently been withdrawn from sale because of centrally mediated side effects such as depression and nausea. Because AM-6545 does not cross the blood–brain barrier to any significant extent, it does not produce these kinds of side effects, but has still been shown to effectively reduce appetite and food consumption in animal studies.
- CB-13 – a peripherally selective cannabinoid agonist
- O-2050 – a centrally active CB1 silent antagonist
- Methylnaltrexone – a peripherally selective mu opioid receptor antagonist
- TM-38837 - another peripherally selective cannabinoid antagonist
- Tam, J.; Vemuri, V. K.; Liu, J.; Bátkai, S. N.; Mukhopadhyay, B.; Godlewski, G.; Osei-Hyiaman, D.; Ohnuma, S.; Ambudkar, S. V.; Pickel, J.; Makriyannis, A.; Kunos, G. (2010). "Peripheral CB1 cannabinoid receptor blockade improves cardiometabolic risk in mouse models of obesity". Journal of Clinical Investigation. 120 (8): 2953–2966. doi:10.1172/JCI42551. PMC . PMID 20664173.
- Randall, PA; Vemuri, VK; Segovia, KN; Torres, EF; Hosmer, S; Nunes, EJ; Santerre, JL; Makriyannis, A; Salamone, JD (Nov 2010). "The novel cannabinoid CB1 antagonist AM6545 suppresses food intake and food-reinforced behavior". Pharmacology, Biochemistry and Behavior. 97 (1): 179–84. doi:10.1016/j.pbb.2010.07.021. PMC . PMID 20713079.
- Cluny, NL; Vemuri, VK; Chambers, AP; Limebeer, CL; Bedard, H; Wood, JT; Lutz, B; Zimmer, A; Parker, LA; Makriyannis, A; Sharkey, KA (Oct 2010). "A novel peripherally restricted cannabinoid receptor antagonist, AM6545, reduces food intake and body weight, but does not cause malaise, in rodents". British Journal of Pharmacology. 161 (3): 629–42. doi:10.1111/j.1476-5381.2010.00908.x. PMC . PMID 20880401.
- Järbe, TU; LeMay, BJ; Vemuri, VK; Vadivel, SK; Zvonok, A; Makriyannis, A (Aug 2011). "Central mediation and differential blockade by cannabinergics of the discriminative stimulus effects of the cannabinoid CB1 receptor antagonist rimonabant in rats". Psychopharmacology (Berlin). 216 (3): 355–65. doi:10.1007/s00213-011-2226-3. PMID 21369753.