AM-6545
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| ECHA InfoCard | 100.216.518 |
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| Formula | C26H23Cl2N5O3S |
| Molar mass | 556.46g·mol−1 |
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AM-6545is a drug which acts as a peripherally selectivesilent antagonistfor theCB1receptor,and was developed for the treatment ofobesity.Othercannabinoid antagonistssuch asrimonabanthave been marketed for this application, but have subsequently been withdrawn from sale because of centrally mediated side effects such asdepressionandnausea.Because AM-6545 does not cross theblood–brain barrierto any significant extent,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.[1][2][3][4]
See also
[edit]- CB-13– a peripherally selective cannabinoid agonist
- O-2050– a centrally active CB1silent antagonist
- Methylnaltrexone– a peripherally selectivemu opioid receptorantagonist
- TM-38837- another peripherally selective cannabinoid antagonist
References
[edit]- ^Tam J, Vemuri VK, Liu J, Bátkai S, Mukhopadhyay B, Godlewski G, Osei-Hyiaman D, Ohnuma S, Ambudkar SV, Pickel J, Makriyannis A, Kunos G (August 2010)."Peripheral CB1 cannabinoid receptor blockade improves cardiometabolic risk in mouse models of obesity".The Journal of Clinical Investigation.120(8): 2953–66.doi:10.1172/JCI42551.PMC2912197.PMID20664173.
- ^Randall PA, Vemuri VK, Segovia KN, Torres EF, Hosmer S, Nunes EJ, Santerre JL,Makriyannis A,Salamone JD (November 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.PMC3522179.PMID20713079.
- ^Cluny NL, Vemuri VK, Chambers AP, Limebeer CL, Bedard H, Wood JT, Lutz B, Zimmer A, Parker LA, Makriyannis A, Sharkey KA (October 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.PMC2990160.PMID20880401.
- ^Järbe TU, LeMay BJ, Vemuri VK, Vadivel SK, Zvonok A, Makriyannis A (August 2011)."Central mediation and differential blockade by cannabinergics of the discriminative stimulus effects of the cannabinoid CB1 receptor antagonist rimonabant in rats".Psychopharmacology.216(3): 355–65.doi:10.1007/s00213-011-2226-3.PMC3727221.PMID21369753.