AM-6545
 | |
| Identifiers | |
|---|---|
| |
| CAS Number |
1245626-05-4  |
| PubChem (CID) | 46912919 |
| ChemSpider |
26333263  |
| Chemical and physical data | |
| Formula | C26H23Cl2N5O3S |
| Molar mass | 556.463 g/mol |
| 3D model (Jmol) | Interactive image |
| |
| |
| (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 Other cannabinoid antagonists such as rimonabant have been marketed for this application, but have subsequently been withdrawn from sale because of centrally mediated side effects such as depression and nausea.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.[1][2][3][4]
See also
- 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
References
- ↑ 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 2912197
. PMID 20664173. PMID 20664173 - ↑ Randall PA, Vemuri VK, Segovia KN, Torres EF, Hosmer S, Nunes EJ, Santerre JL, Makriyannis A, Salamone JD. The novel cannabinoid CB1 antagonist AM6545 suppresses food intake and food-reinforced behavior. Pharmacology, Biochemistry and Behavior. 2010 Nov;97(1):179-84. PMID 20713079
- ↑ Cluny NL, Vemuri VK, Chambers AP, Limebeer CL, Bedard H, Wood JT, Lutz B, Zimmer A, Parker LA, Makriyannis A, Sharkey KA. 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. 2010 Oct;161(3):629-42. PMID 20880401
- ↑ Järbe TU, LeMay BJ, Vemuri VK, Vadivel SK, Zvonok A, Makriyannis A. Central mediation and differential blockade by cannabinergics of the discriminative stimulus effects of the cannabinoid CB1 receptor antagonist rimonabant in rats. Psychopharmacology (Berlin). 2011 Aug;216(3):355-65. PMID 21369753
This article is issued from Wikipedia - version of the 9/8/2016. The text is available under the Creative Commons Attribution/Share Alike but additional terms may apply for the media files.