SB-243213 explained

SB-243213 is a research chemical which acts as a selective inverse agonist for the 5HT_2C receptor and has anxiolytic effects. It has better than 100x selectivity for 5-HT_2C over all other receptor subtypes tested, and a longer duration of action compared to older 5-HT_2C antagonist ligands.^{[1] [2] [3] [4] [5] [6] [7] [8]}

See also

• CEPC
• RS-102221
• SB-242084

Notes and References

1. Wood MD, Reavill C, Trail B, Wilson A, Stean T, Kennett GA, Lightowler S, Blackburn TP, Thomas D, Gager TL, Riley G, Holland V, Bromidge SM, Forbes IT, Middlemiss DN . 6 . SB-243213; a selective 5-HT2C receptor inverse agonist with improved anxiolytic profile: lack of tolerance and withdrawal anxiety . Neuropharmacology . 41 . 2 . 186–99 . August 2001 . 11489455 . 10.1016/S0028-3908(01)00054-5 . 36124035 .
2. Blackburn TP, Minabe Y, Middlemiss DN, Shirayama Y, Hashimoto K, Ashby CR . Effect of acute and chronic administration of the selective 5-HT2C receptor antagonist SB-243213 on midbrain dopamine neurons in the rat: an in vivo extracellular single cell study . Synapse . 46 . 3 . 129–39 . December 2002 . 12325040 . 10.1002/syn.10116 . 36766760 .
3. Di Matteo V, Pierucci M, Esposito E . Selective stimulation of serotonin2c receptors blocks the enhancement of striatal and accumbal dopamine release induced by nicotine administration . Journal of Neurochemistry . 89 . 2 . 418–29 . April 2004 . 15056285 . 10.1111/j.1471-4159.2004.02337.x . 29021463 .
4. Millan MJ, Brocco M, Gobert A, Dekeyne A . Anxiolytic properties of agomelatine, an antidepressant with melatoninergic and serotonergic properties: role of 5-HT2C receptor blockade . Psychopharmacology . 177 . 4 . 448–58 . February 2005 . 15289999 . 10.1007/s00213-004-1962-z . 20866665 .
5. Berg KA, Navailles S, Sanchez TA, Silva YM, Wood MD, Spampinato U, Clarke WP . Differential effects of 5-methyl-1-2-[(2-methyl-3-pyridyl)oxyl]-5-pyridyl]carbamoyl]-6-trifluoromethylindone (SB 243213) on 5-hydroxytryptamine(2C) receptor-mediated responses . The Journal of Pharmacology and Experimental Therapeutics . 319 . 1 . 260–8 . October 2006 . 16807362 . 10.1124/jpet.106.104448 . 14889900 .
6. Monti JM, Jantos H . Effects of the serotonin 5-HT2A/2C receptor agonist DOI and of the selective 5-HT2A or 5-HT2C receptor antagonists EMD 281014 and SB-243213, respectively, on sleep and waking in the rat . European Journal of Pharmacology . 553 . 1–3 . 163–70 . December 2006 . 17059817 . 10.1016/j.ejphar.2006.09.027 .
7. Leggio GM, Cathala A, Moison D, Cunningham KA, Piazza PV, Spampinato U . Serotonin2C receptors in the medial prefrontal cortex facilitate cocaine-induced dopamine release in the rat nucleus accumbens . Neuropharmacology . 56 . 2 . 507–13 . February 2009 . 18977370 . 3130963 . 10.1016/j.neuropharm.2008.10.005 .
8. Kadiri N, Lagière M, Le Moine C, Millan MJ, De Deurwaerdère P, Navailles S . Diverse effects of 5-HT2C receptor blocking agents on c-Fos expression in the rat basal ganglia . European Journal of Pharmacology . 689 . 1–3 . 8–16 . August 2012 . 22643326 . 10.1016/j.ejphar.2012.05.022 .