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SB-243213 is a research chemical which acts as a selective inverse agonist for the 5HT2Creceptor and has anxiolytic effects. It has better than 100x selectivity for 5-HT2C over all other receptor subtypes tested, and a longer duration of action compared to older 5-HT2C antagonist ligands.[1][2][3][4][5][6][7][8]
^Wood MD, Reavill C, Trail B, Wilson A, Stean T, Kennett GA, et al. (August 2001). "SB-243213; a selective 5-HT2C receptor inverse agonist with improved anxiolytic profile: lack of tolerance and withdrawal anxiety". Neuropharmacology. 41 (2): 186–99. doi:10.1016/S0028-3908(01)00054-5. PMID11489455. S2CID36124035.
^Blackburn TP, Minabe Y, Middlemiss DN, Shirayama Y, Hashimoto K, Ashby CR (December 2002). "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. doi:10.1002/syn.10116. PMID12325040. S2CID36766760.
^Di Matteo V, Pierucci M, Esposito E (April 2004). "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. doi:10.1111/j.1471-4159.2004.02337.x. PMID15056285. S2CID29021463.
^Millan MJ, Brocco M, Gobert A, Dekeyne A (February 2005). "Anxiolytic properties of agomelatine, an antidepressant with melatoninergic and serotonergic properties: role of 5-HT2C receptor blockade". Psychopharmacology. 177 (4): 448–58. doi:10.1007/s00213-004-1962-z. PMID15289999. S2CID20866665.
^Berg KA, Navailles S, Sanchez TA, Silva YM, Wood MD, Spampinato U, Clarke WP (October 2006). "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. doi:10.1124/jpet.106.104448. PMID16807362. S2CID14889900.
^Monti JM, Jantos H (December 2006). "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. doi:10.1016/j.ejphar.2006.09.027. PMID17059817.
^Kadiri N, Lagière M, Le Moine C, Millan MJ, De Deurwaerdère P, Navailles S (August 2012). "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. doi:10.1016/j.ejphar.2012.05.022. PMID22643326.
This page was last edited on 22 January 2024, at 21:28