SB-243213

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SB-243213
SB243213 structure.png
Systematic (IUPAC) name
5-methyl-N-(6-[(2-methylpyridin-3-yl)oxy]pyridin-3-yl)-6-(trifluoromethyl)indoline-1-carboxamide
Identifiers
CAS Registry Number 200940-23-4
PubChem CID: 443391
Chemical data
Formula C22H19F3N4O2
Molecular mass 428.41 g/mol

SB-243213 is a research chemical which acts as a selective inverse agonist for the 5HT2C receptor 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]

See also[edit]

References[edit]

  1. ^ Wood, M. D.; Reavill, C.; Trail, B.; Wilson, A.; Stean, T.; Kennett, G. A.; Lightowler, S.; Blackburn, T. P.; Thomas, D.; Gager, T. L.; Riley, G.; Holland, V.; Bromidge, S. M.; Forbes, I. T.; Middlemiss, D. N. (2001). "SB-243213; a selective 5-HT2C receptor inverse agonist with improved anxiolytic profile: Lack of tolerance and withdrawal anxiety". Neuropharmacology 41 (2): 186–199. doi:10.1016/S0028-3908(01)00054-5. PMID 11489455.  edit
  2. ^ Blackburn, T. P.; Minabe, Y.; Middlemiss, D. N.; Shirayama, Y.; Hashimoto, K.; Ashby Jr, C. R. (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): 129–139. doi:10.1002/syn.10116. PMID 12325040.  edit
  3. ^ Di Matteo, V.; Pierucci, M.; Esposito, E. (2004). "Selective stimulation of serotonin2Creceptors blocks the enhancement of striatal and accumbal dopamine release induced by nicotine administration". Journal of Neurochemistry 89 (2): 418–429. doi:10.1111/j.1471-4159.2004.02337.x. PMID 15056285.  edit
  4. ^ Millan, M. J.; Brocco, M.; Gobert, A.; Dekeyne, A. (2004). "Anxiolytic properties of agomelatine, an antidepressant with melatoninergic and serotonergic properties: Role of 5-HT2C receptor blockade". Psychopharmacology 177 (4): 448–458. doi:10.1007/s00213-004-1962-z. PMID 15289999.  edit
  5. ^ Berg, K. A.; Navailles, S.; Sanchez, T. A.; Silva, Y. M.; Wood, M. D.; Spampinato, U.; Clarke, W. P. (2006). "Differential effects of 5-methyl-1-2-(2-methyl-3-pyridyl)oxyl-5-pyridylcarbamoyl-6-trifluoromethylindone (SB 243213) on 5-hydroxytryptamine(2C) receptor-mediated responses". Journal of Pharmacology and Experimental Therapeutics 319 (1): 260–268. doi:10.1124/jpet.106.104448. PMID 16807362.  edit
  6. ^ Monti, J. M.; Jantos, H. C. (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): 163–170. doi:10.1016/j.ejphar.2006.09.027. PMID 17059817.  edit
  7. ^ Leggio, G. M.; Cathala, A.; Moison, D.; Cunningham, K. A.; Piazza, P. V.; Spampinato, U. (2009). "Serotonin2C receptors in the medial prefrontal cortex facilitate cocaine-induced dopamine release in the rat nucleus accumbens". Neuropharmacology 56 (2): 507–513. doi:10.1016/j.neuropharm.2008.10.005. PMC 3130963. PMID 18977370.  edit
  8. ^ Kadiri, N.; Lagière, M. L.; Le Moine, C.; Millan, M. J.; De Deurwaerdère, P.; Navailles, S. (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. PMID 22643326.  edit