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SB-243213

From Wikipedia, the free encyclopedia
Chemical compound

Pharmaceutical compound
SB-243213
Identifiers
  • 5-methyl-N-(6-[(2-methylpyridin-3-yl)oxy]pyridin-3-yl)-6-(trifluoromethyl)indoline-1-carboxamide
CAS Number
PubChemCID
ChemSpider
UNII
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC22H19F3N4O2
Molar mass428.415 g·mol−1
3D model (JSmol)
  • CC1=C(C(F)(F)F)C=C(N(C(NC2=CN=C(OC3=C(C)N=CC=C3)C=C2)=O)CC4)C4=C1
  • InChI=1S/C22H19F3N4O2/c1-13-10-15-7-9-29(18(15)11-17(13)22(23,24)25)21(30)28-16-5-6-20(27-12-16)31-19-4-3-8-26-14(19)2/h3-6,8,10-12H,7,9H2,1-2H3,(H,28,30)
  • Key:ZETBBVYSBABLHL-UHFFFAOYSA-N

SB-243213 is a research chemical which acts as a selectiveinverse agonist for the5HT2Creceptor and hasanxiolytic 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 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.PMID 11489455.S2CID 36124035.
  2. ^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.PMID 12325040.S2CID 36766760.
  3. ^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.PMID 15056285.S2CID 29021463.
  4. ^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.PMID 15289999.S2CID 20866665.
  5. ^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.PMID 16807362.S2CID 14889900.
  6. ^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.PMID 17059817.
  7. ^Leggio GM, Cathala A, Moison D, Cunningham KA, Piazza PV, Spampinato U (February 2009)."Serotonin2C receptors in the medial prefrontal cortex facilitate cocaine-induced dopamine release in the rat nucleus accumbens".Neuropharmacology.56 (2):507–13.doi:10.1016/j.neuropharm.2008.10.005.PMC 3130963.PMID 18977370.
  8. ^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.PMID 22643326.
5-HT1
5-HT1A
5-HT1B
5-HT1D
5-HT1E
5-HT1F
5-HT2
5-HT2A
5-HT2B
5-HT2C
5-HT37
5-HT3
5-HT4
5-HT5A
5-HT6
5-HT7
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