SB-243213 (hydro<wbr/>chloride)

SB-243213 (hydrochloride)

CAT N°: 36217
Price:

From 66.00 56.10

SB-243213 is an inverse agonist of the serotonin (5-HT) receptor subtype 5-HT2C.{62633} It is selective for 5-HT2C over 5-HT2A and 5-HT2B receptors (Kis = 0.001, 0.158, and 0.1 µM, respectively) and the cytochrome P450 (CYP) isoforms CYP1A2, CYP2C9, CYP2C19, CYP2D6, and CYP3A4 (IC50s = >100, 23, >100, >100, and >100 µM, respectively). SB-243213 reduces the basal activity of 5-HT2C in HEK293 cells expressing the human 5-HT2C receptor (pKB = 9.5). It reverses mCPP-induced hypolocomotion in rats (ID50 = 0.7 mg/kg). SB-243213 (0.2-5 mg/kg) has anxiolytic-like activity in the social interaction test in rats.

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • 2,3-dihydro-5-methyl-N-[6-[(2-methyl-3-pyridinyl)oxy]-3-pyridinyl]-6-(trifluoromethyl)-1H-indole-1-carboxamide, dihydrochloride
  • Correlated keywords
    • 200940-22-3 SB243213 HEK-293 CYP-1A2 2C9 2C19 2D6 3A4
  • Product Overview:
    SB-243213 is an inverse agonist of the serotonin (5-HT) receptor subtype 5-HT2C.{62633} It is selective for 5-HT2C over 5-HT2A and 5-HT2B receptors (Kis = 0.001, 0.158, and 0.1 µM, respectively) and the cytochrome P450 (CYP) isoforms CYP1A2, CYP2C9, CYP2C19, CYP2D6, and CYP3A4 (IC50s = >100, 23, >100, >100, and >100 µM, respectively). SB-243213 reduces the basal activity of 5-HT2C in HEK293 cells expressing the human 5-HT2C receptor (pKB = 9.5). It reverses mCPP-induced hypolocomotion in rats (ID50 = 0.7 mg/kg). SB-243213 (0.2-5 mg/kg) has anxiolytic-like activity in the social interaction test in rats.

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