Description
SB 243213 is an orally active, selective and high-affinity 5-HT2C receptor antagonist with a pKi of 9.37 and a pKb of 9.8 for human 5-HT2C receptor. SB 243213 shows greater than a 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels. SB 243213 has improved anxiolytic profile and has the potential for schizophrenia and motor disorders.
Product information
CAS Number: 200940-22-3
Molecular Weight: 428.41
Formula: C22H19F3N4O2
Chemical Name: 5-methyl-N-{6-[(2-methylpyridin-3-yl)oxy]pyridin-3-yl}-6-(trifluoromethyl)-2,3-dihydro-1H-indole-1-carboxamide
Smiles: CC1=NC=CC=C1OC1=CC=C(C=N1)NC(=O)N1CCC2=CC(C)=C(C=C12)C(F)(F)F
InChiKey: ZETBBVYSBABLHL-UHFFFAOYSA-N
InChi: 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)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 125 mg/mL (291.78 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
SB 243213 shows little affinity (pKi<6) for cloned human 5-HT1A, 5-HT1B, 5-HT1E, 5- HT1F and 5-HT7 receptors. It shows weak affinity (pKi<6.5) for the cloned human 5-HT1D and D3 receptors and moderate affinity (pKi=6.7) for the cloned human D2 receptor.
In Vivo:
SB 243213 (0.1-10 mg/kg, p.o. 1 h pre-test) dose-dependently and significantly increases the amount of time rats spent in social interaction over 15 min under brightly lit conditions and in an unfamiliar test box. SB 243213 (0.3 mg/kg; p.o.; 1 h pre-test) significantly increases time spent in social interaction.
Products are for research use only. Not for human use.
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