Description
SB 243213 hydrochloride 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 hydrochloride shows greater than a 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels. SB 243213 hydrochloride has improved anxiolytic profile and has the potential for schizophrenia and motor disorders.
Product information
CAS Number: 200940-23-4
Molecular Weight: 464.87
Formula: C22H20ClF3N4O2
Chemical Name: 5-methyl-N-{6-[(2-methylpyridin-3-yl)oxy]pyridin-3-yl}-6-(trifluoromethyl)-2, 3-dihydro-1H-indole-1-carboxamide hydrochloride
Smiles: Cl.CC1=NC=CC=C1OC1=CC=C(C=N1)NC(=O)N1CCC2=CC(C)=C(C=C12)C(F)(F)F
InChiKey: OOOGUILTDUSZPA-UHFFFAOYSA-N
InChi: InChI=1S/C22H19F3N4O2.ClH/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);1H
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
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 hydrochloride 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. SB 243213 hydrochloride shows 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels.
In Vivo:
SB 243213 hydrochloride (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 hydrochloride (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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