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SB 242084 dihydrochloride

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Catalog No. T37114Cas No. 1049747-87-6

SB 242084 hydrochloride is a 5-HT2C receptor antagonist(pKi=9.0) that displays 158- and 100-fold selectivity over 5-HT2A and 5-HT2B receptors respectively.

SB 242084 dihydrochloride

SB 242084 dihydrochloride

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Catalog No. T37114Cas No. 1049747-87-6
SB 242084 hydrochloride is a 5-HT2C receptor antagonist(pKi=9.0) that displays 158- and 100-fold selectivity over 5-HT2A and 5-HT2B receptors respectively.
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2 mg$73 5 days
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Product Introduction

Bioactivity
Description
SB 242084 hydrochloride is a 5-HT2C receptor antagonist(pKi=9.0) that displays 158- and 100-fold selectivity over 5-HT2A and 5-HT2B receptors respectively.IC50 value: 9.0(pKi) [1]Target: 5-HT2C antagonistin vitro: SB 242084 had over 100-fold selectivity over a range of other 5-HT, dopamine and adrenergic receptors. In studies of 5-HT-stimulated phosphatidylinositol hydrolysis using SH-SY5Y cells stably expressing the cloned human 5-HT2C receptor, SB 242084 acted as an antagonist with a pKb of 9.3, which closely resembled its corresponding receptor binding affinity [1].in vivo: SB 242084 potently inhibited m-chlorophenylpiperazine (mCPP, 7 mgkg i.p. 20 min pre-test)-induced hypolocomotion in rats, a model of in vivo central 5-HT2C receptor function, with an ID50 of 0.11 mg/kg i.p., and 2.0 mg/kg p.o. SB 242084 (0.1-1 mg/kg i.p.) exhibited an anxiolytic-like profile in the rat social interaction test, increasing time spent in social interaction, but having no effect on locomotion. SB 242084 (0.1-1 mg/kg i.p.) also markedly increased punished responding in a rat Geller-Seifter conflict test of anxiety, but had no consistent effect on unpunished responding [1].
In vitro
In vitro, SB 242084 had over 100-fold selectivity over a range of other 5-HT, dopamine and adrenergic receptors. In studies of 5-HT-stimulated phosphatidylinositol hydrolysis using SH-SY5Y cells stably expressing the cloned human 5-HT2C receptor, SB 242084 acted as an antagonist with a pKb of 9.3, which closely resembled its corresponding receptor binding affinity [1].
In vivo
In vivo, SB 242084 potently inhibited m-chlorophenylpiperazine (mCPP, 7 mgkg i.p. 20 min pre-test)-induced hypolocomotion in rats, a model of in vivo central 5-HT2C receptor function, with an ID50 of 0.11 mg/kg i.p., and 2.0 mg/kg p.o. SB 242084 (0.1-1 mg/kg i.p.) exhibited an anxiolytic-like profile in the rat social interaction test, increasing time spent in social interaction, but having no effect on locomotion. SB 242084 (0.1-1 mg/kg i.p.) also markedly increased punished responding in a rat Geller-Seifter conflict test of anxiety, but had no consistent effect on unpunished responding [1].
Chemical Properties
Molecular Weight467.78
FormulaC21H21Cl3N4O2
Cas No.1049747-87-6
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
PBS (pH 7.2): 10 mg/mL (21.38 mM), Sonication is recommended.
Ethanol: 1 mg/mL (2.14 mM), Sonication is recommended.
DMF: 30 mg/mL (64.13 mM), Sonication is recommended.
DMSO: 30 mg/mL (64.13 mM), Sonication is recommended.
Solution Preparation Table
Ethanol/PBS (pH 7.2)/DMF/DMSO
1mg5mg10mg50mg
1 mM2.1378 mL10.6888 mL21.3776 mL106.8879 mL
PBS (pH 7.2)/DMF/DMSO
1mg5mg10mg50mg
5 mM0.4276 mL2.1378 mL4.2755 mL21.3776 mL
10 mM0.2138 mL1.0689 mL2.1378 mL10.6888 mL
20 mM0.1069 mL0.5344 mL1.0689 mL5.3444 mL
DMF/DMSO
1mg5mg10mg50mg
50 mM0.0428 mL0.2138 mL0.4276 mL2.1378 mL

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