| Name | SB 242084 dihydrochloride |
| 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. |
| 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]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| 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.
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| Keywords | SB242084 | SB-242084 | SB-242084 Dihydrochloride | SB 242084 Dihydrochloride | SB 242084 dihydrochloride | SB242084 Dihydrochloride | SB 242084 |
United States
