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SB-242084 HCl

  Cat. No.:  DC7494   Featured
Chemical Structure
1049747-87-6
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More than 5000 active chemicals with high quality for research!
Field of application
5-HT2C receptor antagonist that displays 158- and 100-fold selectivity over 5-HT2A and 5-HT2Breceptors respectively. Also displays selectivity over a range of other 5-HT, dopamine and adrenergic receptors. Brain penetrant; exerts anxiolytic-like activity.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1049747-87-6
Chemical Name: 6-Chloro-2,3-dihydro-5-methyl-N-[6-[(2-methyl-3-pyridinyl)oxy]-3-pyridinyl]-1H-indole-1-carboxyamide dihydrochloride
Synonyms: SB242084,SB 242084,CAS 1049747-87-6
SMILES: O=C1C2=C(ON=C2C3=CC=NC=C3)C=C(C4=CC=C(OC)C=C4)N1C.[H]Cl
Formula: C21H19ClN4O2.2HCl
M.Wt: 467.78
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: IC50 value: 9.0(pKi) [1]Target: 5-HT2C antagonist
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: 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].i
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
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