SB 242084 hydrochloride

CAS No. : 1049747-87-6

SB 242084 hydrochloride,1049747-87-6
Product Details
For research use only. Not Intended for Therapeutic Use!
Cat No:I000275
Synonyms:6-chloro-2,3-dihydro-5-methyl-N-[6-[(2-methyl-3-pyridinyl)oxy]-3-pyridinyl]-1H-indole-1-carboxamide, dihydrochloride
Molecular Formula:C21H19ClN4O2 • 2HCl
Molecular Weight:467.8
Target:5-HT2C antagonist
IC50:9.0(pKi) [1]
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Appearance:A crystalline solid
Cat No:I000275
Cas No:1049747-87-6
Product-Name:SB 242084 hydrochloride

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 antagonist
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: 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].

[1]. Kennett GA, et al. SB 242084, a selective and brain penetrant 5-HT2C receptor antagonist. Neuropharmacology. 1997 Apr-May;36(4-5):609-20.
[2]. Bromidge SM, et al. 6-Chloro-5-methyl-1-[[2-[(2-methyl-3-pyridyl)oxy]-5-pyridyl]carbamoyl]- indoline (SB-242084): the first selective and brain penetrant 5-HT2C receptor antagonist. J Med Chem. 1997 Oct 24;40(22):3494-6.
[3]. Dalton GL, et al. Serotonin 1B and 2C receptor interactions in the modulation of feeding behaviour in the mouse. Psychopharmacology (Berl). 2006 Mar;185(1):45-57.

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