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SB 242084 hydrochloride

Chemical Structure : SB 242084 hydrochloride

CAS No.: 1049747-87-6

SB 242084 hydrochloride (SB242084 hydrochloride)

Catalog No.: PC-43516Not For Human Use, Lab Use Only.

SB 242084 hydrochloride is a potent, selective, brain penetrant 5-HT2C receptor antagonist with pKi of 9.0, 100- and 158-fold selectivity over the closely related 5-HT2B and 5-HT2A subtypes.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

SB 242084 hydrochloride is a potent, selective, brain penetrant 5-HT2C receptor antagonist with pKi of 9.0, 100- and 158-fold selectivity over the closely related 5-HT2B and 5-HT2A subtypes.
SB 242084 hydrochloride also displays >100-fold selectivity over a range of other 5-HT, dopamine and adrenergic receptors.
SB 242084 hydrochloride inhibits 5-HT-stimulated phosphatidylinositol hydrolysis with pKb of 9.3 in cell-baed assays.
SB 242084 hydrochloride potently inhibits m-chlorophenylpiperazine (mCPP)-induced hypolocomotion in rats, with an ID50 of 0.11 mg/kg i.p., and 2.0 mg/kg p.o.

Physicochemical Properties

M.Wt 467.78
Formula C21H21Cl3N4O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

1H-Indole-1-carboxamide, 6-chloro-2,3-dihydro-5-methyl-N-[6-[(2-methyl-3-pyridinyl)oxy]-3-pyridinyl]-, hydrochloride (1:2)

References

1. Bromidge SM, et al. J Med Chem. 1997 Oct 24;40(22):3494-6.

2. Kennett GA, et al. Neuropharmacology. 1997 Apr-May;36(4-5):609-20.

3. Di Matteo V, et al. Neuropharmacology. 1999 Aug;38(8):1195-205.

4. Higgins GA, et al. Br J Pharmacol. 2001 Jun;133(4):459-66.

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