Chemical Structure : SB 242084
CAS No.: 181632-25-7
Catalog No.: PC-43515Not For Human Use, Lab Use Only.
SB 242084 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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SB 242084 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 also displays >100-fold selectivity over a range of other 5-HT, dopamine and adrenergic receptors.
SB 242084 inhibits 5-HT-stimulated phosphatidylinositol hydrolysis with pKb of 9.3 in cell-baed assays.
SB 242084 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.
M.Wt | 394.86 | |
Formula | C21H19ClN4O2 | |
Appearance | Solid | |
Storage |
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Solubility |
DMSO: ≥ 44 mg/mL |
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Chemical Name/SMILES |
1H-Indole-1-carboxamide, 6-chloro-2,3-dihydro-5-methyl-N-[6-[(2-methyl-3-pyridinyl)oxy]-3-pyridinyl]- |
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.
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