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Chemical Structure : SB 242084 hydrochloride
CAS No.: 1049747-87-6
Catalog No.: PC-43516Not 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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $88 | In stock | |
| 25 mg | $198 | In stock | |
| 100 mg | $528 | In stock | |
| 500 mg | Get quote |
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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; also displays >100-fold selectivity over a range of other 5-HT, dopamine and adrenergic receptors; inhibits 5-HT-stimulated phosphatidylinositol hydrolysis with pKb of 9.3 in cell-baed assays; 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 | ||
| Formula | C21H21Cl3N4O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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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]-, hydrochloride (1:2) |
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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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