A 5-HT2C receptor inverse agonist
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SB-243213 (hydrochloride)

Item No. 36217

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2,3-dihydro-5-methyl-N-[6-[(2-methyl-3-pyridinyl)oxy]-3-pyridinyl]-6-(trifluoromethyl)-1H-indole-1-carboxamide, dihydrochloride
CAS Number
1780372-25-9
Molecular Formula
C22H19F3N4O2 • 2HCl
Formula Weight
501.3
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: 50m MEthanol: 100 mM
SMILES
O=C(N1C2=C(CC1)C=C(C)C(C(F)(F)F)=C2)NC3=CN=C(OC4=C(C)N=CC=C4)C=C3.Cl.Cl
InChi Code
InChI=1S/C22H19F3N4O2.2ClH/c1-13-10-15-7-9-29(18(15)11-17(13)22(23,24)25)21(30)28-16-5-6-20(27-12-16)31-19-4-3-8-26-14(19)2;;/h3-6,8,10-12H,7,9H2,1-2H3,(H,28,30);2*1H
InChi Key
UKMTYUXWLKQDNT-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

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    5 mg

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    Product Description

    SB-243213 is an inverse agonist of the serotonin (5-HT) receptor subtype 5-HT2C.1 It is selective for 5-HT2C over 5-HT2A and 5-HT2B receptors (Kis = 0.001, 0.158, and 0.1 µM, respectively) and the cytochrome P450 (CYP) isoforms CYP1A2, CYP2C9, CYP2C19, CYP2D6, and CYP3A4 (IC50s = >100, 23, >100, >100, and >100 µM, respectively). SB-243213 reduces the basal activity of 5-HT2C in HEK293 cells expressing the human 5-HT2C receptor (pKB = 9.5). It reverses mCPP-induced hypolocomotion in rats (ID50 = 0.7 mg/kg). SB-243213 (0.2-5 mg/kg) has anxiolytic-like activity in the social interaction test in rats.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Bromidge, S.M., Dabbs, S., Davies, D.T., et al. Biarylcarbamoylindolines are novel and selective 5-HT2C receptor inverse agonists: Identification of 5-methyl-1-[[2-[(2-methyl-3-pyridyl)oxy]-5-pyridyl]carbamoyl]-6-trifluoromethylindoline (SB-243213) as a potential antidepressant/anxiolytic agent. J. Med. Chem. 43(6), 1123-1134 (2000).