Specific antagonist of 5-HT2C
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SB-242084 (hydrochloride)

Item No. 10096

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6-chloro-2,3-dihydro-5-methyl-N-[6-[(2-methyl-3-pyridinyl)oxy]-3-pyridinyl]-1H-indole-1-carboxamide, dihydrochloride
CAS Number
1049747-87-6
Molecular Formula
C21H19ClN4O2 • 2HCl
Formula Weight
467.8
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 1 mg/ml
λmax
212, 265 nm
SMILES
CC1=NC=CC=C1OC(N=C2)=CC=C2NC(N3CCC4=C3C=C(Cl)C(C)=C4)=O.Cl.Cl
InChi Code
InChI=1S/C21H19ClN4O2.2ClH/c1-13-10-15-7-9-26(18(15)11-17(13)22)21(27)25-16-5-6-20(24-12-16)28-19-4-3-8-23-14(19)2;;/h3-6,8,10-12H,7,9H2,1-2H3,(H,25,27);2*1H
InChi Key
GCMNSEILNIPNSX-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $52

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    5 mg

    $151

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    10 mg

    $201

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    Product Description

    SB-242084 is an antagonist of the 5-HT2C receptor (pKi = 9.0), with at least 100-fold more selectivity over other 5-HT, dopamine, or adrenergic receptors.1,2 In vivo, it is brain penetrant and has significant anxiolytic activity, without sedative, proconvulsant, or hyperphagic properties.1 SB-242084 has been used extensively in animal research to evaluate, for example, 5-HT2C receptor agonists and neurotransmitter receptor interactions in mice.3,4,5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Kennett, G.A., Wood, M.D., Bright, F., et al. SB 242084, a selective and brain penetrant 5-HT2C receptor antagonist. Neuropharmacology 36(4/5), 609-620 (1997).

    2. Bromidge, S.M., Duckworth, M., Forbes, I.T., 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. 40(22), 3494-3496 (1997).

    3. Fletcher, P.J., Tampakeras, M., Sinyard, J., et al. Characterizing the effects of 5-HT2C receptor ligands on motor activity and feeding behaviour in 5-HT2C receptor knockout mice. Neuropharmacology 57(3), 259-267 (2009).

    4. Fletcher, P.J., Sinyard, J., and Higgins, G.A. The effects of the 5-HT2C receptor antagonist SB242084 on locomotor activity induced by selective, or mixed, indirect serotonergic and dopaminergic agonists. Psychopharmacology 187(4), 515-525 (2006).

    5. Dalton, G.L., Lee, M.D., Kennett, G.A., et al. Serotonin 1B and 2C receptor interactions in the modulation of feeding behaviour in the mouse. Psychopharmacology 185(1), 45-47 (2006).

    Product Citations

    Chen, J., Garcia, E.J., Merritt, C.R., et al. Discovery of novel oleamide analogues as brain-penetrant positive allosteric serotonin 5-HT2C receptor and dual 5-HT2C/5-HT2A receptor modulators. J. Med. Chem. 66(14), 9992-10009 (2023).