A 5-HT6 receptor antagonist
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MS 245 (oxalate)

Item No. 11936

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-methoxy-N,N-dimethyl-1-(phenylsulfonyl)-1H-indole-3-ethanamine, monoethanedioate
CAS Number
275363-58-1
Molecular Formula
C19H22N2O3S • C2H2O4
Formula Weight
448.5
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: soluble
λmax
212, 217, 259 nm
SMILES
COC1=CC=C(N(S(C2=CC=CC=C2)(=O)=O)C=C3CCN(C)C)C3=C1.OC(C(O)=O)=O
InChi Code
InChI=1S/C19H22N2O3S.C2H2O4/c1-20(2)12-11-15-14-21(19-10-9-16(24-3)13-18(15)19)25(22,23)17-7-5-4-6-8-17;3-1(4)2(5)6/h4-10,13-14H,11-12H2,1-3H3;(H,3,4)(H,5,6)
InChi Key
BLSWAEGCRSFTJG-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

    $41

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    5 mg

    $157

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    10 mg

    $235

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    Product Description

    MS 245 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT6 (Ki = 2.3 nM for the human recombinant receptor).1 It is selective for 5-HT6 over 5-HT2A and 5-HT2C receptors (Kis = 130 and 23 nM, respectively), as well as 5-HT1A, 5-HT1B, 5-HT1E, 5-HT3, and 5-HT7 receptors (Kis = 720, 9,200, 4,220, 2,390, and 600 nM, respectively). MS 245 decreases cAMP production induced by 5-HT in HEK293 cells expressing 5-HT6 (pA2 = 8.88 nM). It potentiates drug discrimination induced by (+)-amphetamine, but has no effect on cocaine or (–)-nicotine (Item No. 20887) drug discrimination in rats when administered at a dose of 5 mg/kg.2,3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Tsai, Y., Dukat, M., Slassi, A., et al. N1-(Benzenesulfonyl)tryptamines as novel 5-HT6 antagonists. Bioorg. Med. Chem. Lett. 10(20), 2295-2299 (2000).

    2. Pullagurla, M., Bondareva, T., Young, R., et al. Modulation of the stimulus effects of (+)amphetamine by the 5-HT6 antagonist MS-245. Pharmacol. Biochem. Behav. 78(2), 263-268 (2004).

    3. Young, R., Bondareva, T., Wesolowska, A., et al. Effect of the 5-HT6 serotonin antagonist MS-245 on the actions of (−)nicotine. Pharmacol. Biochem. Behav. 85(1), 170-177 (2006).