A 5-HT2C receptor antagonist
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RS 102221 (hydrochloride)

Item No. 31543

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[5-[5-(2,4-dioxo-1,3,8-triazaspiro[4.5]dec-8-yl)-1-oxopentyl]-2,4-dimethoxyphenyl]-4-(trifluoromethyl)-benzenesulfonamide, monohydrochloride
CAS Number
187397-18-8
Molecular Formula
C27H31F3N4O7S • HCl
Formula Weight
649.1
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: 100 mM
SMILES
O=C(C1=CC(NS(=O)(C2=CC=C(C(F)(F)F)C=C2)=O)=C(C=C1OC)OC)CCCCN3CCC4(NC(NC4=O)=O)CC3.Cl
InChi Code
InChI=1S/C27H31F3N4O7S.ClH/c1-40-22-16-23(41-2)20(33-42(38,39)18-8-6-17(7-9-18)27(28,29)30)15-19(22)21(35)5-3-4-12-34-13-10-26(11-14-34)24(36)31-25(37)32-26;/h6-9,15-16,33H,3-5,10-14H2,1-2H3,(H2,31,32,36,37);1H
InChi Key
SZJZEJZLRDIHPB-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    500 µg

    $36

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    1 mg

    $68

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    5 mg

    $186

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    Product Description

    RS 102221 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT2C.1 It binds to 5-HT2C receptors (Ki = 3.8 nM for the recombinant human receptor) and is selective for 5-HT2C receptors over 5-HT2A and 5-HT2B receptors (Kis = 1,122.02 and 812.83 nM, respectively), as well as a panel of additional neurotransmitter receptors and ion channels (Kis = ≥316.23 nM for all). RS 102221 inhibits 5-HT-induced increases in the extracellular media acidification rate of CHO-K1 cells expressing human 5-HT2C receptors (pA2 = 8.1). It increases food intake and weight gain in rats when administered at a dose of 2 mg/kg. RS 102221 (2 mg/kg) increases the time spent in the light compartment in the light-dark exploration test in mice and reduces prepulse inhibition of the startle reflex when administered at a dose of 1 mg/kg.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Bonhaus, D.W., Weinhardt, K.K., Taylor, M., et al. RS-102221: A novel high affinity and selective, 5-HT2C receptor antagonist. Neuropharmacology 36(4-5), 621-629 (1997).

    2. Kuznetsova, E.G., Amstislavskaya, T.G., Shefer, E.A., et al. Effect of 5-HT2C receptor antagonist RS 102221 on mouse behavior. Bull. Exp. Biol. Med. 142(1), 76-79 (2006).