A positive allosteric modulator of GABAB receptors
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GS-39783

Item No. 29482

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N4,N6-dicyclopentyl-2-(methylthio)-5-nitro-4,6-pyrimidinediamine
CAS Number
39069-52-8
Molecular Formula
C15H23N5O2S
Formula Weight
337.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: solubleEthanol: soluble
λmax
220, 358 nm
SMILES
CSC1=NC(NC2CCCC2)=C([N+]([O-])=O)C(NC3CCCC3)=N1
InChi Code
InChI=1S/C15H23N5O2S/c1-23-15-18-13(16-10-6-2-3-7-10)12(20(21)22)14(19-15)17-11-8-4-5-9-11/h10-11H,2-9H2,1H3,(H2,16,17,18,19)
InChi Key
GSGVDKOCBKBMGG-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $75

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    10 mg

    $134

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    25 mg

    $315

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    50 mg

    $589

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    Product Description

    GS-39783 is a positive allosteric modulator of GABAB receptors that potentiates GABA-stimulated [35S]GTPγS binding to recombinant human GABAB receptors and rat cortical membranes (EC50s = 2.1 and 3.1 μM, respectively).1 It amplifies GABAB receptor-mediated transient calcium signaling in HEK293 cells expressing human receptors (EC50 = 2.4 μM). GS-39783 (25-100 mg/kg) suppresses alcohol self-administration, but has no effect on lever-responding for food, in Indiana alcohol-preferring, Sardinian alcohol-preferring, and Alko Alcohol rats.2 It reduces amphetamine- or MK-801-induced hyperactivity in rats and the number of DOI-induced head twitches in mice, indicating antipsychotic-like activity.3 GS-39783 also reduces the incidence of sound-induced tonic convulsions in juvenile mice (ED50 = 55.38 mg/kg).4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Urwyler, S., Pozza, M.F., Lingenhoehl, K., et al. N,N'-Dicyclopentyl-2-methylsulfanyl-5-nitro-pyrimidine-4,6-diamine (GS39783) and structurally related compounds: novel allosteric enhancers of γ-aminobutyric acidB receptor function. J. Pharmacol. Exp. Ther. 307(1), 322-330 (2003).

    2. Maccioni, P., Zaru, A., Loi, B., et al. Comparison of the effect of the GABAΒ receptor agonist, baclofen, and the positive allosteric modulator of the GABAB receptor, GS39783, on alcohol self-administration in 3 different lines of alcohol-preferring rats. Alcohol Clin. Exp. Res. 36(10), 1748-1766 (2012).

    3. Wierońska, J.M., Kusek, M., Tokarski, K., et al. The GABAB receptor agonist CGP44532 and the positive modulator GS39783 reverse some behavioural changes related to positive syndromes of psychosis in mice. Br. J. Pharmacol. 163(5), 1034-1047 (2011).

    4. Brown, J.W., Moeller, A., Schmidt, M., et al. Anticonvulsant effects of structurally diverse GABAB positive allosteric modulators in the DBA/2J audiogenic seizure test: Comparison to baclofen and utility as a pharmacodynamic screening model. Neuropharmacology 101, 358-369 (2016).