GS-39783

GS-39783 is a positive allosteric modulator of GABAB receptors that potentiates GABA-stimulated [35S]GTPgammaS binding to recombinant human GABAB receptors and rat cortical membranes (EC50s = 2.1 and 3.1 µM, respectively). 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. It reduces amphetamine- or MK-801-induced hyperactivity in rats and the number of DOI-induced head twitches in mice, indicating antipsychotic-like activity. GS-39783 also reduces the incidence of sound-induced tonic convulsions in juvenile mice (ED50 = 55.38 mg/kg).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: DMSO: soluble, Ethanol: soluble. lambdamax: 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.