Cat. No. 2001
Chemical Name: N,N'-Dicyclopentyl-2-(methylthio)-5-
Biological ActivityPositive allosteric modulator of GABAB receptor function. Potentiates the effects of GABA on [35S]GTPγS binding at recombinant and native GABAB receptors (EC50 values are 2.1 and 3.1μM respectively). Decreases cocaine self-administration, blocks the rewarding properties of nicotine and produces anxiolytic-like activity without the side effects associated with baclofen or benzodiazepines.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Data Sheet
Mombereau et al (2007) GABAB receptor-positive modulation-induced blockade of the rewarding effects of nicotine is associated with a reduction in nucleus accumbens ΔFosB accumulation. J.Pharmacol.Exp.Ther. 321 172. PMID: 17215447.
Cryan et al (2004) Behavioral characterization of the novel GABAB receptor-positive modulator GS39783 (N,N'-dicyclopentyl-2-methylsulfanyl-5-nitro-pyrimidine-4,6-diamine: anxiolytic-like activity without side effects associated with baclofen or benzodiazepines. J.Pharmacol.Exp.Ther. 310 952. PMID: 15113848.
Urwyler et al (2003) 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. 307 322. PMID: 12954816.
If you know of a relevant reference for this product please let us know.
Citations are publications that use Tocris products. Selected citations for GS 39783 include:
Zhang et al (2015) GABAB receptor upregulates fragile X mental retardation protein expression in neurons. Sci Rep 5 10468. PMID: 26020477.
Pacey et al (2011) Subchronic administration and combination metabotropic glutamate and GABAB receptor drug therapy in fragile X syndrome. Sci Rep 338 897. PMID: 21636656.
Do you know of a great paper that uses GS 39783 from Tocris? If so please let us know.
View Related Products by Product Action
Keywords: GS 39783, supplier, Positive, modulators, GABAB, receptors, GS39783, Tocris Bioscience, GABAB Receptor Modulator products
Find multiple products by catalog number
New Products in this Area
Selective GPR84 agonistIHR-Cy3
Potent fluorescent Smo antagonistRo 6842262
Potent LPA1 antagonistAMG 853
Potent dual CRTH2 and prostaglandin D2 (PGD2) receptor antagonistAM 4668
Potent FFA1 (GPR40) agonistCATPB
FFA2 antagonist/inverse agonistOleanolic acid
Selective GPBA receptor (TGR5) partial agonistPPTN hydrochloride
High affinity and selective P2Y14 antagonistItraconazole
SMO antagonist; acts at different binding site to cyclopamine (Cat No. 1623)SAR 216471 hydrochloride
Potent P2Y12 antagonist; orally available
Follow Tocris on LinkedIn
Visit our LinkedIn page for the latest Tocris news, events and updates.