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Submit ReviewGS 39783
Description: Positive allosteric modulator of GABAB receptors
Chemical Name: N,N'-Dicyclopentyl-2-(methylthio)-5-nitro-4,6-pyrimidinediamine
Purity: ≥98% (HPLC)
Biological Activity for GS 39783
GS 39783 is a positive 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.
Technical Data for GS 39783
| M. Wt | 337.44 |
| Formula | C15H23N5O2S |
| Storage | Store at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 39069-52-8 |
| PubChem ID | 6604928 |
| InChI Key | GSGVDKOCBKBMGG-UHFFFAOYSA-N |
| Smiles | CSC1=NC(NC2CCCC2)=C(C(NC2CCCC2)=N1)[N+]([O-])=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for GS 39783
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| ethanol | 1.69 | 5 | |
| DMSO | 3.37 | 10 |
Preparing Stock Solutions for GS 39783
The following data is based on the product molecular weight 337.44. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 29.63 mL | 148.17 mL | 296.35 mL |
| 0.5 mM | 5.93 mL | 29.63 mL | 59.27 mL |
| 1 mM | 2.96 mL | 14.82 mL | 29.63 mL |
| 5 mM | 0.59 mL | 2.96 mL | 5.93 mL |
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Product Datasheets for GS 39783
References for GS 39783
References are publications that support the biological activity of the product.
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
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 bac. or benzo J.Pharmacol.Exp.Ther. 310 952 PMID: 15113848
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
Pizzo et al (2018) Elucidation of the neural circuits activated by a GABAB receptor positive modulator: Relevance to anxiety. Neuropharmacology 136 129 PMID: 28734870
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Keywords: GS 39783, GS 39783 supplier, Positive, modulators, GABAB, receptors, GS39783, PAM, Receptors, 2001, Tocris Bioscience
2 Citations for GS 39783
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? Please let us know.
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
GABA Receptors Scientific Review
Written by Ian Martin, Norman Bowery and Susan Dunn, this review provides a history of the GABA receptor, as well as discussing the structure and function of the various subtypes and the clinical potential of receptor modulators; compounds available from Tocris are listed.
Addiction Poster
The key feature of drug addiction is the inability to stop using a drug despite clear evidence of harm. This poster describes the brain circuits associated with addiction, and provides an overview of the main classes of addictive drugs and the neurotransmitter systems that they target.