Biological Activity
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
| 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.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 3.37 | 10 | |
| ethanol | 1.69 | 5 |
Preparing Stock Solutions
The following data is based on the product molecular weight 337.44. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.96 mL | 14.82 mL | 29.63 mL |
| 5 mM | 0.59 mL | 2.96 mL | 5.93 mL |
| 10 mM | 0.3 mL | 1.48 mL | 2.96 mL |
| 50 mM | 0.06 mL | 0.3 mL | 0.59 mL |
Molarity Calculator
Reconstitution Calculator
Dilution Calculator
Product Datasheets
References
References are publications that support the products' biological activity.
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 baclofen 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
Keywords: GS 39783, supplier, Positive, modulators, GABAB, receptors, GS39783, GABAB, Receptors, GABAB, Receptors, Tocris Bioscience
