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GS 39783
- Moderately soluble in DMSO
- MF: C15H23N5O2S
- MW: 337.44
Description
GS 39783 is a positive allosteric modulator of the GABAB receptor that enhances receptor responses to endogenous GABA without acting as a direct orthosteric agonist.
GABAB receptors mediate slow inhibitory neurotransmission in the central nervous system and regulate neuronal excitability, synaptic release and behavioral responses. GS 39783 is useful for studying GABAB receptor allostery and CNS inhibitory signaling.
Key Features
- GABAB receptor positive allosteric modulator
- Enhances endogenous GABA-mediated receptor activation
- Useful for allosteric GPCR pharmacology
- Relevant to CNS inhibitory neurotransmission research
Applications
- GABAB receptor functional assays
- Allosteric modulator profiling
- Synaptic inhibition and neuronal excitability studies
- CNS pharmacology and behavioral pathway research
More Information
| Parent CAS No. | 39069-52-8 |
|---|---|
| Chemical Name | N4,N6-dicyclopentyl-2-(methylthio)-5-nitropyrimidine-4,6-diamine |
| SMILES | N1C(NC2CCCC2)=C([N+]([O-])=O)C(NC2CCCC2)=NC=1SC |
| MFCD | MFCD06201849 |
| InChi | 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) |
| InChiKey | GSGVDKOCBKBMGG-UHFFFAOYSA-N |
| CID | 6604928 |
| Short Description | GABA-B PAM |
References
- S Urwyler et al. N,N'-Dicyclopentyl-2-methylsulfanyl-5-nitro-pyrimidine-4,6-diamine (GS39783) and structurally related compounds: novel allosteric enhancers of gamma-aminobutyric acidB receptor function. J. Pharmacol. Exp. Ther. 2003, 307(1), 322-330.
- C Mombereau et al. Genetic and pharmacological evidence of a role for GABA(B) receptors in the modulation of anxiety- and antidepressant-like behavior. Neuropsychopharmacol. 2004, 29(6), 1050-1062.
- P Maccioni et al. Reducing effect of the positive allosteric modulator of the GABA(B) receptor, GS39,783, on alcohol self-administration in alcohol-preferring rats. Psychopharmacology (Berlin). 2007, 193(2), 171-178.
- NE Paterson et al. Positive modulation of GABA(B) receptors decreased nicotine self-administration and counteracted nicotine-induced enhancement of brain reward function in rats. J. Pharmacol. Exp. Ther. 2008, 326(1), 306-314.
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