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GS39783

Cat. No. M8564

All AbMole products are for research use only, cannot be used for human consumption.

GS39783 Structure

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Biological Activity

GS39783 is a positive allosteric modulator (PAM) of GABA-B receptors. GABAB receptor positive allosteric modulators have potential for treatment of many neuro-psychiatric disorders as well as drug dependence and seizures. The receptor is a GPCR expressed throughout the CNS; it acts as both an auto-receptor and heteroreceptor to modulate GABA release and regulate K+ channels and Ca++ channels. GS39783 has been shown to inhibit alcohol self-administration and to have an antipsychotic-like effect in animal models of addiction and schizophrenia, respectively.

Chemical Information
Molecular Weight 337.44
Formula C15H23N5O2S
CAS Number 39069-52-8
Solubility (25°C) DMSO: 5 mg/mL (warmed)
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Maria C Olianas, et al. The GABA B positive allosteric modulators CGP7930 and GS39783 stimulate ERK1/2 signalling in cells lacking functional GABA B receptors

[2] Lauren C Kruse, et al. Positive allosteric modulation of the GABA(B) receptor by GS39783 attenuates the locomotor stimulant actions of ethanol and potentiates the induction of locomotor sensitization

[3] Paola Maccioni, et al. Comparison of the effect of the GABAΒ receptor agonist, baclofen, and the positive allosteric modulator of the GABAB receptor, GS39783, on alcohol self-administration in 3 different lines of alcohol-preferring rats

[4] Briac Halbout, et al. The GABA-B positive modulator GS39783 decreases psychostimulant conditioned-reinforcement and conditioned-reward

[5] Delphine S Dupuis, et al. Point mutations in the transmembrane region of GABAB2 facilitate activation by the positive modulator N,N'-dicyclopentyl-2-methylsulfanyl-5-nitro-pyrimidine-4,6-diamine (GS39783) in the absence of the GABAB1 subunit

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Keywords: GS39783 supplier, inhibitors, activators

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