GS 39783 - CAS 39069-52-8
Catalog number: 39069-52-8
Category: Inhibitor
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Molecular Weight:
GABA Receptor
GS 39783 is an allosteric positive modulator of GABAB receptors, decreases cocaine self-administration, blocks the rewarding properties of nicotine and produces anxiolytic-like activity without the side effects associated with baclofen or benzodiazepines.
Pale orange solid
GS39783; GS-39783; GS 39783; N,N'-Dicyclopentyl-2-(methylthio)-5-nitro-4,6-pyrimidinediamine;4-N,6-N-dicyclopentyl-2-methylsulfanyl-5-nitropyrimidine-4,6-diamine;
Soluble in DMSO
Store at -20 °C
Positive allosteric modulator of GABAB receptor function.
Quality Standard:
Enterprise standard
Shelf Life:
As supplied, 2 years from the QC date provided on the Certificate of Analysis, when stored properly.
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Current Developer:
Gilead Sciences
1.GABA(B) receptor-positive modulation decreases selective molecular and behavioral effects of cocaine.
Lhuillier L;Mombereau C;Cryan JF;Kaupmann K Neuropsychopharmacology. 2007 Feb;32(2):388-98. Epub 2006 May 17.
Exposure to cocaine induces selective behavioral and molecular adaptations. In rodents, acute cocaine induces increased locomotor activity, whereas prolonged drug exposure results in behavioral locomotor sensitization, which is thought to be a consequence of drug-induced neuroadaptive changes. Recent attention has been given to compounds activating GABA(B) receptors as potential antiaddictive therapies. In particular, the principle of allosteric positive GABA(B) receptor modulators is very promising in this respect, as positive modulators lack the sedative and muscle relaxant properties of full GABA(B) receptor agonists such as baclofen. Here, we investigated the effects of systemic application of the GABA(B) receptor-positive modulator GS39783 (N,N'-dicyclopentyl-2-methylsulfanyl-5-nitro-pyrimidine-4, 6-diamine) in animals treated with acute and chronic cocaine administration. Both GS39783 and baclofen dose dependently attenuated acute cocaine-induced hyperlocomotion. Furthermore, both compounds also efficiently blocked cocaine-induced Fos induction in the striatal complex. In chronic studies, GS39783 induced a modest attenuation of cocaine-induced locomotor sensitization. Chronic cocaine induces the accumulation of the transcription factor deltaFosB and upregulates cAMP-response-element-binding protein (CREB) and dopamine- and cAMP-regulated phosphoprotein of 32 kDa (DARPP-32).
2.The GABAB receptor-positive modulator GS39783 and the GABAB receptor agonist baclofen attenuate the reward-facilitating effects of cocaine: intracranial self-stimulation studies in the rat.
Slattery DA;Markou A;Froestl W;Cryan JF Neuropsychopharmacology. 2005 Nov;30(11):2065-72.
There is an increasing interest in the development of nondopaminergic pharmacotherapies for cocaine abuse. Emerging preclinical and clinical data with the metabotropic GABAB receptor agonist baclofen support a role for the modulation of GABAB receptors in the treatment of drug addiction. Nevertheless, the muscle relaxant, hypothermic, and sedative properties of baclofen somewhat limit its widespread potential therapeutic utility. Recently, positive modulators of the GABAB receptor such as GS39783 (N,N'-dicyclopentyl-2-methylsulfanyl-5-nitro-pyrimidine-4,6-diamine) have been identified. These positive modulators enhance the effects of GABA (gamma-aminobutyric acid) through actions at an allosteric site and are devoid of intrinsic agonistic efficacy. The aim of the present study was to assess the ability of the novel GABAB-positive modulator GS39873 or baclofen to modulate the behavioral effects of cocaine. Drugs of abuse such as cocaine lower brain reward thresholds obtained using intracranial self-stimulation (ICSS). We demonstrate here that GS39783 had no intrinsic effects on ICSS reward thresholds (10-100 mg/kg p.o.) in rats, whereas the full GABAB receptor agonist baclofen (2.5-5 mg/kg p.
3.Evaluation of the anxiolytic-like profile of the GABAB receptor positive modulator CGP7930 in rodents.
Jacobson LH;Cryan JF Neuropharmacology. 2008 Apr;54(5):854-62. doi: 10.1016/j.neuropharm.2008.01.004. Epub 2008 Jan 13.
There is a growing body of data to support the notion that GABA(B) receptors may be a therapeutic target for anxiety disorders. However, the application of GABA(B) receptor agonists in anxiety research and psychiatry is hampered by side effects that include motor in-coordination and hypothermia. Recently the GABA(B) receptor positive modulator GS39783 was shown to be anxiolytic in rodent models, but was devoid of accompanying side effects characteristic of full agonists. However, it is important to test whether such anxiolytic effects generalise to another chemical class of GABA(B) receptor positive modulators. We therefore aimed to investigate the anxiolytic and side-effect profile of CGP7930, the first-reported GABA(B) receptor positive modulator, in rodent models of anxiety, motor coordination and hypothermia. CGP7930 (3-300 mg/kg) showed a modest, compared to the benzodiazepine chlordiazepoxide (10mg/kg), dose-dependent anxiolytic profile in the mouse stress-induced hyperthermia (100mg/kg), staircase (100 and 300 mg/kg) and elevated zero maze tests (3-100mg/kg), but did not have any anxiolytic effects in the rat elevated plus maze. Similar to GS39783, CGP7930 also demonstrated a greatly reduced side-effect profile in comparison to the GABA(B) receptor full agonist baclofen in the mouse rotarod and traction wire tests and did not induce hypothermia.
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CAS 39069-52-8 GS 39783

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