Chemistry:GS-39783

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Short description: Chemical compound
GS-39783
GS-39783 structure.png
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
Chemical and physical data
FormulaC15H23N5O2S
Molar mass337.44 g·mol−1
3D model (JSmol)
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GS-39783 is a compound used in scientific research which acts as a positive allosteric modulator at the GABAB receptor.[1][2] It has been shown to produce anxiolytic effects in animal studies,[3][4][5] and reduces self-administration of alcohol,[6][7] cocaine[8][9][10] and nicotine.[11]

References

  1. ↑ "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". The Journal of Pharmacology and Experimental Therapeutics 307 (1): 322–30. October 2003. doi:10.1124/jpet.103.053074. PMID 12954816. 
  2. ↑ "Syntheses and optimization of new GS39783 analogues as positive allosteric modulators of GABA B receptors". Bioorganic & Medicinal Chemistry Letters 17 (22): 6206–11. November 2007. doi:10.1016/j.bmcl.2007.09.023. PMID 17884493. 
  3. ↑ "Genetic and pharmacological evidence of a role for GABA(B) receptors in the modulation of anxiety- and antidepressant-like behavior". Neuropsychopharmacology 29 (6): 1050–62. June 2004. doi:10.1038/sj.npp.1300413. PMID 15039762. 
  4. ↑ "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 benzodiazepines". The Journal of Pharmacology and Experimental Therapeutics 310 (3): 952–63. September 2004. doi:10.1124/jpet.104.066753. PMID 15113848. 
  5. ↑ "Evaluation of the anxiolytic-like profile of the GABAB receptor positive modulator CGP7930 in rodents". Neuropharmacology 54 (5): 854–62. April 2008. doi:10.1016/j.neuropharm.2008.01.004. PMID 18328507. 
  6. ↑ "Reducing effect of the positive allosteric modulators of the GABA(B) receptor, CGP7930 and GS39783, on alcohol intake in alcohol-preferring rats". European Journal of Pharmacology 525 (1–3): 105–11. November 2005. doi:10.1016/j.ejphar.2005.10.005. PMID 16289452. 
  7. ↑ "Reducing effect of the positive allosteric modulator of the GABA(B) receptor, GS39,783, on alcohol self-administration in alcohol-preferring rats". Psychopharmacology 193 (2): 171–8. August 2007. doi:10.1007/s00213-007-0776-1. PMID 17393141. 
  8. ↑ "Effects of positive allosteric modulators of the GABAB receptor on cocaine self-administration in rats". Psychopharmacology 173 (1–2): 105–11. April 2004. doi:10.1007/s00213-003-1706-5. PMID 14712341. 
  9. ↑ "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". Neuropsychopharmacology 30 (11): 2065–72. November 2005. doi:10.1038/sj.npp.1300734. PMID 15841108. 
  10. ↑ "GABA(B) receptor-positive modulation decreases selective molecular and behavioral effects of cocaine". Neuropsychopharmacology 32 (2): 388–98. February 2007. doi:10.1038/sj.npp.1301102. PMID 16710312. 
  11. ↑ "Positive modulation of GABA(B) receptors decreased nicotine self-administration and counteracted nicotine-induced enhancement of brain reward function in rats". The Journal of Pharmacology and Experimental Therapeutics 326 (1): 306–14. July 2008. doi:10.1124/jpet.108.139204. PMID 18445779. 

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See also
Receptor/signaling modulators
GABAA receptor positive modulators
GABA metabolism/transport modulators

}}



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