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Gs-39783

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Title: Gs-39783  
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Subject: N4-Chloroacetylcytosine arabinoside, GABA transaminase inhibitor, (1,2,5,6-Tetrahydropyridin-4-yl)methylphosphinic acid, Pharmacology, Phaclofen
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Gs-39783

GS-39783
Systematic (IUPAC) name
N,N-Dicyclopentyl-2-methylsulfanyl-5-nitropyrimidine-4,6-diamine
Clinical data
Legal status
?
Identifiers
CAS number
ATC code ?
PubChem
Chemical data
Formula C15H23N5O2S 
Mol. mass 337.440 g/mol
 YesY   

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 ethanol,[6][7] cocaine [8][9][10] and nicotine.[11]

References

  1. ^ Urwyler S, Pozza MF, Lingenhoehl K, Mosbacher J, Lampert C, Froestl W, Koller M, Kaupmann K. 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. Journal of Pharmacology and Experimental Therapeutics. 2003 Oct;307(1):322-30. doi:10.1124/jpet.103.053074 PMID 12954816
  2. ^ Guery S, Floersheim P, Kaupmann K, Froestl W. Syntheses and optimization of new GS39783 analogues as positive allosteric modulators of GABA B receptors. Bioorganic and Medicinal Chemistry Letters. 2007 Nov 15;17(22):6206-11. doi:10.1016/j.bmcl.2007.09.023 PMID 17884493
  3. ^ Mombereau C, Kaupmann K, Froestl W, Sansig G, van der Putten H, Cryan JF. Genetic and pharmacological evidence of a role for GABA(B) receptors in the modulation of anxiety- and antidepressant-like behavior. Neuropsychopharmacology. 2004 Jun;29(6):1050-62. PMID 15039762
  4. ^ Cryan JF, Kelly PH, Chaperon F, Gentsch C, Mombereau C, Lingenhoehl K, Froestl W, Bettler B, Kaupmann K, Spooren WP. 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. Journal of Pharmacology and Experimental Therapeutics. 2004 Sep;310(3):952-63. PMID 15113848
  5. ^ Jacobson LH, Cryan JF. Evaluation of the anxiolytic-like profile of the GABAB receptor positive modulator CGP7930 in rodents. Neuropharmacology. 2008 Apr;54(5):854-62. PMID 18328507
  6. ^ Orrù A, Lai P, Lobina C, Maccioni P, Piras P, Scanu L, Froestl W, Gessa GL, Carai MA, Colombo G. 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. 2005 Nov 21;525(1-3):105-11. PMID 16289452
  7. ^ Maccioni P, Pes D, Orrù A, Froestl W, Gessa GL, Carai MA, Colombo G. 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 Aug;193(2):171-8. PMID 17393141
  8. ^ Smith MA, Yancey DL, Morgan D, Liu Y, Froestl W, Roberts DC. Effects of positive allosteric modulators of the GABAB receptor on cocaine self-administration in rats. Psychopharmacology (Berlin). 2004 Apr;173(1-2):105-11. PMID 14712341
  9. ^ Slattery DA, Markou A, Froestl W, Cryan JF. 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. 2005 Nov;30(11):2065-72. PMID 15841108
  10. ^ Lhuillier L, Mombereau C, Cryan JF, Kaupmann K. GABA(B) receptor-positive modulation decreases selective molecular and behavioral effects of cocaine. Neuropsychopharmacology. 2007 Feb;32(2):388-98. PMID 16710312
  11. ^ Paterson NE, Vlachou S, Guery S, Kaupmann K, Froestl W, Markou A. Positive modulation of GABA(B) receptors decreased nicotine self-administration and counteracted nicotine-induced enhancement of brain reward function in rats. Journal of Pharmacology and Experimental Therapeutics. 2008 Jul;326(1):306-14. doi:10.1124/jpet.108.139204 PMID 18445779
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