GS-39783 explained

GS-39783 is a compound used in scientific research which acts as a positive allosteric modulator at the GABA_B 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]

Notes and References

1. Urwyler S, Pozza MF, Lingenhoehl K, Mosbacher J, Lampert C, Froestl W, Koller M, Kaupmann K . 6 . 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 . 12954816 . 10.1124/jpet.103.053074 .
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 & Medicinal Chemistry Letters . 17 . 22 . 6206–11 . November 2007 . 17884493 . 2278029 . 10.1016/j.bmcl.2007.09.023 .
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 . 29 . 6 . 1050–62 . June 2004 . 15039762 . 10.1038/sj.npp.1300413 . free .
4. Cryan JF, Kelly PH, Chaperon F, Gentsch C, Mombereau C, Lingenhoehl K, Froestl W, Bettler B, Kaupmann K, Spooren WP . 6 . 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 . 15113848 . 10.1124/jpet.104.066753 .
5. Jacobson LH, Cryan JF . Evaluation of the anxiolytic-like profile of the GABAB receptor positive modulator CGP7930 in rodents . Neuropharmacology . 54 . 5 . 854–62 . April 2008 . 18328507 . 10.1016/j.neuropharm.2008.01.004 .
6. Orrù A, Lai P, Lobina C, Maccioni P, Piras P, Scanu L, Froestl W, Gessa GL, Carai MA, Colombo G . 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 . 16289452 . 10.1016/j.ejphar.2005.10.005 .
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 . 193 . 2 . 171–8 . August 2007 . 17393141 . 10.1007/s00213-007-0776-1 .
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 . 173 . 1–2 . 105–11 . April 2004 . 14712341 . 10.1007/s00213-003-1706-5 .
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 . 30 . 11 . 2065–72 . November 2005 . 15841108 . 10.1038/sj.npp.1300734 . free .
10. Lhuillier L, Mombereau C, Cryan JF, Kaupmann K . GABA(B) receptor-positive modulation decreases selective molecular and behavioral effects of cocaine . Neuropsychopharmacology . 32 . 2 . 388–98 . February 2007 . 16710312 . 1774586 . 10.1038/sj.npp.1301102 .
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 . The Journal of Pharmacology and Experimental Therapeutics . 326 . 1 . 306–14 . July 2008 . 18445779 . 2574924 . 10.1124/jpet.108.139204 .