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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.
Urwyler S, Pozza MF, Lingenhoehl K, Mosbacher J, Lampert C, Froestl W, Koller M, Kaupmann K. Urwyler S, et al. Among authors: froestl w. J Pharmacol Exp Ther. 2003 Oct;307(1):322-30. doi: 10.1124/jpet.103.053074. Epub 2003 Sep 3. J Pharmacol Exp Ther. 2003. PMID: 12954816
SGS742: the first GABA(B) receptor antagonist in clinical trials.
Froestl W, Gallagher M, Jenkins H, Madrid A, Melcher T, Teichman S, Mondadori CG, Pearlman R. Froestl W, et al. Biochem Pharmacol. 2004 Oct 15;68(8):1479-87. doi: 10.1016/j.bcp.2004.07.030. Biochem Pharmacol. 2004. PMID: 15451390 Clinical Trial.
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.
Cryan JF, Kelly PH, Chaperon F, Gentsch C, Mombereau C, Lingenhoehl K, Froestl W, Bettler B, Kaupmann K, Spooren WP. Cryan JF, et al. Among authors: froestl w. J Pharmacol Exp Ther. 2004 Sep;310(3):952-63. doi: 10.1124/jpet.104.066753. Epub 2004 Apr 27. J Pharmacol Exp Ther. 2004. PMID: 15113848
Specific gamma-hydroxybutyrate-binding sites but loss of pharmacological effects of gamma-hydroxybutyrate in GABA(B)(1)-deficient mice.
Kaupmann K, Cryan JF, Wellendorph P, Mombereau C, Sansig G, Klebs K, Schmutz M, Froestl W, van der Putten H, Mosbacher J, Bräuner-Osborne H, Waldmeier P, Bettler B. Kaupmann K, et al. Among authors: froestl w. Eur J Neurosci. 2003 Nov;18(10):2722-30. doi: 10.1111/j.1460-9568.2003.03013.x. Eur J Neurosci. 2003. PMID: 14656321
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