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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.

J Pharmacol Exp Ther. 2004 Sep;310(3):952-63. Epub 2004 Apr 27.


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.


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.

J Pharmacol Exp Ther. 2003 Oct;307(1):322-30. Epub 2003 Sep 3.


Specific reduction of alcohol's motivational properties by the positive allosteric modulator of the GABAB receptor, GS39783--comparison with the effect of the GABAB receptor direct agonist, baclofen.

Maccioni P, Fantini N, Froestl W, Carai MA, Gessa GL, Colombo G.

Alcohol Clin Exp Res. 2008 Sep;32(9):1558-64. doi: 10.1111/j.1530-0277.2008.00725.x. Epub 2008 Jul 9.


In vitro and in vivo characterization of the novel GABAB receptor positive allosteric modulator, 2-{1-[2-(4-chlorophenyl)-5-methylpyrazolo[1,5-a]pyrimidin-7-yl]-2-piperidinyl}ethanol (CMPPE).

Perdona' E, Costantini VJ, Tessari M, Martinelli P, Carignani C, Valerio E, Mok MH, Zonzini L, Visentini F, Gianotti M, Gordon L, Rocheville M, Corsi M, Capelli AM.

Neuropharmacology. 2011 Oct-Nov;61(5-6):957-66. doi: 10.1016/j.neuropharm.2011.06.024. Epub 2011 Jul 5.


The positive allosteric modulator GS39783 enhances GABA(B) receptor-mediated inhibition of cyclic AMP formation in rat striatum in vivo.

Gjoni T, Desrayaud S, Imobersteg S, Urwyler S.

J Neurochem. 2006 Mar;96(5):1416-22. Epub 2006 Jan 25.


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.


Anxiolytic-like effects of the corticotropin-releasing factor1 (CRF1) antagonist DMP904 [4-(3-pentylamino)-2,7-dimethyl-8-(2-methyl-4-methoxyphenyl)-pyrazolo-[1,5-a]-pyrimidine] administered acutely or chronically at doses occupying central CRF1 receptors in rats.

Lelas S, Wong H, Li YW, Heman KL, Ward KA, Zeller KL, Sieracki KK, Polino JL, Godonis HE, Ren SX, Yan XX, Arneric SP, Robertson DW, Hartig PR, Grossman S, Trainor GL, Taub RA, Zaczek R, Gilligan PJ, McElroy JF.

J Pharmacol Exp Ther. 2004 Apr;309(1):293-302. Epub 2004 Jan 23.


Baclofen, a selective GABAB receptor agonist, dose-dependently impairs spatial learning in rats.

McNamara RK, Skelton RW.

Pharmacol Biochem Behav. 1996 Feb;53(2):303-8.


Reducing effect of the positive allosteric modulators of the GABA(B) receptor, CGP7930 and GS39783, on alcohol intake in alcohol-preferring rats.

Orrù A, Lai P, Lobina C, Maccioni P, Piras P, Scanu L, Froestl W, Gessa GL, Carai MA, Colombo G.

Eur J Pharmacol. 2005 Nov 21;525(1-3):105-11. Epub 2005 Nov 14.


Comparison of the effects of the GABAB receptor positive modulator BHF177 and the GABAB receptor agonist baclofen on anxiety-like behavior, learning, and memory in mice.

Li X, Risbrough VB, Cates-Gatto C, Kaczanowska K, Finn MG, Roberts AJ, Markou A.

Neuropharmacology. 2013 Jul;70:156-67. doi: 10.1016/j.neuropharm.2013.01.018. Epub 2013 Jan 29.


GABAB1 receptor subunit isoforms exert a differential influence on baseline but not GABAB receptor agonist-induced changes in mice.

Jacobson LH, Bettler B, Kaupmann K, Cryan JF.

J Pharmacol Exp Ther. 2006 Dec;319(3):1317-26. Epub 2006 Sep 21.


Modification of d-amphetamine-induced responses by baclofen in rats.

Phillis BD, Ong J, White JM, Bonnielle C.

Psychopharmacology (Berl). 2001 Jan;153(3):277-84.


Positive allosteric modulators at GABAB receptors exert intrinsic actions and enhance the influence of baclofen on light-induced phase shifts of hamster circadian activity rhythms.

Gannon RL, Millan MJ.

Pharmacol Biochem Behav. 2011 Oct;99(4):712-7. doi: 10.1016/j.pbb.2011.06.029. Epub 2011 Jul 6.


The GABA-B positive modulator GS39783 decreases psychostimulant conditioned-reinforcement and conditioned-reward.

Halbout B, Quarta D, Valerio E, Heidbreder CA, Hutcheson DM.

Addict Biol. 2011 Jul;16(3):416-27. doi: 10.1111/j.1369-1600.2010.00278.x. Epub 2011 Feb 11.


Annomontine, an alkaloid isolated from Annona purpurea, has anxiolytic-like effects in the elevated plus-maze.

Rejón-Orantes Jdel C, González-Esquinca AR, de la Mora MP, Roldan Roldan G, Cortes D.

Planta Med. 2011 Mar;77(4):322-7. doi: 10.1055/s-0030-1250406. Epub 2010 Oct 1.


Genetic and pharmacological evidence of a role for GABA(B) receptors in the modulation of anxiety- and antidepressant-like behavior.

Mombereau C, Kaupmann K, Froestl W, Sansig G, van der Putten H, Cryan JF.

Neuropsychopharmacology. 2004 Jun;29(6):1050-62.


Characterization of (R,S)-5,7-di-tert-butyl-3-hydroxy-3-trifluoromethyl-3H-benzofuran-2-one as a positive allosteric modulator of GABAB receptors.

Malherbe P, Masciadri R, Norcross RD, Knoflach F, Kratzeisen C, Zenner MT, Kolb Y, Marcuz A, Huwyler J, Nakagawa T, Porter RH, Thomas AW, Wettstein JG, Sleight AJ, Spooren W, Prinssen EP.

Br J Pharmacol. 2008 Jun;154(4):797-811. doi: 10.1038/bjp.2008.135. Epub 2008 Apr 21.

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