Published in J Pharmacol Exp Ther on September 03, 2003
Allosteric modulation of seven transmembrane spanning receptors: theory, practice, and opportunities for central nervous system drug discovery. J Med Chem (2012) 2.10
The heptahelical domain of GABA(B2) is activated directly by CGP7930, a positive allosteric modulator of the GABA(B) receptor. J Biol Chem (2004) 1.45
Positive modulation of GABA(B) receptors decreased nicotine self-administration and counteracted nicotine-induced enhancement of brain reward function in rats. J Pharmacol Exp Ther (2008) 1.08
Biphasic effects of cannabinoids in anxiety responses: CB1 and GABA(B) receptors in the balance of GABAergic and glutamatergic neurotransmission. Neuropsychopharmacology (2012) 1.05
Targeting opioid receptor heterodimers: strategies for screening and drug development. AAPS J (2006) 1.02
Effects of positive allosteric modulators of the GABAB receptor on cocaine self-administration in rats. Psychopharmacology (Berl) (2004) 1.02
Reducing effect of the positive allosteric modulator of the GABA(B) receptor, GS39,783, on alcohol self-administration in alcohol-preferring rats. Psychopharmacology (Berl) (2007) 1.00
Comparison of the effect of the GABAΒ receptor agonist, baclofen, and the positive allosteric modulator of the GABAB receptor, GS39783, on alcohol self-administration in 3 different lines of alcohol-preferring rats. Alcohol Clin Exp Res (2012) 0.98
Syntheses and optimization of new GS39783 analogues as positive allosteric modulators of GABA B receptors. Bioorg Med Chem Lett (2007) 0.98
Allosteric modulators of GABA(B) receptors: mechanism of action and therapeutic perspective. Curr Neuropharmacol (2007) 0.98
GABA(B) receptor-positive modulation decreases selective molecular and behavioral effects of cocaine. Neuropsychopharmacology (2006) 0.97
Alterations in the rate of binge ethanol consumption: implications for preclinical studies in mice. Addict Biol (2013) 0.96
Trans-activation between 7TM domains: implication in heterodimeric GABAB receptor activation. EMBO J (2010) 0.96
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. Br J Pharmacol (2008) 0.95
Repeated administration of the GABAB receptor positive modulator BHF177 decreased nicotine self-administration, and acute administration decreased cue-induced reinstatement of nicotine seeking in rats. Psychopharmacology (Berl) (2010) 0.92
Mechanism-based medication development for the treatment of nicotine dependence. Acta Pharmacol Sin (2009) 0.91
Differential sensitivity to the motor and hypothermic effects of the GABA B receptor agonist baclofen in various mouse strains. Psychopharmacology (Berl) (2005) 0.90
A Gut Feeling about GABA: Focus on GABA(B) Receptors. Front Pharmacol (2010) 0.89
Point mutations in the transmembrane region of GABAB2 facilitate activation by the positive modulator N,N'-dicyclopentyl-2-methylsulfanyl-5-nitro-pyrimidine-4,6-diamine (GS39783) in the absence of the GABAB1 subunit. Mol Pharmacol (2006) 0.87
Structure and ligand recognition of class C GPCRs. Acta Pharmacol Sin (2012) 0.86
GABA(B) receptor modulators potentiate baclofen-induced depression of dopamine neuron activity in the rat ventral tegmental area. Br J Pharmacol (2005) 0.86
GABAB receptor-positive modulators: enhancement of GABAB receptor agonist effects in vivo. J Pharmacol Exp Ther (2010) 0.84
Positive allosteric modulation of the GABA(B) receptor by GS39783 attenuates the locomotor stimulant actions of ethanol and potentiates the induction of locomotor sensitization. Alcohol (2012) 0.83
Both GABA(B) receptor activation and blockade exacerbated anhedonic aspects of nicotine withdrawal in rats. Eur J Pharmacol (2011) 0.82
Reduction by the Positive Allosteric Modulator of the GABA(B) Receptor, GS39783, of Alcohol Self-Administration in Sardinian Alcohol-Preferring Rats Exposed to the "Sipper" Procedure. Front Psychiatry (2010) 0.81
Operant, oral alcoholic beer self-administration by C57BL/6J mice: effect of BHF177, a positive allosteric modulator of GABA(B) receptors. Psychopharmacology (Berl) (2012) 0.80
Anxiety-like behaviors at the end of the nocturnal period in sP rats with a "history" of unpredictable, limited access to alcohol. Alcohol (2015) 0.79
GABAB receptor upregulates fragile X mental retardation protein expression in neurons. Sci Rep (2015) 0.78
Sleep-deprivation induces changes in GABA(B) and mGlu receptor expression and has consequences for synaptic long-term depression. PLoS One (2011) 0.78
Positive allosteric modulation of GABAB receptors ameliorates sensorimotor gating in rodent models. CNS Neurosci Ther (2014) 0.78
Effects of the GABAB receptor-positive modulators CGP7930 and rac-BHFF in baclofen- and γ-hydroxybutyrate-discriminating pigeons. J Pharmacol Exp Ther (2012) 0.77
Allosteric modulation of the M₃ muscarinic receptor by amiodarone and N-ethylamiodarone: application of the four-ligand allosteric two-state model. Mol Pharmacol (2011) 0.76
Discriminative stimulus effects of the GABAB receptor-positive modulator rac-BHFF: comparison with GABAB receptor agonists and drugs of abuse. J Pharmacol Exp Ther (2012) 0.76
Evaluation of peripheral versus central effects of GABA(B) receptor activation using a novel, positive allosteric modulator of the GABA(B) receptor ADX71943, a pharmacological tool compound with a fully peripheral activity profile. Br J Pharmacol (2014) 0.76
Discovery of a Negative Allosteric Modulator of GABAB Receptors. ACS Med Chem Lett (2014) 0.76
GABAB receptor allosteric modulators exhibit pathway-dependent and species-selective activity. Pharmacol Res Perspect (2017) 0.75
Ligand-guided homology modelling of the GABAB2 subunit of the GABAB receptor. PLoS One (2017) 0.75
KK-92A, a novel GABAB receptor positive allosteric modulator, attenuates nicotine self-administration and cue-induced nicotine seeking in rats. Psychopharmacology (Berl) (2017) 0.75
Suppressing effect of COR659 on alcohol, sucrose, and chocolate self-administration in rats: involvement of the GABAB and cannabinoid CB1 receptors. Psychopharmacology (Berl) (2017) 0.75
ANKTM1, a TRP-like channel expressed in nociceptive neurons, is activated by cold temperatures. Cell (2003) 10.94
Role of NMDA receptor subtypes in governing the direction of hippocampal synaptic plasticity. Science (2004) 5.76
Molecular structure and physiological functions of GABA(B) receptors. Physiol Rev (2004) 3.53
Immunodeficiency at the start of combination antiretroviral therapy in low-, middle-, and high-income countries. J Acquir Immune Defic Syndr (2014) 2.79
Differential compartmentalization and distinct functions of GABAB receptor variants. Neuron (2006) 2.53
Nogo-A inhibits neurite outgrowth and cell spreading with three discrete regions. J Neurosci (2003) 2.03
Metabotropic glutamate 2/3 receptors in the ventral tegmental area and the nucleus accumbens shell are involved in behaviors relating to nicotine dependence. J Neurosci (2007) 1.85
Don't worry 'B' happy!: a role for GABA(B) receptors in anxiety and depression. Trends Pharmacol Sci (2005) 1.84
5-Phosphonomethylquinoxalinediones as competitive NMDA receptor antagonists with a preference for the human 1A/2A, rather than 1A/2B receptor composition. Bioorg Med Chem Lett (2002) 1.79
Generalization of amygdala LTP and conditioned fear in the absence of presynaptic inhibition. Nat Neurosci (2006) 1.78
Genetic and pharmacological evidence of a role for GABA(B) receptors in the modulation of anxiety- and antidepressant-like behavior. Neuropsychopharmacology (2004) 1.72
Redistribution of GABAB(1) protein and atypical GABAB responses in GABAB(2)-deficient mice. J Neurosci (2004) 1.66
LRRK2 protein levels are determined by kinase function and are crucial for kidney and lung homeostasis in mice. Hum Mol Genet (2011) 1.52
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. J Pharmacol Exp Ther (2004) 1.45
Specific gamma-hydroxybutyrate-binding sites but loss of pharmacological effects of gamma-hydroxybutyrate in GABA(B)(1)-deficient mice. Eur J Neurosci (2003) 1.34
The GABAB receptor agonists baclofen and CGP44532 decreased nicotine self-administration in the rat. Psychopharmacology (Berl) (2003) 1.28
Repeated administration of the GABAB receptor agonist CGP44532 decreased nicotine self-administration, and acute administration decreased cue-induced reinstatement of nicotine-seeking in rats. Neuropsychopharmacology (2005) 1.18
Therapeutic intervention in mice deficient for succinate semialdehyde dehydrogenase (gamma-hydroxybutyric aciduria). J Pharmacol Exp Ther (2002) 1.13
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. Alcohol Clin Exp Res (2008) 1.09
Reduction of alcohol's reinforcing and motivational properties by the positive allosteric modulator of the GABA(B) receptor, BHF177, in alcohol-preferring rats. Alcohol Clin Exp Res (2009) 1.08
Positive modulation of GABA(B) receptors decreased nicotine self-administration and counteracted nicotine-induced enhancement of brain reward function in rats. J Pharmacol Exp Ther (2008) 1.08
GABA(B(1)) receptor isoforms differentially mediate the acquisition and extinction of aversive taste memories. J Neurosci (2006) 1.05
Altered anxiety and depression-related behaviour in mice lacking GABAB(2) receptor subunits. Neuroreport (2005) 1.05
The selective nicotinic acetylcholine receptor alpha7 agonist JN403 is active in animal models of cognition, sensory gating, epilepsy and pain. Neuropharmacology (2008) 1.04
Characterizing human ion channels in induced pluripotent stem cell-derived neurons. J Biomol Screen (2012) 1.04
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) 1.02
Effects of positive allosteric modulators of the GABAB receptor on cocaine self-administration in rats. Psychopharmacology (Berl) (2004) 1.02
The GABA(B) receptor agonists baclofen and CGP 44532 prevent acquisition of alcohol drinking behaviour in alcohol-preferring rats. Alcohol Alcohol (2002) 1.01
Reducing effect of the positive allosteric modulator of the GABA(B) receptor, GS39,783, on alcohol self-administration in alcohol-preferring rats. Psychopharmacology (Berl) (2007) 1.00
Behavioral evaluation of mice deficient in GABA(B(1)) receptor isoforms in tests of unconditioned anxiety. Psychopharmacology (Berl) (2006) 0.99
A screen for enhancers of clearance identifies huntingtin as a heat shock protein 90 (Hsp90) client protein. J Biol Chem (2011) 0.98
Syntheses and optimization of new GS39783 analogues as positive allosteric modulators of GABA B receptors. Bioorg Med Chem Lett (2007) 0.98
Specific roles of GABA(B(1)) receptor isoforms in cognition. Behav Brain Res (2007) 0.98
Reducing effect of the positive allosteric modulators of the GABA(B) receptor, CGP7930 and GS39783, on alcohol intake in alcohol-preferring rats. Eur J Pharmacol (2005) 0.97
The anticonvulsant gabapentin (neurontin) does not act through gamma-aminobutyric acid-B receptors. Mol Pharmacol (2002) 0.97
GABA(B) receptor-positive modulation decreases selective molecular and behavioral effects of cocaine. Neuropsychopharmacology (2006) 0.97
Attenuation of cocaine-seeking by GABA B receptor agonists baclofen and CGP44532 but not the GABA reuptake inhibitor tiagabine in baboons. Drug Alcohol Depend (2007) 0.97
The RXR-type endoplasmic reticulum-retention/retrieval signal of GABAB1 requires distant spacing from the membrane to function. Mol Pharmacol (2005) 0.96
Effects of GABAergic modulators on food and cocaine self-administration in baboons. Drug Alcohol Depend (2005) 0.93
Roles of GABAB receptor subtypes in presynaptic auto- and heteroreceptor function regulating GABA and glutamate release. J Neural Transm (Vienna) (2008) 0.93
GABAB receptor-positive modulation-induced blockade of the rewarding properties of nicotine is associated with a reduction in nucleus accumbens DeltaFosB accumulation. J Pharmacol Exp Ther (2007) 0.93
Spontaneous and precipitated withdrawal after chronic intragastric administration of gamma-hydroxybutyrate (GHB) in baboons. Psychopharmacology (Berl) (2005) 0.93
Quinazolinedione sulfonamides: a novel class of competitive AMPA receptor antagonists with oral activity. Bioorg Med Chem Lett (2011) 0.92
Involvement of gamma-hydroxybutyrate (GHB) and GABA-B receptors in the acute behavioral effects of GHB in baboons. Psychopharmacology (Berl) (2005) 0.92
Repeated administration of the GABAB receptor positive modulator BHF177 decreased nicotine self-administration, and acute administration decreased cue-induced reinstatement of nicotine seeking in rats. Psychopharmacology (Berl) (2010) 0.92
Independent maturation of the GABA(B) receptor subunits GABA(B1) and GABA(B2) during postnatal development in rodent brain. J Comp Neurol (2004) 0.90
The sushi domains of secreted GABA(B1) isoforms selectively impair GABA(B) heteroreceptor function. J Biol Chem (2008) 0.90
GABAB1 receptor subunit isoforms exert a differential influence on baseline but not GABAB receptor agonist-induced changes in mice. J Pharmacol Exp Ther (2006) 0.88
Chronic intragastric administration of gamma-butyrolactone produces physical dependence in baboons. Psychopharmacology (Berl) (2006) 0.88
Coupling of human nicotinic acetylcholine receptors alpha 7 to calcium channels in GH3 cells. Neuropharmacology (2004) 0.88
Subtype-selective interaction with the transcription factor CCAAT/enhancer-binding protein (C/EBP) homologous protein (CHOP) regulates cell surface expression of GABA(B) receptors. J Biol Chem (2005) 0.87
In vivo effectiveness of CGP7930, a positive allosteric modulator of the GABAB receptor. Eur J Pharmacol (2004) 0.87
Point mutations in the transmembrane region of GABAB2 facilitate activation by the positive modulator N,N'-dicyclopentyl-2-methylsulfanyl-5-nitro-pyrimidine-4,6-diamine (GS39783) in the absence of the GABAB1 subunit. Mol Pharmacol (2006) 0.87
Prolonged nicotine exposure does not alter GABA(B) receptor-mediated regulation of brain reward function. Neuropharmacology (2005) 0.85
Discovery and structure activity relationship of small molecule inhibitors of toxic β-amyloid-42 fibril formation. J Biol Chem (2012) 0.85
GABAB receptors in Schwann cells influence proliferation and myelin protein expression. Eur J Neurosci (2004) 0.84
Altered response to benzodiazepine anxiolytics in mice lacking GABA B(1) receptors. Eur J Pharmacol (2004) 0.84
6-Amino quinazolinedione sulfonamides as orally active competitive AMPA receptor antagonists. Bioorg Med Chem Lett (2011) 0.83
The development of medications for alcohol-use disorders targeting the GABAB receptor system. Recent Pat CNS Drug Discov (2012) 0.83
Differential roles of mGlu(7) and mGlu(8) in amygdala-dependent behavior and physiology. Neuropharmacology (2013) 0.82
Both GABA(B) receptor activation and blockade exacerbated anhedonic aspects of nicotine withdrawal in rats. Eur J Pharmacol (2011) 0.82
Blocking metabotropic glutamate receptor subtype 7 (mGlu7) via the Venus flytrap domain (VFTD) inhibits amygdala plasticity, stress, and anxiety-related behavior. J Biol Chem (2014) 0.82
Altered hippocampal expression of calbindin-D-28k and calretinin in GABA(B(1))-deficient mice. Biochem Pharmacol (2004) 0.81
Selected amino acids, dipeptides and arylalkylamine derivatives do not act as allosteric modulators at GABAB receptors. Eur J Pharmacol (2004) 0.80
Recognition molecule associated carbohydrate inhibits postsynaptic GABA(B) receptors: a mechanism for homeostatic regulation of GABA release in perisomatic synapses. Mol Cell Neurosci (2003) 0.80
Hyperdopaminergia and altered locomotor activity in GABAB1-deficient mice. J Neurochem (2006) 0.80
JN403, in vitro characterization of a novel nicotinic acetylcholine receptor alpha7 selective agonist. Neurosci Lett (2007) 0.80
alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) antagonists: from bench to bedside. J Med Chem (2010) 0.80
Suppression of GABA(B) receptor function in vivo by disulfide reducing agent, DL-dithiothreitol (DTT). Psychopharmacology (Berl) (2004) 0.79
Determination of the minimal functional ligand-binding domain of the GABAB1b receptor. Biochem J (2005) 0.79
The GABA(B) antagonist CGP56433A attenuates the effect of baclofen on cocaine but not heroin self-administration in the rat. Psychopharmacology (Berl) (2001) 0.78
Increased efflux of amyloid-β peptides through the blood-brain barrier by muscarinic acetylcholine receptor inhibition reduces pathological phenotypes in mouse models of brain amyloidosis. J Alzheimers Dis (2014) 0.78
Gastrin-releasing peptide signaling plays a limited and subtle role in amygdala physiology and aversive memory. PLoS One (2012) 0.78
Influence of a GABA(B) and GABA(C) receptor antagonist on sleep-waking cycle in the rat. Eur J Pharmacol (2006) 0.78
Ligands for expression cloning and isolation of GABA(B) receptors. Farmaco (2003) 0.78