Published in ChemMedChem on September 03, 2010
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Recent advances in potential clinical application of ghrelin in obesity. J Obes (2012) 0.75
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From pyrroles to 1-oxo-2,3,4,9-tetrahydro-1H-beta-carbolines: a new class of orally bioavailable mGluR1 antagonists. Bioorg Med Chem Lett (2007) 2.06
Phenylethynyl-pyrrolo[1,2-a]pyrazine: a new potent and selective tool in the mGluR5 antagonists arena. Bioorg Med Chem Lett (2008) 1.40
The use of knock-out mice unravels distinct roles for mGlu2 and mGlu3 metabotropic glutamate receptors in mechanisms of neurodegeneration/neuroprotection. J Neurosci (2007) 1.38
Identification and characterization of novel NMDA receptor antagonists selective for NR2A- over NR2B-containing receptors. J Pharmacol Exp Ther (2010) 1.30
The Ca(V)3.3 calcium channel is the major sleep spindle pacemaker in thalamus. Proc Natl Acad Sci U S A (2011) 1.26
Neurokinin 1 receptor and relative abundance of the short and long isoforms in the human brain. Eur J Neurosci (2003) 1.20
Selective antagonism at dopamine D3 receptors prevents nicotine-triggered relapse to nicotine-seeking behavior. Neuropsychopharmacology (2003) 1.17
Structure-activity studies on neuropeptide S: identification of the amino acid residues crucial for receptor activation. J Biol Chem (2006) 1.13
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
Evidence that the metabotropic glutamate receptor 5 antagonist MPEP may act as an inhibitor of the norepinephrine transporter in vitro and in vivo. Synapse (2003) 1.06
A comparative study of the effects of the intravenous self-administration or subcutaneous minipump infusion of nicotine on the expression of brain neuronal nicotinic receptor subtypes. Mol Pharmacol (2010) 1.03
Scanning the Escherichia coli chromosome by random transposon mutagenesis and multiple phenotypic screening. Res Microbiol (2004) 1.02
Differential effects of the CRF-R1 antagonist GSK876008 on fear-potentiated, light- and CRF-enhanced startle suggest preferential involvement in sustained vs phasic threat responses. Neuropsychopharmacology (2008) 1.00
Correlation between serum ghrelin levels and cocaine-seeking behaviour triggered by cocaine-associated conditioned stimuli in rats. Addict Biol (2007) 0.99
Systemic administration of ghrelin increases extracellular dopamine in the shell but not the core subdivision of the nucleus accumbens. Neurochem Int (2008) 0.98
Functional magnetic resonance imaging reveals different neural substrates for the effects of orexin-1 and orexin-2 receptor antagonists. PLoS One (2011) 0.98
SB-656104-A, a novel selective 5-HT7 receptor antagonist, modulates REM sleep in rats. Br J Pharmacol (2003) 0.98
Occupancy of brain dopamine D3 receptors and drug craving: a translational approach. Neuropsychopharmacology (2012) 0.97
Altered levels of glutamatergic receptors and Na+/K+ ATPase-α1 in the prefrontal cortex of subjects with schizophrenia. Schizophr Res (2011) 0.97
Upregulation of [3H]methyllycaconitine binding sites following continuous infusion of nicotine, without changes of alpha7 or alpha6 subunit mRNA: an autoradiography and in situ hybridization study in rat brain. Eur J Neurosci (2002) 0.95
SB-649915-B, a novel 5-HT1A/B autoreceptor antagonist and serotonin reuptake inhibitor, is anxiolytic and displays fast onset activity in the rat high light social interaction test. Neuropsychopharmacology (2007) 0.93
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
The mGluR2/3 agonist LY379268 induced anti-reinstatement effects in rats exhibiting addiction-like behavior. Neuropsychopharmacology (2013) 0.91
GSK1614343, a novel ghrelin receptor antagonist, produces an unexpected increase of food intake and body weight in rodents and dogs. Neuroendocrinology (2011) 0.91
Neuroimaging evidence of altered fronto-cortical and striatal function after prolonged cocaine self-administration in the rat. Neuropsychopharmacology (2011) 0.90
A preclinical model of binge eating elicited by yo-yo dieting and stressful exposure to food: effect of sibutramine, fluoxetine, topiramate, and midazolam. Psychopharmacology (Berl) (2009) 0.90
In vitro and in vivo pharmacological characterization of the novel UT receptor ligand [Pen5,DTrp7,Dab8]urotensin II(4-11) (UFP-803). Br J Pharmacol (2006) 0.89
Discovery of potent, nonsystemic apical sodium-codependent bile acid transporter inhibitors (Part 1). J Med Chem (2005) 0.89
Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders. Bioorg Med Chem Lett (2011) 0.86
Discovery of NBI-77860/GSK561679, a potent corticotropin-releasing factor (CRF1) receptor antagonist with improved pharmacokinetic properties. Bioorg Med Chem Lett (2010) 0.86
Enhancement of CA3 hippocampal network activity by activation of group II metabotropic glutamate receptors. Proc Natl Acad Sci U S A (2011) 0.86
Glutamate receptor mGlu2 and mGlu3 knockout striata are dopamine supersensitive, with elevated D2(High) receptors and marked supersensitivity to the dopamine agonist (+)PHNO. Synapse (2009) 0.85
Role of orexin-1 receptor mechanisms on compulsive food consumption in a model of binge eating in female rats. Neuropsychopharmacology (2012) 0.85
Activation of mGlu3 receptors stimulates the production of GDNF in striatal neurons. PLoS One (2009) 0.85
Synthesis and pharmacological characterization of novel druglike corticotropin-releasing factor 1 antagonists. J Med Chem (2008) 0.85
Discovery of potent, nonsystemic apical sodium-codependent bile acid transporter inhibitors (Part 2). J Med Chem (2005) 0.84
Functional and binding kinetic studies make a distinction between OX1 and OX2 orexin receptor antagonists. Eur J Pharmacol (2012) 0.84
Anxiolytic-like effects of the neurokinin 1 receptor antagonist GR-205171 in the elevated plus maze and contextual fear-potentiated startle model of anxiety in gerbils. Behav Pharmacol (2009) 0.84
AMN082, an allosteric mGluR7 agonist that inhibits afferent glutamatergic transmission in rat basolateral amygdala. Neuropharmacology (2008) 0.83
Synergistic effects of cAMP-dependent signalling pathways and IL-1 on IL-6 production by H19-7/IGF-IR neuronal cells. Cell Signal (2006) 0.83
Slow dissociation of partial agonists from the D₂ receptor is linked to reduced prolactin release. Int J Neuropsychopharmacol (2011) 0.82
Delay of ejaculation induced by SB-277011, a selective dopamine D3 receptor antagonist, in the rat. J Sex Med (2008) 0.82
Both GABA(B) receptor activation and blockade exacerbated anhedonic aspects of nicotine withdrawal in rats. Eur J Pharmacol (2011) 0.82
Pharmacological characterization of the ghrelin receptor antagonist, GSK1614343 in rat RC-4B/C cells natively expressing GHS type 1a receptors. Eur J Pharmacol (2010) 0.82
PXS-4681A, a potent and selective mechanism-based inhibitor of SSAO/VAP-1 with anti-inflammatory effects in vivo. J Pharmacol Exp Ther (2013) 0.82
[3H]GR205171 displays similar NK1 receptor binding profile in gerbil and human brain. Br J Pharmacol (2006) 0.82
Pyrrolo[1,2-a]pyrazine and pyrazolo[1,5-a]pyrazine: novel, potent, and selective series of Vasopressin 1b receptor antagonists. Bioorg Med Chem Lett (2010) 0.81
Synthesis and pharmacological characterisation of 2,4-dicarboxy-pyrroles as selective non-competitive mGluR1 antagonists. Bioorg Med Chem (2003) 0.81
Synthesis and pharmacological characterization of constrained analogues of Vestipitant as in vitro potent and orally active NK(1) receptor antagonists. Bioorg Med Chem Lett (2009) 0.81
Individual contribution of metabotropic glutamate receptor (mGlu) 2 and 3 to c-Fos expression pattern evoked by mGlu2/3 antagonism. Psychopharmacology (Berl) (2008) 0.81
6-(3,4-dichlorophenyl)-1-[(methyloxy)methyl]-3-azabicyclo[4.1.0]heptane: a new potent and selective triple reuptake inhibitor. J Med Chem (2010) 0.80
Neurokinin 1 receptor antagonists--current prospects. Curr Opin Drug Discov Devel (2007) 0.80
3-Methyl pyrrole-2,4-dicarboxylic acid 2-propyl ester 4-(1,2,2-trimethyl-propyl) ester: an exploration of the C-2 position. Part I. Farmaco (2004) 0.79
Brain reinforcement system function is ghrelin dependent: studies in the rat using pharmacological fMRI and intracranial self-stimulation. Addict Biol (2011) 0.79
Down-regulation of amygdala preprotachykinin A mRNA but not 3H-SP receptor binding sites in subjects affected by mood disorders and schizophrenia. Eur J Neurosci (2005) 0.79
2,5-Disubstituted pyridines as potent GPR119 agonists. Bioorg Med Chem Lett (2010) 0.79
Effects of antidepressant drugs and GR 205171, an neurokinin-1 (NK1) receptor antagonist, on the response in the forced swim test and on monoamine extracellular levels in the frontal cortex of the mouse. Neurosci Lett (2003) 0.79
Chiral tetrahydroquinoline derivatives as potent anti-hyperalgesic agents in animal models of sustained inflammation and chronic neuropathic pain. Bioorg Med Chem Lett (2006) 0.79
New fused benzazepine as selective D3 receptor antagonists. Synthesis and biological evaluation. Part one: [h]-fused tricyclic systems. Bioorg Med Chem Lett (2008) 0.79
2,4-Dicarboxy-pyrroles as selective non-competitive mGluR1 antagonists: further characterization of 3,5-dimethyl pyrrole-2,4-dicarboxylic acid 2-propyl ester 4-(1,2,2-trimethyl-propyl) ester and structure-activity relationships. Bioorg Med Chem Lett (2003) 0.78
1-(Aryl)-6-[alkoxyalkyl]-3-azabicyclo[3.1.0]hexanes and 6-(aryl)-6-[alkoxyalkyl]-3-azabicyclo[3.1.0]hexanes: a new series of potent and selective triple reuptake inhibitors. J Med Chem (2010) 0.78
Azabicyclo[3.1.0]hexane-1-carbohydrazides as potent and selective GHSR1a ligands presenting a specific in vivo behavior. ChemMedChem (2011) 0.78
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). Neuropharmacology (2011) 0.78
The identification of novel orally active mGluR5 antagonist GSK2210875. Bioorg Med Chem Lett (2010) 0.78
Oxa-azaspiro derivatives: a novel class of triple re-uptake inhibitors. ChemMedChem (2010) 0.78