Published in Bioorg Med Chem on December 25, 2007
Design, synthesis, and antiviral activity of entry inhibitors that target the CD4-binding site of HIV-1. J Med Chem (2012) 1.02
Virtual screening based identification of novel small-molecule inhibitors targeted to the HIV-1 capsid. Bioorg Med Chem (2010) 0.92
Ciproxifan, an H3 receptor antagonist, alleviates hyperactivity and cognitive deficits in the APP Tg2576 mouse model of Alzheimer's disease. Neurobiol Learn Mem (2010) 0.87
Targeting acetylcholinesterase: identification of chemical leads by high throughput screening, structure determination and molecular modeling. PLoS One (2011) 0.84
Synthesis, biological evaluation, and computational studies of Tri- and tetracyclic nitrogen-bridgehead compounds as potent dual-acting AChE inhibitors and hH3 receptor antagonists. ACS Chem Neurosci (2014) 0.77
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Computational analysis of novel drugs designed for use as acetylcholinesterase inhibitors and histamine H3 receptor antagonists for Alzheimer's disease by docking, scoring and de novo evolution. Mol Med Rep (2012) 0.75
Probing the origins of human acetylcholinesterase inhibition via QSAR modeling and molecular docking. PeerJ (2016) 0.75
Oxysterols direct B-cell migration through EBI2. Nature (2011) 1.94
Selective blockade of the capsaicin receptor TRPV1 attenuates bone cancer pain. J Neurosci (2005) 1.83
Inhibition of fatty acid amide hydrolase produces analgesia by multiple mechanisms. Br J Pharmacol (2006) 1.77
Lactate inhibits lipolysis in fat cells through activation of an orphan G-protein-coupled receptor, GPR81. J Biol Chem (2008) 1.75
Blockade of orexin-1 receptors attenuates orexin-2 receptor antagonism-induced sleep promotion in the rat. J Pharmacol Exp Ther (2009) 1.40
Identification of relaxin-3/INSL7 as an endogenous ligand for the orphan G-protein-coupled receptor GPCR135. J Biol Chem (2003) 1.39
Targeted disruption of RC3 reveals a calmodulin-based mechanism for regulating metaplasticity in the hippocampus. J Neurosci (2002) 1.33
The first potent and selective non-imidazole human histamine H4 receptor antagonists. J Med Chem (2003) 1.28
Behavioral characterization of mice lacking histamine H(3) receptors. Mol Pharmacol (2002) 1.26
Identification and biological evaluation of 4-(3-trifluoromethylpyridin-2-yl)piperazine-1-carboxylic acid (5-trifluoromethylpyridin-2-yl)amide, a high affinity TRPV1 (VR1) vanilloid receptor antagonist. J Med Chem (2005) 1.20
Identification of relaxin-3/INSL7 as a ligand for GPCR142. J Biol Chem (2003) 1.19
A simple stopped assay for fatty acid amide hydrolase avoiding the use of a chloroform extraction phase. J Biochem Biophys Methods (2004) 1.19
Palladium-catalyzed coupling of pyrazole triflates with arylboronic acids. J Org Chem (2005) 1.12
INSL5 is a high affinity specific agonist for GPCR142 (GPR100). J Biol Chem (2004) 1.12
International Union of Basic and Clinical Pharmacology. LXXXII: Nomenclature and Classification of Hydroxy-carboxylic Acid Receptors (GPR81, GPR109A, and GPR109B). Pharmacol Rev (2011) 1.11
Selective blockade of the orexin-2 receptor attenuates ethanol self-administration, place preference, and reinstatement. Psychopharmacology (Berl) (2010) 1.08
Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase. Bioorg Med Chem Lett (2008) 1.05
Biochemical and biological properties of 4-(3-phenyl-[1,2,4] thiadiazol-5-yl)-piperazine-1-carboxylic acid phenylamide, a mechanism-based inhibitor of fatty acid amide hydrolase. Anesth Analg (2009) 1.04
R3(BDelta23 27)R/I5 chimeric peptide, a selective antagonist for GPCR135 and GPCR142 over relaxin receptor LGR7: in vitro and in vivo characterization. J Biol Chem (2007) 1.03
A novel form of neurotensin post-translationally modified by arginylation. J Biol Chem (2005) 1.01
Selective blockade of 5-hydroxytryptamine (5-HT)7 receptors enhances 5-HT transmission, antidepressant-like behavior, and rapid eye movement sleep suppression induced by citalopram in rodents. J Pharmacol Exp Ther (2007) 0.99
Decreased intracellular calcium mediates the histamine H3-receptor-induced attenuation of norepinephrine exocytosis from cardiac sympathetic nerve endings. Proc Natl Acad Sci U S A (2001) 0.97
Distribution of G-protein-coupled receptor (GPCR)135 binding sites and receptor mRNA in the rat brain suggests a role for relaxin-3 in neuroendocrine and sensory processing. Neuroendocrinology (2005) 0.95
Norepinephrine release from the ischemic heart is greatly enhanced in mice lacking histamine H3 receptors. Mol Pharmacol (2003) 0.95
Relaxin-3/insulin-like peptide 5 chimeric peptide, a selective ligand for G protein-coupled receptor (GPCR)135 and GPCR142 over leucine-rich repeat-containing G protein-coupled receptor 7. Mol Pharmacol (2004) 0.94
The novel, selective, brain-penetrant neuropeptide Y Y2 receptor antagonist, JNJ-31020028, tested in animal models of alcohol consumption, relapse, and anxiety. Alcohol (2010) 0.92
3,5-Dihydroxybenzoic acid, a specific agonist for hydroxycarboxylic acid 1, inhibits lipolysis in adipocytes. J Pharmacol Exp Ther (2012) 0.92
Non-imidazole heterocyclic histamine H3 receptor antagonists. Bioorg Med Chem Lett (2003) 0.90
In vitro and in vivo characterization of JNJ-31020028 (N-(4-{4-[2-(diethylamino)-2-oxo-1-phenylethyl]piperazin-1-yl}-3-fluorophenyl)-2-pyridin-3-ylbenzamide), a selective brain penetrant small molecule antagonist of the neuropeptide Y Y(2) receptor. Psychopharmacology (Berl) (2009) 0.90
Pharmacological characterization of JNJ-28583867, a histamine H(3) receptor antagonist and serotonin reuptake inhibitor. Eur J Pharmacol (2007) 0.90
Pharmacokinetics and pharmacodynamics of norfluoxetine in rats: Increasing extracellular serotonin level in the frontal cortex. Pharmacol Biochem Behav (2009) 0.89
Preparation and biological evaluation of indole, benzimidazole, and thienopyrrole piperazine carboxamides: potent human histamine h(4) antagonists. J Med Chem (2005) 0.89
Molecular and pharmacological characterization of the mouse histamine H3 receptor. Eur J Pharmacol (2003) 0.88
Effects of SB-269970, a 5-HT7 receptor antagonist, in mouse models predictive of antipsychotic-like activity. Behav Pharmacol (2008) 0.88
Pharmacological blockade of serotonin 5-HT₇ receptor reverses working memory deficits in rats by normalizing cortical glutamate neurotransmission. PLoS One (2011) 0.88
Histamine H3 antagonists as wake-promoting and pro-cognitive agents. Curr Top Med Chem (2008) 0.88
JNJ-39220675, a novel selective histamine H3 receptor antagonist, reduces the abuse-related effects of alcohol in rats. Psychopharmacology (Berl) (2010) 0.87
Pharmacological characterization of a novel centrally permeable P2X7 receptor antagonist: JNJ-47965567. Br J Pharmacol (2013) 0.87
Reconsideration of 5-hydroxytryptamine (5-HT)(7) receptor distribution using [(3)H]5-carboxamidotryptamine and [(3)H]8-hydroxy-2-(di-n-propylamino)tetraline: analysis in brain of 5-HT(1A) knockout and 5-HT(1A/1B) double-knockout mice. J Pharmacol Exp Ther (2002) 0.86
Pharmacological characterization of relaxin-3/INSL7 receptors GPCR135 and GPCR142 from different mammalian species. J Pharmacol Exp Ther (2004) 0.86
Neuropeptide S stimulates dopaminergic neurotransmission in the medial prefrontal cortex. J Neurochem (2010) 0.86
Identification of structural motifs critical for epstein-barr virus-induced molecule 2 function and homology modeling of the ligand docking site. Mol Pharmacol (2012) 0.86
JNJ-10181457, a selective non-imidazole histamine H(3) receptor antagonist, normalizes acetylcholine neurotransmission and has efficacy in translational rat models of cognition. Neuropharmacology (2009) 0.85
Effects of histamine H(3) antagonists and donepezil on learning and mnemonic deficits induced by pentylenetetrazol kindling in weanling mice. Neuropharmacology (2005) 0.85
A high-throughput-compatible assay for determining the activity of fatty acid amide hydrolase. Anal Biochem (2003) 0.84
Aplysamine-1 and related analogs as histamine H3 receptor antagonists. Bioorg Med Chem Lett (2005) 0.84
Translational evaluation of JNJ-18038683, a 5-hydroxytryptamine type 7 receptor antagonist, on rapid eye movement sleep and in major depressive disorder. J Pharmacol Exp Ther (2012) 0.84
Relaxin-3, INSL5, and their receptors. Results Probl Cell Differ (2008) 0.83
Pre-clinical characterization of aryloxypyridine amides as histamine H3 receptor antagonists: identification of candidates for clinical development. Bioorg Med Chem Lett (2010) 0.83
Novel substituted 4-phenyl-[1,3]dioxanes: potent and selective orexin receptor 2 (OX(2)R) antagonists. Bioorg Med Chem Lett (2004) 0.83
A new class of diamine-based human histamine H3 receptor antagonists: 4-(aminoalkoxy)benzylamines. J Med Chem (2003) 0.83
2-Aryloxymethylmorpholine histamine H(3) antagonists. Bioorg Med Chem Lett (2008) 0.83
Heteroaryl urea inhibitors of fatty acid amide hydrolase: structure-mutagenicity relationships for arylamine metabolites. Bioorg Med Chem Lett (2012) 0.83
In vitro microbiological characterization of a novel azalide, two triamilides and an azalide ketal against bovine and porcine respiratory pathogens. J Antibiot (Tokyo) (2004) 0.82
The discovery and synthesis of JNJ 31020028, a small molecule antagonist of the Neuropeptide Y Y₂ receptor. Bioorg Med Chem Lett (2011) 0.82
Radiosynthesis and biodistribution of a histamine H3 receptor antagonist 4-[3-(4-piperidin-1-yl-but-1-ynyl)-[11C]benzyl]-morpholine: evaluation of a potential PET ligand. Nucl Med Biol (2006) 0.81
Novel non-peptidic neuropeptide Y Y2 receptor antagonists. Bioorg Med Chem Lett (2004) 0.81
Novel human histamine H(3) receptor antagonists. Bioorg Med Chem Lett (2002) 0.81
Relaxin family peptides and receptors in mammalian brain. Ann N Y Acad Sci (2009) 0.81