Published in Nat Rev Drug Discov on February 01, 2005
Histamine and its receptors. Br J Pharmacol (2006) 1.53
The histamine H3 receptor: an attractive target for the treatment of cognitive disorders. Br J Pharmacol (2008) 1.49
Histamine-induced itch and its relationship with pain. Mol Pain (2008) 1.34
Marked changes in signal transduction upon heteromerization of dopamine D1 and histamine H3 receptors. Br J Pharmacol (2009) 1.25
A bulky biaryl phosphine ligand allows for palladium-catalyzed amidation of five-membered heterocycles as electrophiles. Angew Chem Int Ed Engl (2012) 1.22
Interactions between histamine H3 and dopamine D2 receptors and the implications for striatal function. Neuropharmacology (2008) 1.15
Itch signaling in the nervous system. Physiology (Bethesda) (2011) 1.13
Histamine excites neurones in the human submucous plexus through activation of H1, H2, H3 and H4 receptors. J Physiol (2007) 1.08
Molecular and biochemical pharmacology of the histamine H4 receptor. Br J Pharmacol (2009) 1.06
Mild and general conditions for negishi cross-coupling enabled by the use of palladacycle precatalysts. Angew Chem Int Ed Engl (2012) 1.06
Dopamine D1-histamine H3 receptor heteromers provide a selective link to MAPK signaling in GABAergic neurons of the direct striatal pathway. J Biol Chem (2010) 1.02
Molecular and cellular analysis of human histamine receptor subtypes. Trends Pharmacol Sci (2012) 1.01
Current therapeutic targets for the treatment of Alzheimer's disease. Expert Rev Neurother (2010) 0.99
The role of carcinine in signaling at the Drosophila photoreceptor synapse. PLoS Genet (2007) 0.99
Therapeutic potential of histamine H3 receptor agonist for the treatment of obesity and diabetes mellitus. Proc Natl Acad Sci U S A (2006) 0.95
Role of histamine and its receptor subtypes in stimulation of conjunctival goblet cell secretion. Invest Ophthalmol Vis Sci (2012) 0.94
Histaminergic mechanisms for modulation of memory systems. Neural Plast (2011) 0.94
Neuropharmacology of vestibular system disorders. Curr Neuropharmacol (2010) 0.93
Total synthesis and biological evaluation of phidianidines A and B uncovers unique pharmacological profiles at CNS targets. ACS Chem Neurosci (2012) 0.93
Generation of a homology model of the human histamine H(3) receptor for ligand docking and pharmacophore-based screening. J Comput Aided Mol Des (2007) 0.92
H3 receptors and pain modulation: peripheral, spinal, and brain interactions. J Pharmacol Exp Ther (2010) 0.91
Total Synthesis (+)-7-Bromotrypargine and Unnatural Analogs: Biological Evaluation Uncovers Activity at CNS Targets of Therapeutic Relevance. ACS Chem Neurosci (2011) 0.89
Histamine H3 receptor antagonists/inverse agonists on cognitive and motor processes: relevance to Alzheimer's disease, ADHD, schizophrenia, and drug abuse. Front Syst Neurosci (2012) 0.89
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Pharmacological characterization of GSK1004723, a novel, long-acting antagonist at histamine H(1) and H(3) receptors. Br J Pharmacol (2011) 0.88
Histaminergic and glycinergic modulation of GABA release in the vestibular nuclei of normal and labyrinthectomised rats. J Physiol (2006) 0.87
Anxiolytic-like profiles of histamine H3 receptor agonists in animal models of anxiety: a comparative study with antidepressants and benzodiazepine anxiolytic. Psychopharmacology (Berl) (2009) 0.87
Pharmacological characterization of the new histamine H4 receptor agonist VUF 8430. Br J Pharmacol (2009) 0.87
Histamine H3 receptors aggravate cerebral ischaemic injury by histamine-independent mechanisms. Nat Commun (2014) 0.86
Histamine H3 receptor antagonists in relation to epilepsy and neurodegeneration: a systemic consideration of recent progress and perspectives. Br J Pharmacol (2012) 0.86
Modulation of prepulse inhibition and stereotypies in rodents: no evidence for antipsychotic-like properties of histamine H3-receptor inverse agonists. Psychopharmacology (Berl) (2010) 0.86
The waking brain: an update. Cell Mol Life Sci (2011) 0.86
Role of histamine and its receptors in cerebral ischemia. ACS Chem Neurosci (2012) 0.85
Short photoperiod-induced decrease of histamine H3 receptors facilitates activation of hypothalamic neurons in the Siberian hamster. Endocrinology (2009) 0.85
The psychostimulant and rewarding effects of cocaine in histidine decarboxylase knockout mice do not support the hypothesis of an inhibitory function of histamine on reward. Psychopharmacology (Berl) (2006) 0.84
Alzheimer's disease and age-related memory decline (preclinical). Pharmacol Biochem Behav (2011) 0.83
Palladium-catalyzed intramolecular C-H difluoroalkylation: synthesis of substituted 3,3-difluoro-2-oxindoles. Angew Chem Int Ed Engl (2014) 0.81
A single-point mutation (Ala280Val) in the third intracellular loop alters the signalling properties of the human histamine H₃ receptor stably expressed in CHO-K1 cells. Br J Pharmacol (2013) 0.80
Palladium-catalyzed completely linear-selective Negishi cross-coupling of allylzinc halides with aryl and vinyl electrophiles. Angew Chem Int Ed Engl (2013) 0.80
Highly selective palladium-catalyzed cross-coupling of secondary alkylzinc reagents with heteroaryl halides. Org Lett (2014) 0.80
Natriuretic peptide-induced catecholamine release from cardiac sympathetic neurons: inhibition by histamine H3 and H4 receptor activation. J Pharmacol Exp Ther (2012) 0.79
Anxiolytic and antidepressant-like activities of the novel and potent non-imidazole histamine H₃ receptor antagonist ST-1283. Drug Des Devel Ther (2014) 0.79
Effect of a novel histamine subtype-3 receptor inverse agonist and modafinil on EEG power spectra during sleep deprivation and recovery sleep in male volunteers. Psychopharmacology (Berl) (2011) 0.79
Comparison of Different 2D and 3D-QSAR Methods on Activity Prediction of Histamine H3 Receptor Antagonists. Iran J Pharm Res (2012) 0.79
Improvement of the Prediction Power of the CoMFA and CoMSIA Models on Histamine H3 Antagonists by Different Variable Selection Methods. Sci Pharm (2012) 0.79
Histamine-HisCl1 receptor axis regulates wake-promoting signals in Drosophila melanogaster. PLoS One (2013) 0.78
The histamine autoreceptor is a short isoform of the H₃ receptor. Br J Pharmacol (2012) 0.78
Inhibition of histamine receptor 3 suppresses glioblastoma tumor growth, invasion, and epithelial-to-mesenchymal transition. Oncotarget (2015) 0.78
Radiosynthesis and evaluation of an (18)F-labeled positron emission tomography (PET) radioligand for brain histamine subtype-3 receptors based on a nonimidazole 2-aminoethylbenzofuran chemotype. J Med Chem (2012) 0.77
Waking with the hypothalamus. Pflugers Arch (2011) 0.77
The expression and function of histamine H₃ receptors in pancreatic beta cells. Br J Pharmacol (2014) 0.77
Synthesis and characterization of new bivalent agents as melatonin- and histamine H3-ligands. Int J Mol Sci (2014) 0.76
In vitro and in vivo pharmacological analysis of imidazole-free histamine H3 receptor antagonists: promising results for a brain-penetrating H3 blocker with weak anticholinesterase activity. Naunyn Schmiedebergs Arch Pharmacol (2008) 0.76
Role of histamine H3 receptor in glucagon-secreting αTC1.6 cells. FEBS Open Bio (2014) 0.75
Ciproxifan, a histamine H3 receptor antagonist, reversibly inhibits monoamine oxidase A and B. Sci Rep (2017) 0.75
The histamine H3 receptor antagonist thioperamide rescues circadian rhythm and memory function in experimental parkinsonism. Transl Psychiatry (2017) 0.75
Mathematical analysis of the sodium sensitivity of the human histamine H3 receptor. In Silico Pharmacol (2014) 0.75
Proxyfan acts as a neutral antagonist of histamine H3 receptors in the feeding-related hypothalamic ventromedial nucleus. Br J Pharmacol (2012) 0.75
Discovery of a potent thiadiazole class of histamine h3 receptor antagonist for the treatment of diabetes. ACS Med Chem Lett (2011) 0.75
Assessment of the abuse liability of ABT-288, a novel histamine H₃ receptor antagonist. Psychopharmacology (Berl) (2013) 0.75
ALDH enzyme activity is regulated by Nodal and histamine in the A549 cell line. Oncol Lett (2017) 0.75
Methylphenidate Decreases ATP Levels and Impairs Glutamate Uptake and Na(+),K(+)-ATPase Activity in Juvenile Rat Hippocampus. Mol Neurobiol (2016) 0.75
Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist. J Pharmacol Exp Ther (2005) 1.52
Pharmacogenomic and structural analysis of constitutive g protein-coupled receptor activity. Annu Rev Pharmacol Toxicol (2007) 1.42
Diazepam-bound GABAA receptor models identify new benzodiazepine binding-site ligands. Nat Chem Biol (2012) 1.31
Crystal structure-based virtual screening for fragment-like ligands of the human histamine H(1) receptor. J Med Chem (2011) 1.30
A G(q/11)-coupled mutant histamine H(1) receptor F435A activated solely by synthetic ligands (RASSL). J Biol Chem (2005) 1.29
Pentameric ligand-gated ion channel ELIC is activated by GABA and modulated by benzodiazepines. Proc Natl Acad Sci U S A (2012) 1.22
Fragment based design of new H4 receptor-ligands with anti-inflammatory properties in vivo. J Med Chem (2008) 1.20
Keynote review: histamine H3 receptor antagonists reach out for the clinic. Drug Discov Today (2005) 1.19
Chemical insights in the concept of hybrid drugs: the antitumor effect of nitric oxide-donating aspirin involves a quinone methide but not nitric oxide nor aspirin. J Med Chem (2007) 1.18
A structural insight into the reorientation of transmembrane domains 3 and 5 during family A G protein-coupled receptor activation. Mol Pharmacol (2010) 1.14
Linking agonist binding to histamine H1 receptor activation. Nat Chem Biol (2005) 1.14
Towards small-molecule CXCR3 ligands with clinical potential. ChemMedChem (2008) 1.11
Use of acetylcholine binding protein in the search for novel alpha7 nicotinic receptor ligands. In silico docking, pharmacological screening, and X-ray analysis. J Med Chem (2009) 1.11
Constitutively active Gq/11-coupled receptors enable signaling by co-expressed G(i/o)-coupled receptors. J Biol Chem (2003) 1.10
Transforming fragments into candidates: small becomes big in medicinal chemistry. Drug Discov Today (2009) 1.09
Molecular and biochemical pharmacology of the histamine H4 receptor. Br J Pharmacol (2009) 1.06
Antiinflammatory and antinociceptive effects of the selective histamine H4-receptor antagonists JNJ7777120 and VUF6002 in a rat model of carrageenan-induced acute inflammation. Eur J Pharmacol (2007) 1.04
Synthesis and structure-activity relationships of indole and benzimidazole piperazines as histamine H(4) receptor antagonists. Bioorg Med Chem Lett (2004) 1.04
CC12, a high-affinity ligand for [3H]cimetidine binding, is an improgan antagonist. Neuropharmacology (2007) 1.02
CC and CX3C chemokines differentially interact with the N terminus of the human cytomegalovirus-encoded US28 receptor. J Biol Chem (2004) 1.01
Oligomerization of recombinant and endogenously expressed human histamine H(4) receptors. Mol Pharmacol (2006) 1.00
Fragment growing induces conformational changes in acetylcholine-binding protein: a structural and thermodynamic analysis. J Am Chem Soc (2011) 1.00
Catechol pyrazolinones as trypanocidals: fragment-based design, synthesis, and pharmacological evaluation of nanomolar inhibitors of trypanosomal phosphodiesterase B1. J Med Chem (2012) 0.99
Noncompetitive antagonism and inverse agonism as mechanism of action of nonpeptidergic antagonists at primate and rodent CXCR3 chemokine receptors. J Pharmacol Exp Ther (2008) 0.99
Discovery of quinazolines as histamine H4 receptor inverse agonists using a scaffold hopping approach. J Med Chem (2008) 0.98
Mutational analysis of the histamine H1-receptor binding pocket of histaprodifens. Eur J Pharmacol (2004) 0.98
Identification of the first nonpeptidergic inverse agonist for a constitutively active viral-encoded G protein-coupled receptor. J Biol Chem (2002) 0.97
Sex- and histamine-dependent long-term cognitive effects of methamphetamine exposure. Neuropsychopharmacology (2006) 0.96
Synthesis and structure-activity relationship of the first nonpeptidergic inverse agonists for the human cytomegalovirus encoded chemokine receptor US28. J Med Chem (2005) 0.96
Antinociceptive activity of chemical congeners of improgan: optimization of side chain length leads to the discovery of a new, potent, non-opioid analgesic. Neuropharmacology (2006) 0.96
Cloning and characterization of dominant negative splice variants of the human histamine H4 receptor. Biochem J (2008) 0.96
Online fluorescence enhancement assay for the acetylcholine binding protein with parallel mass spectrometric identification. J Med Chem (2010) 0.96
Molecular aspects of the histamine H3 receptor. Biochem Pharmacol (2007) 0.93
Molecular determinants of ligand binding to H4R species variants. Mol Pharmacol (2010) 0.93
Improgan antinociception does not require neuronal histamine or histamine receptors. Brain Res (2003) 0.92
Phenylalanine 169 in the second extracellular loop of the human histamine H4 receptor is responsible for the difference in agonist binding between human and mouse H4 receptors. J Pharmacol Exp Ther (2008) 0.92
Discovery of novel Trypanosoma brucei phosphodiesterase B1 inhibitors by virtual screening against the unliganded TbrPDEB1 crystal structure. J Med Chem (2013) 0.91
SYNOPSIS: SYNthesize and OPtimize System in Silico. J Med Chem (2003) 0.90
Non-imidazole histamine H3 ligands. Part III. New 4-n-propylpiperazines as non-imidazole histamine H3-antagonists. Eur J Med Chem (2005) 0.89
GPCR proteomics: mass spectrometric and functional analysis of histamine H1 receptor after baculovirus-driven and in vitro cell free expression. J Proteome Res (2008) 0.89
The Akt/GSK-3beta axis as a new signaling pathway of the histamine H(3) receptor. J Neurochem (2007) 0.89
Identification of a novel scaffold for allosteric inhibition of wild type and drug resistant HIV-1 reverse transcriptase by fragment library screening. J Med Chem (2011) 0.89
Discovery of S-(2-guanidylethyl)-isothiourea (VUF 8430) as a potent nonimidazole histamine H4 receptor agonist. J Med Chem (2006) 0.88
Histamine protects against NMDA-induced necrosis in cultured cortical neurons through H receptor/cyclic AMP/protein kinase A and H receptor/GABA release pathways. J Neurochem (2006) 0.88
KLIFS: a knowledge-based structural database to navigate kinase-ligand interaction space. J Med Chem (2013) 0.88
Development of a selective ESI-MS derivatization reagent: synthesis and optimization for the analysis of aldehydes in biological mixtures. Anal Chem (2008) 0.88
Acetylcholine binding protein (AChBP) as template for hierarchical in silico screening procedures to identify structurally novel ligands for the nicotinic receptors. Bioorg Med Chem (2011) 0.87
Pharmacological characterization of the new histamine H4 receptor agonist VUF 8430. Br J Pharmacol (2009) 0.87
Differential activation of murine herpesvirus 68- and Kaposi's sarcoma-associated herpesvirus-encoded ORF74 G protein-coupled receptors by human and murine chemokines. J Virol (2004) 0.86
From heptahelical bundle to hits from the Haystack: structure-based virtual screening for GPCR ligands. Methods Enzymol (2013) 0.86
Fragment library screening reveals remarkable similarities between the G protein-coupled receptor histamine H₄ and the ion channel serotonin 5-HT₃A. Bioorg Med Chem Lett (2011) 0.86
The histamine H3 receptor antagonist clobenpropit enhances GABA release to protect against NMDA-induced excitotoxicity through the cAMP/protein kinase A pathway in cultured cortical neurons. Eur J Pharmacol (2007) 0.86
Design, synthesis, and structure-activity relationships of highly potent 5-HT₃ receptor ligands. J Med Chem (2012) 0.85
Major advances in the development of histamine H4 receptor ligands. Drug Discov Today (2009) 0.85
Delineation of agonist binding to the human histamine H4 receptor using mutational analysis, homology modeling, and ab initio calculations. J Chem Inf Model (2008) 0.85
En route to new blockbuster anti-histamines: surveying the offspring of the expanding histamine receptor family. Trends Pharmacol Sci (2011) 0.85
Synthesis and pharmacological characterization of novel inverse agonists acting on the viral-encoded chemokine receptor US28. Bioorg Med Chem (2006) 0.85
Identification of overlapping but differential binding sites for the high-affinity CXCR3 antagonists NBI-74330 and VUF11211. Mol Pharmacol (2013) 0.85
Identification of 4-(1H-imidazol-4(5)-ylmethyl)pyridine (immethridine) as a novel, potent, and highly selective histamine H(3) receptor agonist. J Med Chem (2004) 0.84
Effect of the histamine H3-antagonist clobenpropit on spatial memory deficits induced by MK-801 as evaluated by radial maze in Sprague-Dawley rats. Behav Brain Res (2004) 0.84
Fragment based lead discovery of small molecule inhibitors for the EPHA4 receptor tyrosine kinase. Eur J Med Chem (2011) 0.84
Assembly of a π-π stack of ligands in the binding site of an acetylcholine-binding protein. Nat Commun (2013) 0.84
Virtual fragment screening: discovery of histamine H3 receptor ligands using ligand-based and protein-based molecular fingerprints. J Chem Inf Model (2012) 0.84
N-substituted piperidinyl alkyl imidazoles: discovery of methimepip as a potent and selective histamine H3 receptor agonist. J Med Chem (2005) 0.84
Characterization of the histamine H4 receptor binding site. Part 1. Synthesis and pharmacological evaluation of dibenzodiazepine derivatives. J Med Chem (2006) 0.84
Synthesis and pharmacological identification of neutral histamine H1-receptor antagonists. J Med Chem (2003) 0.84
A flow-through fluorescence polarization detection system for measuring GPCR-mediated modulation of cAMP production. J Biomol Screen (2007) 0.83
Synthesis, modeling and functional activity of substituted styrene-amides as small-molecule CXCR7 agonists. Eur J Med Chem (2012) 0.83
Helix 8 of the viral chemokine receptor ORF74 directs chemokine binding. J Biol Chem (2006) 0.83
Development of a microfluidic confocal fluorescence detection system for the hyphenation of nano-LC to on-line biochemical assays. Anal Bioanal Chem (2010) 0.82
Several down, a few to go: histamine H3 receptor ligands making the final push towards the market? Expert Opin Investig Drugs (2011) 0.82
A new generation of anti-histamines: Histamine H4 receptor antagonists on their way to the clinic. Curr Opin Drug Discov Devel (2009) 0.82
Large-scale overproduction, functional purification and ligand affinities of the His-tagged human histamine H1 receptor. Eur J Biochem (2004) 0.82
Small and colorful stones make beautiful mosaics: fragment-based chemogenomics. Drug Discov Today (2012) 0.82
A selective human H(4)-receptor agonist: (-)-2-cyano-1-methyl-3-[(2R,5R)-5- [1H-imidazol-4(5)-yl]tetrahydrofuran-2-y] methylguanidine. J Med Chem (2003) 0.82
Constitutively active mutants of the histamine H1 receptor suggest a conserved hydrophobic asparagine-cage that constrains the activation of class A G protein-coupled receptors. Mol Pharmacol (2007) 0.82
Interaction kinetic and structural dynamic analysis of ligand binding to acetylcholine-binding protein. Biochemistry (2010) 0.82
Targeted LC-MS derivatization for aldehydes and carboxylic acids with a new derivatization agent 4-APEBA. Anal Bioanal Chem (2010) 0.81
Crystal structure of the EphA4 protein tyrosine kinase domain in the apo- and dasatinib-bound state. FEBS Lett (2011) 0.81
CXCR3 antagonists: quaternary ammonium salts equipped with biphenyl- and polycycloaliphatic-anchors. Bioorg Med Chem (2011) 0.81
An 80-amino acid deletion in the third intracellular loop of a naturally occurring human histamine H3 isoform confers pharmacological differences and constitutive activity. J Pharmacol Exp Ther (2007) 0.81
Synthesis and structure-activity relationships of 3H-quinazolin-4-ones and 3H-pyrido[2,3-d]pyrimidin-4-ones as CXCR3 receptor antagonists. Arch Pharm (Weinheim) (2007) 0.81
Synthesis and structure-activity relationships of conformationally constrained histamine H(3) receptor agonists. J Med Chem (2003) 0.80
Identification of novel α7 nicotinic receptor ligands by in silico screening against the crystal structure of a chimeric α7 receptor ligand binding domain. Bioorg Med Chem (2012) 0.80
From three-dimensional GPCR structure to rational ligand discovery. Adv Exp Med Biol (2014) 0.80
QUASI: a novel method for simultaneous superposition of multiple flexible ligands and virtual screening using partial similarity. J Chem Inf Model (2007) 0.80