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Histamine receptor H3

histamine H3 receptor
Histamine is a ubiquitous messenger molecule released from mast cells, enterochromaffin-like cells, and neurons. Its various actions are mediated by histamine receptors H1, H2, H3 and H4. This gene encodes one of the histamine receptors (H3) which belongs to the family 1 of G protein-coupled receptors. It is an integral membrane protein and can regulate neurotransmitter release. This receptor can also increase voltage-dependent calcium current in smooth muscles and innervates the blood vessels and the heart in cardiovascular system. [provided by RefSeq, Jul 2008] (from NCBI)
Top mentioned proteins: H1, HAD, CAN, ACID, V1a
Papers on histamine H3 receptor
Chlorophenoxy aminoalkyl derivatives as histamine H3R ligands and antiseizure agents.
Kieć-Kononowicz et al., Kraków, Poland. In Bioorg Med Chem, Feb 2016
A series of twenty new chlorophenoxyalkylamine derivatives (9-28) was synthesized and evaluated on their binding properties at the human histamine H3 receptor (hH3R).
The dual-acting H3 receptor antagonist and AChE inhibitor UW-MD-71 dose-dependently enhances memory retrieval and reverses dizocilpine-induced memory impairment in rats.
Sadek et al., Al `Ayn, United Arab Emirates. In Behav Brain Res, Feb 2016
Both the histamine H3 receptor (H3R) and acetylcholine esterase (AChE) are involved in the regulation of release and metabolism of acetylcholine and several other central neurotransmitters.
Spinal histamine in attenuation of mechanical hypersensitivity in the spinal nerve ligation-induced model of experimental neuropathy.
Pertovaara et al., Helsinki, Finland. In Eur J Pharmacol, Jan 2016
A-960656, a histamine H3 receptor antagonist alone that presumably increased endogenous histamine levels reduced hypersensitivity.
Benzamide derivatives and their constrained analogs as histamine H3 receptor antagonists.
Abraham et al., Hyderābād, India. In Eur J Med Chem, Jan 2016
UNASSIGNED: A series of 4-(1-substituted piperidin-4-yloxy) benzamides and 6-(1-substituted piperidin-4-yloxy)-3,4-dihydro-2H-isoquinolin-1-one derivatives have been synthesized and tested for their binding affinity towards H3 receptor.
Anticonvulsant and procognitive properties of the non-imidazole histamine H3 receptor antagonist DL77 in male adult rats.
Kieć-Kononowiczc et al., Al `Ayn, United Arab Emirates. In Neuropharmacology, Nov 2015
The new non-imidazole H3R antagonist DL77 has excellent selectivity profile and shows high in-vivo potency as well as in-vitro antagonist affinity with ED50 values of 2.1 ± 0.2 mg/kg and 8.4 ± 1.3 [nM], respectively.
Lipopolysaccharide and histaminergic systems interact to mediate food intake in broilers.
Hassanpour et al., Tehrān, Iran. In Br Poult Sci, Oct 2015
The effects of intracerebroventricular (ICV) injection of α-fluoromethylhistidine (α-FMH, histidine decarboxylase inhibitor), chlorpheniramine (histamine H1 receptor antagonist), famotidine (histamine H2 receptor antagonist) and thioperamide (histamine H3 receptor antagonist) on lipopolysaccharide (LPS)-induced hypophagia in broilers were studied.
3-(1'-Cyclobutylspiro[4H-1,3-benzodioxine-2,4'-piperidine]-6-yl)-5,5-dimethyl-1,4-dihydropyridazin-6-one (CEP-32215), a new wake-promoting histamine H3 antagonist/inverse agonist.
Ator et al., West Chester, United States. In Neuropharmacology, Oct 2015
UNASSIGNED: CEP-32215 is a new, potent, selective, and orally bioavailable inverse agonist of the histamine H3 receptor (H3R) with drug-like properties.
The Effect of Subchronic Dosing of Ciproxifan and Clobenpropit on Dopamine and Histamine Levels in Rats.
Akhtar et al., New Delhi, India. In J Exp Neurosci, 2014
The present study was designed to investigate the effect of once daily for 7-day (subchronic treatment) dosing of histamine H3 receptor antagonists, ciproxifan (CPX) (3 mg/kg, i.p.), and clobenpropit (CBP) (15 mg/kg, i.p), including clozapine (CLZ) (3.0 mg/kg, i.p.) and chlorpromazine (CPZ) (3.0 mg/kg, i.p.), the atypical and typical antipsychotic, respectively, on MK-801(0.2
Histamine H3 Receptor Antagonists for Alzheimer's Disease: A Systematic Review and Meta-Analysis of Randomized Placebo-Controlled Trials.
Iwata et al., In J Alzheimers Dis, 2014
BACKGROUND: No comprehensive meta-analysis has been performed concerning the efficacy and tolerability of histamine H3 receptor antagonists (H3R-ANTs) in Alzheimer's disease patients.
Where do we stand in the field of anti-abuse drug discovery?
Tzschentke, Aachen, Germany. In Expert Opin Drug Discov, 2014
It is hoped that at least a few of the investigated approaches (e.g., various glutamate and GABA receptor modulators, nociceptin/orphanin FQ peptide receptor agonists, or histamine H3 receptor antagonists) reach the stage of clinical development and eventually reach regulatory approval.
Emerging drugs for neuropathic pain.
Dickenson et al., Kingston, Canada. In Expert Opin Emerg Drugs, 2014
These include calcium channel antagonists, vanilloid receptor antagonists, potassium channel agonists, NMDA antagonists, novel opioid receptor agonists, histamine H3 receptor antagonists, a novel sodium channel antagonist, serotonin modulators, a novel acetylcholine receptor agonist, α-2b adrenoreceptor agonist, cannabinoid CB2 receptor agonist, nitric oxide synthase inhibitor, orexin receptor antagonist, angiotensin II 2 antagonist, imidazoline I2 receptor agonist, apoptosis inhibitor and fatty acid amide hydrolase inhibitor.
Procognitive properties of drugs with single and multitargeting H3 receptor antagonist activities.
Stark et al., Belgrade, Serbia. In Cns Neurosci Ther, 2014
The histamine H3 receptor (H3 R) is an important modulator of numerous central control mechanisms.
The other side of the histamine H3 receptor.
Ghiabi et al., Wellington, New Zealand. In Trends Neurosci, 2014
Although histamine H3 receptors are predominantly known as presynaptic receptors, regulating the release of neurotransmitters such as dopamine, acetylcholine, and histamine, in the striatal complex the vast majority of these receptors are actually located on the other side, in other words postsynaptically.
Pitolisant versus placebo or modafinil in patients with narcolepsy: a double-blind, randomised trial.
HARMONY I study group et al., Montpellier, France. In Lancet Neurol, 2013
We assessed the safety and efficacy of pitolisant (previously called BF2.649), a selective histamine H3 receptor inverse agonist that activates these neurons, in patients with narcolepsy.
Preservation of cortical histamine H3 receptors in ischemic vascular and mixed dementias.
Lai et al., Singapore, Singapore. In J Neurol Sci, 2012
Histamine H3 receptor levels are unchanged in subcortical ischemic vascular dementia and mixed dementias in all brain areas studied.
The hydrophobic amino acids in putative helix 8 in carboxy-terminus of histamine H(3) receptor are involved in receptor-G-protein coupling.
Yanai et al., Sendai, Japan. In Cell Signal, 2011
The hydrophobic amino acids in putative helix 8 in carboxy-terminus of histamine H(3) receptor are involved in receptor-G-protein coupling.
The histamine H3 receptor and eating behavior.
Torrealba et al., Florence, Italy. In J Pharmacol Exp Ther, 2011
This review outlines the relevance of the histaminergic system in controlling feeding behavior and evaluates the potential role of the histamine H3 receptor as a target for regulating obesity.
A280V polymorphism in the histamine H3 receptor as a risk factor for migraine.
Trujillo-Hernández et al., Mexico. In Arch Med Res, 2011
Data suggest that V-allele genotypes in the H3 receptor gene increase inactive receptors, enhancing inhibition of negative feedback mechanism on the H3 receptor and increasing histamine release, correlating with migraine attacks in susceptible patients.
H3 histamine receptor-mediated activation of protein kinase Calpha inhibits the growth of cholangiocarcinoma in vitro and in vivo.
Alpini et al., Temple, United States. In Mol Cancer Res, 2009
Modulation of PKCalpha by histamine receptors may be important in regulating cholangiocarcinoma growth.
The histamine H3 receptor: from gene cloning to H3 receptor drugs.
de Esch et al., Amsterdam, Netherlands. In Nat Rev Drug Discov, 2005
"The human H(3)receptor gene suggested to consist of either 3 exons and 2 introns, or 4 exons and 3 introns, with ...additional exon accounting for...8 additional carboxy(C)-terminal amino some human H(3) receptor sequences"
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