| Tclin | 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]
Comments
Property Summary
| NCBI Gene PubMed Count | 47 |
| Grant Count | 23 |
| R01 Count | 18 |
| Funding | $4,034,822 |
| PubMed Score | 555.57 |
| PubTator Score | 334.43 |
| Disease | log2 FC | p |
|---|---|---|
| posterior fossa group B ependymoma | -2.300 | 0.000 |
| astrocytoma | -1.200 | 0.000 |
| glioblastoma | -1.600 | 0.000 |
| osteosarcoma | 1.374 | 0.000 |
| group 3 medulloblastoma | -2.400 | 0.002 |
| atypical teratoid/rhabdoid tumor | -1.900 | 0.000 |
| adult high grade glioma | -1.500 | 0.006 |
| pilocytic astrocytoma | -2.000 | 0.000 |
| ovarian cancer | 1.100 | 0.000 |
| pituitary cancer | 1.100 | 0.000 |
| psoriasis | 4.000 | 0.000 |
CHEMBL1923530
pKi 7.00
CHEMBL473928
pKi 7.00
CHEMBL180061
pKi 7.00
CHEMBL1170580
pKi 7.00
CHEMBL204615
pKi 7.00
CHEMBL423070
pKi 7.00
CHEMBL597879
pKi 7.00
CHEMBL560358
pKi 7.00
CHEMBL503733
pKi 7.00
CHEMBL403736
pKi 7.00
CHEMBL158518
pKi 7.00
CHEMBL361355
pKi 7.00
CHEMBL1951056
pKi 7.00
CHEMBL12160
pKd 7.00
CHEMBL351671
pKi 7.01
CHEMBL3127680
pKi 7.01
CHEMBL1688973
pKi 7.01
CHEMBL1935573
pKi 7.01
CHEMBL260374
pEC50 7.01
CHEMBL1958156
pKi 7.02
| AID | Type | Active / Inconclusive / Inactive | Description |
|---|---|---|---|
| 1788 | other |
0 / 0 / 0 | Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Ancillary Activity |
| 434974 | screening |
0 / 0 / 0 | Late-stage radioligand binding assay to identify inhibitors of NADPH oxidase 1 (NOX1): PDSP screen |
| 504381 | other |
0 / 0 / 0 | Late-stage radioligand binding assay to identify inhibitors of NADPH oxidase 1 (NOX1): PDSP screen Set 2 |
| 624355 | other |
0 / 0 / 0 | Late stage results from the probe development efforts to identify dual inhibitors of signal transducer and activator of transcription 3 (STAT3) and nuclear factor NF-kappa-B (NF-kB): Cell-based radioligand binding assay to determine the binding affinities for selected transporters, receptors, and GPCRs |
| 624406 | other |
0 / 0 / 0 | Late stage results from the probe development effort to identify inhibitors of Hepatitis C Virus (HCV) core protein dimerization: Cell-based radioligand binding assay to determine the binding affinities for selected transporters, receptors, and GPCRs |
| 686924 | other |
0 / 0 / 1 | ML347 Eurofin Panel Assay for BMP Inhibitor (Probe Compound) |
| 686925 | other |
0 / 0 / 1 | ML352 Eurofin Panel Assay for Choline Transporter Inhibitor (Probe Compound) |
| 686926 | other |
0 / 0 / 1 | ML354 Eurofin Panel Assay for PAR4 Antagonists Inhibitor (Probe Compound) |
| 686927 | other |
0 / 0 / 1 | ML353 Eurofin Panel Assay for mGlu5 SAM Inhibitor (Probe Compound) |
| 743249 | screening |
1 / 0 / 0 | Development of the First Potent, Selective and CNS penetrant M5 Negative Allosteric Modulator (NAM) |
| More... |
| PMID | Text |
|---|---|
| 26915454 | Decrease in histamine H3 receptor function was linked to epileptic activity in the hippocampus and temporal neocortex of patients with pharmacoresistant mesial temporal lobe epilepsy. |
| 25098339 | Molecular modelling studies, including molecular dynamic simulations and calculation of Gibbs energy of solvation of hH3R and hH4R, were studied. |
| 24835231 | The polymorphisms of HNMT and HRH3 were irrelevant with breast cancer in the present study. |
| 24493592 | Report synthesis/functional characterization of imbutamine analogs as histamine H3 agonists. |
| 23713487 | The A280V mutation reduces the signalling efficacy of the human H3 receptor; this effect may be relevant to the pathophysiology of disorders associated with the mutation |
| 23677734 | In this review, we focus on the role of histamine and its receptors in the treatment of Alzheimer's disease. |
| 23647606 | the anatomical localization of Hreceptors suggests a complex interaction that could both enhance and inhibit dopaminergic neurotransmission; tt is conceivable that Hreceptors can moderate the development and maintenance of drug addiction. |
| 22885137 | study identified novel functional properties in terms of voltage sensitivities and deactivation rates, which differed between the histamine hH3445, hH3365, and H4 receptors |
| 22870296 | ZEL-H16 is a novel and potent nonimidazole agonist of H3R, which might serve as a pharmacological tool for future investigations or as possible therapeutic agent of H3R. |
| 22860191 | [review] The H1, H2, and H3 receptors are all involved in recovery of neurological function when extracellular histamine is gradually increasing, after cerebral ischemia. |
| More... |
MERAPPDGPLNASGALAGEAAAAGGARGFSAAWTAVLAALMALLIVATVLGNALVMLAFVADSSLRTQNN 1 - 70 FFLLNLAISDFLVGAFCIPLYVPYVLTGRWTFGRGLCKLWLVVDYLLCTSSAFNIVLISYDRFLSVTRAV 71 - 140 SYRAQQGDTRRAVRKMLLVWVLAFLLYGPAILSWEYLSGGSSIPEGHCYAEFFYNWYFLITASTLEFFTP 141 - 210 FLSVTFFNLSIYLNIQRRTRLRLDGAREAAGPEPPPEAQPSPPPPPGCWGCWQKGHGEAMPLHRYGVGEA 211 - 280 AVGAEAGEATLGGGGGGGSVASPTSSSGSSSRGTERPRSLKRGSKPSASSASLEKRMKMVSQSFTQRFRL 281 - 350 SRDRKVAKSLAVIVSIFGLCWAPYTLLMIIRAACHGHCVPDYWYETSFWLLWANSAVNPVLYPLCHHSFR 351 - 420 RAFTKLLCPQKLKIQPHSSLEHCWK 421 - 445 //
| PMID | Year | Title |
|---|---|---|
| 26915454 | 2016 | Pharmacoresistant temporal lobe epilepsy modifies histamine turnover and H3 receptor function in the human hippocampus and temporal neocortex. |
| 25098339 | 2014 | Sodium binding to hH3R and hH 4R--a molecular modeling study. |
| 24835231 | 2014 | Associations of polymorphisms in histidine decarboxylase, histamine N-methyltransferase and histamine receptor H3 genes with breast cancer. |
| 24493592 | 2014 | Synthesis and functional characterization of imbutamine analogs as histamine H3 and H4 receptor ligands. |
| 23713487 | 2013 | A single-point mutation (Ala280Val) in the third intracellular loop alters the signalling properties of the human histamine H? receptor stably expressed in CHO-K1 cells. |
| 23677734 | 2013 | The neglected role of histamine in Alzheimer's disease. |
| 23647606 | 2013 | Histamine H? receptors, the complex interaction with dopamine and its implications for addiction. |
| 23535732 | 2013 | Identification of 23 new prostate cancer susceptibility loci using the iCOGS custom genotyping array. |
| 22885137 | 2012 | Voltage sensitivities and deactivation kinetics of histamine H? and H? receptors. |
| 22870296 | 2012 | Identification and characterization of ZEL-H16 as a novel agonist of the histamine H3 receptor. |
| More... |
