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H2 receptor

Family: Histamine receptors

Contents:
Gene and Protein Information
Previous and Unofficial Names
Database Links
Agonists
Antagonists
Transduction Mechanisms
Tissue Distribution
Expression Datasets
Functional Assays
Physiological Functions
Physiological Consequences of Altering Gene Expression
Phenotypes, Alleles and Disease Models
Biologically Significant Variants
References
Gene and Protein Information
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 359 5q35.2 HRH2 histamine receptor H2 10
Mouse 7 358 13 B1 Hrh2 histamine receptor H2 16
Rat 7 358 17p14 Hrh2 histamine receptor H 2 38
Previous and Unofficial Names
H2R
HH2R
Histamine H2 receptor
gastric receptor I
Database Links
ChEMBL Target 102 (Hs), 11297 (Mm), 11298 (Rn)
DrugBank Target 124 (Hs)
Ensembl ENSG00000113749 (Hs), ENSMUSG00000034987 (Mm), ENSRNOG00000018260 (Rn)
Entrez Gene 3274 (Hs), 15466 (Mm), 25461 (Rn)
GeneCards HRH2 (Hs)
GenitoUrinary Development Molecular Anatomy Project Hrh2 (Mm)
HomoloGene 40613 (Hs)
Human Protein Reference Database 00816 (Hs)
InterPro P25021 (Hs), P97292 (Mm), P25102 (Rn)
KEGG Gene hsa:3274 (Hs), mmu:15466 (Mm), rno:25461 (Rn)
OMIM 142703 (Hs)
PharmGKB Gene PA29457 (Hs)
PhosphoSitePlus P25021 (Hs), P97292 (Mm), P25102 (Rn)
Protein Ontology (PRO) PRO:000001423 (Hs)
RefSeq Nucleotide NM_022304 (Hs), NM_008286 (Mm), NM_012965 (Rn)
RefSeq Protein NP_071640 (Hs), NP_032312 (Mm), NP_037097 (Rn)
TreeFam ENSG00000113749 (Hs), ENSMUSG00000034987 (Mm), ENSRNOG00000018260 (Rn)
UniGene Hs. 247885 (Hs)
UniProt P25021 (Hs), P97292 (Mm), P25102 (Rn)
Wikipedia H2 receptor
Histamine receptors
Search for 3D structures on the PDB
Search by keyword: Histamine receptors H2 receptor Search by accession number: P25102, P25021, P97292
Natural/Endogenous Ligand(s)
histamine
Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
impromidine Hs Full agonist 7.2 pKi 45
arpromidine Hs Full agonist 6.3 – 8.0 pKi 45
UR-PG136 Hs Full agonist 7.0 pKi 45
UR-PG146 Hs Full agonist 6.0 pKi 45
histamine Rn Full agonist 3.8 pKi 3
amthamine Hs Full agonist 6.4 pEC50 18
burimamide Hs Full agonist 5.6 – 5.7 pEC50 1
View species-specific agonist tables
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
[125I]aminopotentidine Rn Antagonist 8.7 pKd 19
[3H]tiotidine Hs Antagonist 7.7 – 8.7 pKd 32
iodoaminopotentidine Rn Antagonist 9.2 pKi 3
tiotidine Rn Antagonist 7.5 pKi 3
ranitidine Hs Antagonist 7.1 pKi 21
ranitidine Rn Antagonist 6.2 pKi 3
cimetidine Rn Antagonist 5.9 pKi 3
metiamide Rn Antagonist 5.8 pKi 3
burimamide Rn Antagonist 5.5 pKi 42
ABT-239 Hs Inverse agonist 5.2 pKi 7
clobenpropit Hs Antagonist 5.2 pKi 8
View species-specific antagonist tables
Antagonist Comments
Nizatidine is a H2 antagonist clinically in use to block histamine-induced gastric acid secretion [33].

Explore drug-target interactions for this set of compounds using iPHACE

Primary Transduction Mechanisms
Transducer Effector/Response
Gq/G11 family Phospholipase C stimulation
References:  19,30
Secondary Transduction Mechanisms
Transducer Effector/Response
Gs family Adenylate cyclase stimulation
References:  19,30
Tissue Distribution
Mast cells.
Species:  Human
Technique:  RT-PCR.
References:  22
Gastrointestinal tract.
Species:  Human
Technique:  qRT-PCR and immunohistochemistry.
References:  40
Brain: caudate and putamen nuclei, external layers of cerebral cortex > hippocampal formation > dentate nucleus of cerebellum.
Species:  Human
Technique:  in situ hybridisation.
References:  14
Brain: cerebrum.
Heart: myocardium (atrium and ventricle).
Species:  Human
Technique:  Northern and Western blotting.
References:  26
Mast cells.
Species:  Mouse
Technique:  RT-PCR.
References:  13
Brain: cerebrum.
Heart: myocardium (atrium and ventricle).
Species:  Rat
Technique:  Northern and Western blotting.
References:  26
Cochlea.
Species:  Rat
Technique:  RT-PCR.
References:  2
Expression Datasets

Click here to show/hide data

Log average relative transcript abundance in mouse tissues measured by qPCR from Regard, J.B., Sato, I.T., and Coughlin, S.R. (2008). Anatomical profiling of G protein-coupled receptor expression. Cell, 135(3): 561-71. [PMID:18984166] [Raw data: website]

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Functional Assays
Measurement of IP levels in COS-7 cells transfected with the rat H2 receptor.
Species:  Rat
Tissue:  COS-7 cells.
Response measured:  Stimulation of IP formation.
References:  19
Measurment of cAMP levels in COS-7 cells transfected with the rat H2 receptor.
Species:  Rat
Tissue:  COS-7 cells.
Response measured:  Stimulation of cAMP accumulation.
References:  19
Measurement of Ca2+ levels in primary cultured human uterine arterial endothelial (HUAEC) cells endogenously expressing the H2 receptor.
Species:  Human
Tissue:  HUAEC cells.
Response measured:  Increase in Ca2+ concentration.
References:  44
Measurement of cAMP levels in human neutrophils endogenously expressing the H2 receptor.
Species:  Human
Tissue:  Neutrophils.
Response measured:  Stimulation of cAMP accumulation.
References:  11
Measurement of cAMP levels in human promyelocytic leukemic HL-60 cells endogenously expressing the H2 receptor.
Species:  Human
Tissue:  HL-60 cells.
Response measured:  Stimulation of cAMP accumulation.
References:  12,34
Measurement of Ca2+ levels in human HL-60 cells endogenously expressing the H2 receptor.
Species:  Human
Tissue:  HL-60 cells.
Response measured:  Ca2+ mobilisation from intracellular stores.
References:  30
Measurement of cAMP levels in mast cells endogenously expressing the H2 receptor.
Species:  Mouse
Tissue:  Mast cells.
Response measured:  Stimulation of cAMP accumulation.
References:  13
Measurement of cAMP levels in CHO cells transfected with the human H2 receptor.
Species:  Human
Tissue:  CHO cells.
Response measured:  cAMP accumulation.
References:  9,39
Physiological Functions
Stimulation of gastric acid secretion.
Species:  Rat
Tissue:  In vivo.
References:  4-5,23,37,41
Stimulation of gastric acid secretion.
Species:  Human
Tissue:  In vivo.
References:  20,27-28
Regulation of cytokine production.
Species:  Mouse
Tissue:  CD4+ and CD8+ T cells.
References:  43
Endothelium-independent vasodilation via smooth muscle H2 receptors.
Species:  Rat
Tissue:  Mesenteric vascular beds.
References:  15
Relaxation of smooth muscle.
Species:  Human
Tissue:  Isolated uterine strips.
References:  24
Inhibition of neutrophil activation.
Species:  Human
Tissue:  Neutrophils.
References:  30
Inhibition of neutrophil chemotaxis and T-lymphocyte proliferation.
Species:  Human
Tissue:  In vivo.
References:  34
Relaxation of smooth muscle.
Species:  Rat
Tissue:  Isolated uterine strips.
References:  29
Relaxation of smooth muscle.
Species:  Rat
Tissue:  Isolated stomach fundus.
References:  6
Increase in substantia nigra pars reticulata (SNr) inhibitory projection neuron firing frequency (via cell depolarisation).
The balance between the effect of H1 and H2 receptors and the opposing effect of H3 receptors may contribute to movement control.
Species:  Mouse
Tissue:  Coronal midbrain slices.
References:  47
Depolarisation of CA3 pyramidal cells.
Species:  Mouse
Tissue:  Hippocampal slices.
References:  46
Physiological Consequences of Altering Gene Expression
H2 receptor knockout mice develop normally with normal basal gastric acid levels. However they exhibit hypertrophy of gastric mucosa and an increase in the number of parietal and enterochromaffin-like (ECL) cells. Neither histamine nor gastrin stimulated gastric acid secretion in the knockout mice.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  17
H2 receptor knockout mice exhibit an increase in stomach weight, enlarged gastric folds with cystic dilatation, hypergastrinemia, hypoalbuminemia, an increase in mucus secretion and overexpression of mucosal TGFα. These symptoms resemble Menetrier's disease.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  35
H2 receptor knockout mice exhibit attenuation of the histamine-induced inhibition of the development of liver injury seen in wild-type mice.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  25
CD4+ T cells from H2 receptor knockout mice exhibit a decrease in the release of IL-2 and IL-10, and increase in IL-4 release. CD8+ T cells from H2 receptor knockout mice also exhibit a decrease in the release of IL-2 and IL-10, as well as an increase in IFN-γ release.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  43
H1 receptor knockout mice exhibit enhanced antinociception by administration of orexin-A, compared to wild-type mice following administration of orexin-A.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  31
Phenotypes, Alleles and Disease Models Mouse data from MGI

Click here to show/hide data

Allele Composition & genetic background Accession Phenotype Id Phenotype Reference
Hrh2tm1Yfks Hrh2tm1Yfks/Hrh2tm1Yfks
involves: 129S6/SvEvTac * C57BL/6		 MGI:108482  MP:0004140 abnormal chief cell morphology PMID: 12729842 
Hrh2tm1Yfks Hrh2tm1Yfks/Hrh2tm1Yfks
involves: 129S6/SvEvTac * C57BL/6		 MGI:108482  MP:0003892 abnormal gastric gland PMID: 12729842 
Hrh2tm1Wtn Hrh2tm1Wtn/Hrh2tm1Wtn
involves: 129P2/OlaHsd * C57BL/6J		 MGI:108482  MP:0005209 abnormal gastric mucosa morphology PMID: 10862789 
Hrh2tm1Wtn Hrh2tm1Wtn/Hrh2tm1Wtn
involves: 129P2/OlaHsd * C57BL/6J		 MGI:108482  MP:0004139 abnormal gastric parietal cell morphology PMID: 10862789 
Hrh2tm1Yfks Hrh2tm1Yfks/Hrh2tm1Yfks
involves: 129S6/SvEvTac * C57BL/6		 MGI:108482  MP:0004139 abnormal gastric parietal cell morphology PMID: 12729842 
Hrh2tm1Yfks Hrh2tm1Yfks/Hrh2tm1Yfks
involves: 129S6/SvEvTac * C57BL/6		 MGI:108482  MP:0004138 abnormal mucous neck cell morphology PMID: 12729842 
Hrh2tm1Yfks Hrh2tm1Yfks/Hrh2tm1Yfks
involves: 129S6/SvEvTac * C57BL/6		 MGI:108482  MP:0001650 abnormal seizure response to electrical stimulation PMID: 12729842 
Hrh2tm1Wtn Hrh2tm1Wtn/Hrh2tm1Wtn
involves: 129P2/OlaHsd * C57BL/6J		 MGI:108482  MP:0008004 abnormal stomach pH PMID: 10862789 
Hrh2tm1Wtn Hrh2tm1Wtn/Hrh2tm1Wtn
involves: 129P2/OlaHsd * C57BL/6J		 MGI:108482  MP:0000505 decreased digestive secretion PMID: 10862789 
Hrh2tm1Yfks Hrh2tm1Yfks/Hrh2tm1Yfks
involves: 129S6/SvEvTac * C57BL/6		 MGI:108482  MP:0000505 decreased digestive secretion PMID: 12729842 
Hrh2tm1Yfks Hrh2tm1Yfks/Hrh2tm1Yfks
involves: 129S6/SvEvTac * C57BL/6		 MGI:108482  MP:0003883 enlarged stomach PMID: 12729842 
Hrh2tm1Wtn Hrh2tm1Wtn/Hrh2tm1Wtn
involves: 129P2/OlaHsd * C57BL/6J		 MGI:108482  MP:0004731 increased circulating gastrin level PMID: 10862789 
Hrh2tm1Yfks Hrh2tm1Yfks/Hrh2tm1Yfks
involves: 129S6/SvEvTac * C57BL/6		 MGI:108482  MP:0004731 increased circulating gastrin level PMID: 12729842 
Hrh2tm1Yfks Hrh2tm1Yfks/Hrh2tm1Yfks
involves: 129S6/SvEvTac * C57BL/6		 MGI:108482  MP:0008006 increased stomach pH PMID: 12729842 
Hrh2tm1Wtn Hrh2tm1Wtn/Hrh2tm1Wtn
involves: 129P2/OlaHsd * C57BL/6J		 MGI:108482  MP:0005211 increased thickness of gastric mucosa PMID: 10862789 
Hrh2tm1Yfks Hrh2tm1Yfks/Hrh2tm1Yfks
involves: 129S6/SvEvTac * C57BL/6		 MGI:108482  MP:0005211 increased thickness of gastric mucosa PMID: 12729842 
Hrh2tm1Yfks Hrh2tm1Yfks/Hrh2tm1Yfks
involves: 129S6/SvEvTac * C57BL/6		 MGI:108482  MP:0002574 increased vertical activity PMID: 12729842 
Biologically Significant Variants
A 649 A -> G substitution may be linked to schizophrenia.
Type:  Single nucleotide polymorphism.
Species:  Human
References:  36

REFERENCES

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To cite this database page, please use the following:

Paul Chazot, Hiroyuki Fukui, C. Robin Ganellin, Helmut L. Haas, Stephen J. Hill, Rebecca Hills, Roberto Levi, Walter Schunack, Jean-Charles Schwartz, Nigel P. Shankley, Henk Timmerman, J. Michael Young.
Histamine receptors: H2 receptor. Last modified on 28/02/2013. Accessed on 23/05/2013. IUPHAR database (IUPHAR-DB), http://www.iuphar-db.org/DATABASE/ObjectDisplayForward?objectId=263.


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