Nomenclature: H2 receptor

Family: Histamine receptors

Annotation status:  image of a green circle Annotated and expert reviewed. Please contact us if you can help with updates. 

Contents

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 11
Mouse 7 358 13 B1 Hrh2 histamine receptor H2 18
Rat 7 358 17p14 Hrh2 histamine receptor H 2 40
Previous and Unofficial Names
H2R
HH2R
Histamine H2 receptor
gastric receptor I
Database Links
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
GPCRDB
GeneCards
GenitoUrinary Development Molecular Anatomy Project
HomoloGene
Human Protein Reference Database
InterPro
KEGG Gene
OMIM
PharmGKB Gene
PhosphoSitePlus
Protein Ontology (PRO)
RefSeq Nucleotide
RefSeq Protein
TreeFam
UniGene Hs.
UniProtKB
Wikipedia
Natural/Endogenous Ligands
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 47
pKi 7.2 [47]
arpromidine Hs Full agonist 6.3 – 8.0 pKi 47
pKi 6.3 – 8.0 [47]
UR-PG136 Hs Full agonist 7.0 pKi 47
pKi 7.0 [47]
UR-PG146 Hs Full agonist 6.0 pKi 47
pKi 6.0 [47]
histamine Rn Full agonist 3.8 pKi 3
pKi 3.8 [3]
amthamine Hs Full agonist 6.4 pEC50 20
pEC50 6.4 (EC50 4.5x10-7 M) [20]
burimamide Hs Full agonist 5.6 – 5.7 pEC50 1
pEC50 5.6 – 5.7 [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 21
pKd 8.7 (Kd 2x10-9 M) [21]
[3H]tiotidine Hs Antagonist 7.7 – 8.7 pKd 34
pKd 7.7 – 8.7 (Kd 2.2x10-9 – 2x10-8 M) [34]
iodoaminopotentidine Rn Antagonist 9.2 pKi 3
pKi 9.2 [3]
tiotidine Rn Antagonist 7.5 pKi 3
pKi 7.5 [3]
ranitidine Hs Antagonist 7.1 pKi 23
pKi 7.1 [23]
cimetidine Hs Antagonist 6.85 pKi 6
pKi 6.85 (Ki 1.4x10-7 M) [6]
ranitidine Rn Antagonist 6.2 pKi 3
pKi 6.2 [3]
cimetidine Rn Antagonist 5.9 pKi 3
pKi 5.9 [3]
metiamide Rn Antagonist 5.8 pKi 3
pKi 5.8 [3]
burimamide Rn Antagonist 5.5 pKi 44
pKi 5.5 [44]
clobenpropit Hs Antagonist 5.2 pKi 9
pKi 5.2 [9]
ABT-239 Hs Inverse agonist 5.2 pKi 8
pKi 5.2 [8]
famotidine Hs Antagonist - -
View species-specific antagonist tables
Antagonist Comments
Nizatidine is a H2 antagonist clinically in use to block histamine-induced gastric acid secretion [35].
Famotidine is also a selective H2 antagonist. The only affinity data, in free access journals, found to date relates to the canine H2 receptor, where famotidine has an IC50 of 26.3nM [17].
Primary Transduction Mechanisms
Transducer Effector/Response
Gq/G11 family Phospholipase C stimulation
References:  21,32
Secondary Transduction Mechanisms
Transducer Effector/Response
Gs family Adenylate cyclase stimulation
References:  21,32
Tissue Distribution
Mast cells.
Species:  Human
Technique:  RT-PCR.
References:  24
Brain: cerebrum.
Heart: myocardium (atrium and ventricle).
Species:  Human
Technique:  Northern and Western blotting.
References:  28
Gastrointestinal tract.
Species:  Human
Technique:  qRT-PCR and immunohistochemistry.
References:  42
Brain: caudate and putamen nuclei, external layers of cerebral cortex > hippocampal formation > dentate nucleus of cerebellum.
Species:  Human
Technique:  in situ hybridisation.
References:  15
Mast cells.
Species:  Mouse
Technique:  RT-PCR.
References:  14
Cochlea.
Species:  Rat
Technique:  RT-PCR.
References:  2
Brain: cerebrum.
Heart: myocardium (atrium and ventricle).
Species:  Rat
Technique:  Northern and Western blotting.
References:  28
Expression Datasets

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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:  21
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:  21
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:  46
Measurement of cAMP levels in human neutrophils endogenously expressing the H2 receptor.
Species:  Human
Tissue:  Neutrophils.
Response measured:  Stimulation of cAMP accumulation.
References:  12
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:  13,36
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:  32
Measurement of cAMP levels in mast cells endogenously expressing the H2 receptor.
Species:  Mouse
Tissue:  Mast cells.
Response measured:  Stimulation of cAMP accumulation.
References:  14
Measurement of cAMP levels in CHO cells transfected with the human H2 receptor.
Species:  Human
Tissue:  CHO cells.
Response measured:  cAMP accumulation.
References:  10,41
Physiological Functions
Stimulation of gastric acid secretion.
Species:  Rat
Tissue:  In vivo.
References:  4-5,25,39,43
Stimulation of gastric acid secretion.
Species:  Human
Tissue:  In vivo.
References:  22,29-30
Endothelium-independent vasodilation via smooth muscle H2 receptors.
Species:  Rat
Tissue:  Mesenteric vascular beds.
References:  16
Relaxation of smooth muscle.
Species:  Human
Tissue:  Isolated uterine strips.
References:  26
Inhibition of neutrophil activation.
Species:  Human
Tissue:  Neutrophils.
References:  32
Inhibition of neutrophil chemotaxis and T-lymphocyte proliferation.
Species:  Human
Tissue:  In vivo.
References:  36
Relaxation of smooth muscle.
Species:  Rat
Tissue:  Isolated uterine strips.
References:  31
Relaxation of smooth muscle.
Species:  Rat
Tissue:  Isolated stomach fundus.
References:  7
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:  49
Depolarisation of CA3 pyramidal cells.
Species:  Mouse
Tissue:  Hippocampal slices.
References:  48
Regulation of cytokine production.
Species:  Mouse
Tissue:  CD4+ and CD8+ T cells.
References:  45
Physiological Consequences of Altering Gene Expression
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:  45
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:  19
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:  37
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:  27
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:  33
Phenotypes, Alleles and Disease Models Mouse data from MGI

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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
Type:  Single nucleotide polymorphism.
Species:  Human
Description:  A 649 A -> G substitution may be linked to schizophrenia.
References:  38
Available Assays
DiscoveRx PathHunter® CHO-K1 HRH2 β-Arrestin Cell Line (Cat no. 93-0208C2)
PathHunter® eXpress HRH2 CHO-K1 β-Arrestin GPCR Assay (Cat no. 93-0208E2CP0M)
more info

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 30/04/2014. Accessed on 23/10/2014. IUPHAR database (IUPHAR-DB), http://www.iuphar-db.org/DATABASE/ObjectDisplayForward?objectId=263.

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