H<sub>2</sub> receptor | Histamine receptors | IUPHAR/BPS Guide to PHARMACOLOGY

H2 receptor

Target id: 263

Nomenclature: H2 receptor

Family: Histamine receptors

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   GtoImmuPdb view: OFF :     H2 receptor has curated GtoImmuPdb data

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 12
Mouse 7 358 13 B1 Hrh2 histamine receptor H2 20
Rat 7 358 17p14 Hrh2 histamine receptor H 2 45
Previous and Unofficial Names
H2R | HH2R | gastric receptor I
Database Links
Specialist databases
GPCRDB hrh2_human (Hs), hrh2_mouse (Mm), hrh2_rat (Rn)
Other databases
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Natural/Endogenous Ligands
histamine

Download all structure-activity data for this target as a CSV file

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 52
pKi 7.2 [52]
arpromidine Hs Full agonist 6.3 – 8.0 pKi 52
pKi 6.3 – 8.0 [52]
oxo-arpromidine Hs Full agonist 7.0 pKi 52
pKi 7.0 [52]
UR-PG146 Hs Full agonist 6.0 pKi 52
pKi 6.0 [52]
ST-1006 Hs Agonist <6.0 pKi 42
pKi <6.0 (Ki >1x10-6 M) [42]
histamine Rn Full agonist 3.8 pKi 3
pKi 3.8 [3]
amthamine Hs Full agonist 6.4 pEC50 22
pEC50 6.4 (EC50 4.5x10-7 M) [22]
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]iodoaminopotentidine Rn Antagonist 8.7 pKd 23
pKd 8.7 (Kd 2x10-9 M) [23]
[3H]tiotidine Hs Antagonist 7.7 – 8.7 pKd 37
pKd 7.7 – 8.7 (Kd 2x10-8 – 2.2x10-9 M) [37]
iodoaminopotentidine Rn Antagonist 9.2 pKi 3
pKi 9.2 [3]
tiotidine Rn Antagonist 7.5 pKi 3
pKi 7.5 (Ki 3.16x10-8 M) [3]
ranitidine Hs Antagonist 7.1 pKi 25
pKi 7.1 (Ki 7.94x10-8 M) [25]
cimetidine Hs Antagonist 6.8 pKi 6
pKi 6.8 (Ki 1.4x10-7 M) [6]
ranitidine Rn Antagonist 6.2 pKi 3
pKi 6.2 (Ki 6.31x10-7 M) [3]
JNJ-39758979 Hs Antagonist <6.0 pKi 42
pKi <6.0 (Ki >1x10-6 M) [42]
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 49
pKi 5.5 [49]
INCB-38579 Hs Antagonist <5.3 pKi 42
pKi <5.3 (Ki >1x10-5 M) [42]
ABT-239 Hs Inverse agonist 5.2 pKi 8
pKi 5.2 [8]
clobenpropit Hs Antagonist 5.2 pKi 9
pKi 5.2 [9]
ciproxifan Hs Antagonist <5.0 pKi 42
pKi <5.0 (Ki >1x10-5 M) [42]
MK-0249 Hs Antagonist <5.0 pKi 42
pKi <5.0 (Ki >1x10-5 M) [42]
conessine Hs Antagonist <5.0 pKi 42
pKi <5.0 (Ki >1x10-5 M) [42]
pitolisant Hs Antagonist 5.0 pKi 42
pKi 5.0 [42]
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 [38].
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 [19].
Immunopharmacology Comments
Histamine action via the H2 receptor inhibits eosinophil, mast cell and neutrophil chemotaxis, IL-12 production by dendritic cells and also suppresses Th2 cells and cytokine formation. In airway inflammation the H2 receptor mediates bronchial smooth muscle relaxation, vasodilation and mucus production [43].
Cell Type Associations
Immuno Cell Type:  Granulocytes
Cell Ontology Term:   eosinophil (CL:0000771)
Comment:  Eosinophils express all four histamine receptor subtypes.
References:  15,34
Immuno Cell Type:  Mast cells
Cell Ontology Term:   mast cell (CL:0000097)
Comment:  In humans, mast cells express H1R, H2R and H4R.
References:  11
Primary Transduction Mechanisms
Transducer Effector/Response
Gq/G11 family Phospholipase C stimulation
References:  23,35
Secondary Transduction Mechanisms
Transducer Effector/Response
Gs family Adenylate cyclase stimulation
References:  23,35
Tissue Distribution
Mast cells.
Species:  Human
Technique:  RT-PCR.
References:  26
Gastrointestinal tract.
Species:  Human
Technique:  qRT-PCR and immunohistochemistry.
References:  47
Brain: caudate and putamen nuclei, external layers of cerebral cortex > hippocampal formation > dentate nucleus of cerebellum.
Species:  Human
Technique:  in situ hybridisation.
References:  17
Brain: cerebrum.
Heart: myocardium (atrium and ventricle).
Species:  Human
Technique:  Northern and Western blotting.
References:  30
Mast cells.
Species:  Mouse
Technique:  RT-PCR.
References:  16
Brain: cerebrum.
Heart: myocardium (atrium and ventricle).
Species:  Rat
Technique:  Northern and Western blotting.
References:  30
Cochlea.
Species:  Rat
Technique:  RT-PCR.
References:  2
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:  23
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:  23
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:  51
Measurement of cAMP levels in human neutrophils endogenously expressing the H2 receptor.
Species:  Human
Tissue:  Neutrophils.
Response measured:  Stimulation of cAMP accumulation.
References:  13
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:  14,39
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:  35
Measurement of cAMP levels in mast cells endogenously expressing the H2 receptor.
Species:  Mouse
Tissue:  Mast cells.
Response measured:  Stimulation of cAMP accumulation.
References:  16
Measurement of cAMP levels in CHO cells transfected with the human H2 receptor.
Species:  Human
Tissue:  CHO cells.
Response measured:  cAMP accumulation.
References:  10,46
Physiological Functions
Stimulation of gastric acid secretion.
Species:  Rat
Tissue:  In vivo.
References:  4-5,27,44,48
Stimulation of gastric acid secretion.
Species:  Human
Tissue:  In vivo.
References:  24,31-32
Endothelium-independent vasodilation via smooth muscle H2 receptors.
Species:  Rat
Tissue:  Mesenteric vascular beds.
References:  18
Relaxation of smooth muscle.
Species:  Human
Tissue:  Isolated uterine strips.
References:  28
Inhibition of neutrophil activation.
Species:  Human
Tissue:  Neutrophils.
References:  35
Inhibition of neutrophil chemotaxis and T-lymphocyte proliferation.
Species:  Human
Tissue:  In vivo.
References:  39
Relaxation of smooth muscle.
Species:  Rat
Tissue:  Isolated uterine strips.
References:  33
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:  54
Depolarisation of CA3 pyramidal cells.
Species:  Mouse
Tissue:  Hippocampal slices.
References:  53
Regulation of cytokine production.
Species:  Mouse
Tissue:  CD4+ and CD8+ T cells.
References:  50
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:  21
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:  40
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:  29
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:  50
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:  36
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:  41

References

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1. Alewijnse AE, Smit MJ, Hoffmann M, Verzijl D, Timmerman H, Leurs R. (1998) Constitutive activity and structural instability of the wild-type human H2 receptor. J Neurochem, 71: 799-807. [PMID:9681472]

2. Azuma H, Sawada S, Takeuchi S, Higashiyama K, Kakigi A, Takeda T. (2003) Expression of mRNA encoding the H1, H2, and H3 histamine receptors in the rat cochlea. Neuroreport, 14: 423-425. [PMID:12634496]

3. Beukers MW, Klaassen CH, De Grip WJ, Verzijl D, Timmerman H, Leurs R. (1997) Heterologous expression of rat epitope-tagged histamine H2 receptors in insect Sf9 cells. Br J Pharmacol, 122: 867-874. [PMID:9384502]

4. Borella LE, Lippmann W. (1978) A relatively specific and quantitative assay for histamine H2-receptor blocking activity by determination of inhibition of histamine-induced gastric acid secretion in the rat. Eur J Pharmacol, 52: 153-159. [PMID:32047]

5. Brimblecombe RW, Duncan WA, Durant GJ, Emmett JC, Ganellin CR, Leslie GB, Parsons ME. (1978) Characterization and development of cimetidine as a histamine H2-receptor antagonist. Gastroenterology, 74: 339-347. [PMID:23336]

6. Cappelli A, Manini M, Valenti S, Castriconi F, Giuliani G, Anzini M, Brogi S, Butini S, Gemma S, Campiani G et al.. (2013) Synthesis and structure-activity relationship studies in serotonin 5-HT1A receptor agonists based on fused pyrrolidone scaffolds. Eur. J. Med. Chem., 63: 85-94. [PMID:23466604]

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8. Esbenshade TA, Fox GB, Krueger KM, Miller TR, Kang CH, Denny LI, Witte DG, Yao BB, Pan L, Wetter J, Marsh K, Bennani YL, Cowart MD, Sullivan JP, Hancock AA. (2005) Pharmacological properties of ABT-239 [4-(2-{2-[(2R)-2-Methylpyrrolidinyl]ethyl}-benzofuran-5-yl)benzonitrile]: I. Potent and selective histamine H3 receptor antagonist with drug-like properties. J Pharmacol Exp Ther, 313: 165-175. [PMID:15608078]

9. Esbenshade TA, Krueger KM, Miller TR, Kang CH, Denny LI, Witte DG, Yao BB, Fox GB, Faghih R, Bennani YL, Williams M, Hancock AA. (2003) Two novel and selective nonimidazole histamine H3 receptor antagonists A-304121 and A-317920: I. In vitro pharmacological effects. J Pharmacol Exp Ther, 305: 887-896. [PMID:12606603]

10. Fukushima Y, Otsuka H, Ishikawa M, Asano T, Anai M, Katsube T, Ogawa K, Kajiwara T, Ohkawa S, Ishikawa T, Omata M, Saitoh T. (2001) Potent and long-lasting action of lafutidine on the human histamine H(2) receptor. Digestion, 64: 155-160. [PMID:11786663]

11. Gangwar RS, Landolina N, Arpinati L, Levi-Schaffer F. (2017) Mast cell and eosinophil surface receptors as targets for anti-allergic therapy. Pharmacol. Ther., 170: 37-63. [PMID:27773785]

12. Gantz I, Munzert G, Tashiro T, Schaffer M, Wang L, Yamada T. (1991) Molecular cloning of the human histamine H2-receptor. Biochem. Biophys. Res. Commun., 178: 1386-1392. [PMID:1714721]

13. Gespach C, Abita JP. (1982) Human polymorphonuclear neutrophils. Pharmacological characterization of histamine receptors mediating the elevation of cyclic AMP. Mol Pharmacol, 21: 78-85. [PMID:6127623]

14. Gespach C, Saal F, Cost H, Abita JP. (1982) Identification and characterization of surface receptors for histamine in the human promyelocytic leukemia cell line HL-60. Comparison with human peripheral neutrophils. Mol Pharmacol, 22: 547-553. [PMID:6185835]

15. Gibbs BF, Levi-Schaffer F. (2012) H₄ receptors in mast cells and basophils: a new therapeutic target for allergy?. Front Biosci (Landmark Ed), 17: 430-7. [PMID:22201753]

16. Hofstra CL, Desai PJ, Thurmond RL, Fung-Leung WP. (2003) Histamine H4 receptor mediates chemotaxis and calcium mobilization of mast cells. J Pharmacol Exp Ther, 305: 1212-1221. [PMID:12626656]

17. Honrubia MA, Vilaro MT, Palacios JM, Mengod G. (2000) Distribution of the histamine H(2) receptor in monkey brain and its mRNA localization in monkey and human brain. Synapse, 38: 343-354. [PMID:11020238]

18. Jin H, Koyama T, Hatanaka Y, Akiyama S, Takayama F, Kawasaki H. (2006) Histamine-induced vasodilation and vasoconstriction in the mesenteric resistance artery of the rat. Eur J Pharmacol, 529: 136-144. [PMID:16337938]

19. Kaku S, Isobe Y, Kiuchi Y, Tanaka M, Muramatsu M, Higuchi S. (1999) Interaction of the new histamine H2-receptor antagonist pibutidine hydrochloride with canine cloned H2-receptor expressed cells. Arzneimittelforschung, 49 (1): 67-71. [PMID:10028383]

20. Kobayashi T, Inoue I, Jenkins NA, Gilbert DJ, Copeland NG, Watanabe T. (1996) Cloning, RNA expression, and chromosomal location of a mouse histamine H2 receptor gene. Genomics, 37: 390-394. [PMID:8938453]

21. Kobayashi T, Tonai S, Ishihara Y, Koga R, Okabe S, Watanabe T. (2000) Abnormal functional and morphological regulation of the gastric mucosa in histamine H2 receptor-deficient mice. J Clin Invest, 105: 1741-1749. [PMID:10862789]

22. Kraus A, Ghorai P, Birnkammer T, Schnell D, Elz S, Seifert R, Dove S, Bernhardt G, Buschauer A. (2009) N(G)-acylated aminothiazolylpropylguanidines as potent and selective histamine H(2) receptor agonists. ChemMedChem, 4 (2): 232-40. [PMID:19072936]

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24. Leth R, Elander B, Haglund U, Olbe L, Fellenius E. (1987) Histamine H2-receptor of human and rabbit parietal cells. Am J Physiol, 253: G497-G501. [PMID:3661710]

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26. Lippert U, Artuc M, Grützkau A, Babina M, Guhl S, Haase I, Blaschke V, Zachmann K, Knosalla M, Middel P, Krüger-Krasagakis S, Henz BM. (2004) Human skin mast cells express H2 and H4, but not H3 receptors. J Invest Dermatol, 123: 116-123. [PMID:15191551]

27. Main IH, Whittle BJ. (1976) A study of the vascular and acid-secretory responses of the rat gastric mucosa to histamine. J Physiol, 257: 407-418. [PMID:950600]

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29. Masaki T, Chiba S, Tatsukawa H, Noguchi H, Kakuma T, Endo M, Seike M, Watanabe T, Yoshimatsu H. (2005) The role of histamine H1 receptor and H2 receptor in LPS-induced liver injury. FASEB J, 19: 1245-1252. [PMID:16051691]

30. Matsuda N, Jesmin S, Takahashi Y, Hatta E, Kobayashi M, Matsuyama K, Kawakami N, Sakuma I, Gando S, Fukui H, Hattori Y, Levi R. (2004) Histamine H1 and H2 receptor gene and protein levels are differentially expressed in the hearts of rodents and humans. J Pharmacol Exp Ther, 309: 786-795. [PMID:14752062]

31. McIsaac RL, Johnston BJ, Flannery MC. (1983) Dose-response curve analysis of gastric secretory responses in the dog and man to impromidine: a new histamine-H2-receptor agonist. J Pharmacol Exp Ther, 225: 186-190. [PMID:6131998]

32. McIsaac RL, Johnston BJ, Flannery MC, Fielding LP. (1982) Gastric acid secretion induced by impromidine in the dog and man: analysis of dose-response relationships. Agents Actions, 12: 166-167. [PMID:6211064]

33. McNeill JH, Verma SC. (1975) Histamine2 receptors in rat uterus. Res Commun Chem Pathol Pharmacol, 11: 639-644. [PMID:1179032]

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35. Mitsuhashi M, Mitsuhashi T, Payan DG. (1989) Multiple signaling pathways of histamine H2 receptors. Identification of an H2 receptor-dependent Ca2+ mobilization pathway in human HL-60 promyelocytic leukemia cells. J Biol Chem, 264: 18356-18362. [PMID:2553705]

36. Mobarakeh JI, Takahashi K, Sakurada S, Nishino S, Watanabe H, Kato M, Naghdi N, Yanai K. (2005) Enhanced antinociception by intracerebroventricularly administered orexin A in histamine H1 or H2 receptor gene knockout mice. Pain, 118: 254-262. [PMID:16202530]

37. Monczor F, Fernandez N, Legnazzi BL, Riveiro ME, Baldi A, Shayo C, Davio C. (2003) Tiotidine, a histamine H2 receptor inverse agonist that binds with high affinity to an inactive G-protein-coupled form of the receptor. Experimental support for the cubic ternary complex model. Mol. Pharmacol., 64 (2): 512-20. [PMID:12869657]

38. Morton DM. (1987) Pharmacology and toxicology of nizatidine. Scand J Gastroenterol Suppl, 136: 1-8. [PMID:2892249]

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40. Ogawa T, Maeda K, Tonai S, Kobayashi T, Watanabe T, Okabe S. (2003) Utilization of knockout mice to examine the potential role of gastric histamine H2-receptors in Menetrier's disease. J Pharmacol Sci, 91: 61-70. [PMID:12686732]

41. Orange PR, Heath PR, Wright SR, Ramchand CN, Kolkeiwicz L, Pearson RC. (1996) Individuals with schizophrenia have an increased incidence of the H2R649G allele for the histamine H2 receptor gene. Mol Psychiatry, 1: 466-469. [PMID:9154248]

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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 20/02/2018. Accessed on 18/11/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=263.