Page last updated: 2024-08-05 15:16:11
H2-receptor antagonist
H2-receptor antagonists are the drugs that selectively bind to but do not activate histamine H2 receptors, thereby blocking the actions of endogenous histamine.
ChEBI ID: 37961
Members (10)
| Member | Definition | Class |
|---|---|---|
| aminopotentidine | A benzamide obtained by formal condensation of the carboxy group of 4-aminobenzoic acid with the primary amino group of 1-(2-aminoethyl)-2-cyano-3-{3-[3-(piperidin-1-ylmethyl)phenoxy]propyl}guanidine. | aminopotentidine |
| cimetidine | A member of the class of guanidines that consists of guanidine carrying a methyl substituent at position 1, a cyano group at position 2 and a 2-{[(5-methyl-1H-imidazol-4-yl)methyl]sulfanyl}ethyl group at position 3. It is a H2-receptor antagonist that inhibits the production of acid in stomach. | cimetidine |
| famotidine | famotidine | |
| famotidine | famotidine | |
| loxtidine | A triazole that consists of 1,2,4-triazole bearing a methyl substituent at position 1, a hydroxymethyl substituent at position 3 and a {3-[3-(piperidin-1-ylmethyl)phenoxy]propyl}amino group at position 5. A highly potent and selective H2-receptor antagonist. | loxtidine |
| nizatidine | A member of the class of 1,3-thiazoles having a dimethylaminomethyl substituent at position 2 and an alkylthiomethyl moiety at position 4. | nizatidine |
| oxmetidine | A 2-aminopyrimidin-4(1H)-one derivative bearing a 1,3-benzodioxol-5-ylmethyl group at the 5-position and with a 4-(5-methyl-(1H)imidazol-4-yl)-3-thiabutyl substituent attached to the 2-amino group. It is a specific histamine H2-receptor antagonist. | oxmetidine |
| pibutidine | An aromtic ether that is 4-(piperidin-1-ylmethyl)pyridin-2-ol in which the hydroxy group has been substituted by a {(2Z)-4-[(2-amino-3,4-dioxocyclobut-1-en-1-yl)amino]but-2-en-1-yl}oxy group. It is a H2 receptor antagonist which was developed for the treatment of peptic ulcers and duodenal ulcers. | pibutidine |
| pibutidine hydrochloride | The hydrochloride salt of pibutidine. It is a H2 receptor antagonist which was developed for the treatment of peptic ulcers and duodenal ulcers. It was in phase III clinical trials in Japan (now discontinued). | pibutidine hydrochloride |
| ranitidine | A member of the class of furans used to treat peptic ulcer disease (PUD) and gastroesophageal reflux disease. | ranitidine |
Research
Studies (13,719)
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 6,988 (50.94) | 18.7374 |
| 1990's | 3,708 (27.03) | 18.2507 |
| 2000's | 1,795 (13.08) | 29.6817 |
| 2010's | 927 (6.76) | 24.3611 |
| 2020's | 301 (2.19) | 2.80 |
Study Types
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 3,989 (23.86%) | 5.53% |
| Reviews | 998 (5.97%) | 6.00% |
| Case Studies | 1,507 (9.01%) | 4.05% |
| Observational | 7 (0.04%) | 0.25% |
| Other | 10,218 (61.12%) | 84.16% |
Protein Targets (120)
Potency Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| acetylcholinesterase | Homo sapiens (human) | Potency | 18.3080 | 3 | 8 |
| alpha-galactosidase | Homo sapiens (human) | Potency | 22.3872 | 1 | 1 |
| apical membrane antigen 1, AMA1 | Plasmodium falciparum 3D7 | Potency | 15.8489 | 1 | 1 |
| AR protein | Homo sapiens (human) | Potency | 27.0409 | 3 | 5 |
| aryl hydrocarbon receptor | Homo sapiens (human) | Potency | 11.8832 | 1 | 1 |
| arylsulfatase A | Homo sapiens (human) | Potency | 6.3096 | 1 | 1 |
| ATP-dependent phosphofructokinase | Trypanosoma brucei brucei TREU927 | Potency | 25.5410 | 1 | 3 |
| Bloom syndrome protein isoform 1 | Homo sapiens (human) | Potency | 0.0016 | 2 | 2 |
| Cellular tumor antigen p53 | Homo sapiens (human) | Potency | 60.5715 | 1 | 1 |
| Chain A, Cruzipain | Trypanosoma cruzi | Potency | 12.9244 | 2 | 2 |
| Chain A, HADH2 protein | Homo sapiens (human) | Potency | 3.1623 | 1 | 1 |
| Chain A, JmjC domain-containing histone demethylation protein 3A | Homo sapiens (human) | Potency | 22.3872 | 1 | 1 |
| Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASE | Homo sapiens (human) | Potency | 21.1613 | 2 | 2 |
| Chain B, HADH2 protein | Homo sapiens (human) | Potency | 3.1623 | 1 | 1 |
| chromobox protein homolog 1 | Homo sapiens (human) | Potency | 89.1251 | 1 | 1 |
| cytochrome P450 2C19 precursor | Homo sapiens (human) | Potency | 35.7168 | 1 | 2 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 13.8029 | 1 | 1 |
| cytochrome P450 2D6 | Homo sapiens (human) | Potency | 16.5196 | 1 | 4 |
| cytochrome P450 3A4 isoform 1 | Homo sapiens (human) | Potency | 20.4839 | 2 | 4 |
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 20.1833 | 1 | 3 |
| DNA polymerase iota isoform a (long) | Homo sapiens (human) | Potency | 49.5626 | 1 | 2 |
| DNA polymerase kappa isoform 1 | Homo sapiens (human) | Potency | 28.1838 | 1 | 1 |
| estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 22.9543 | 4 | 6 |
| estrogen receptor 2 (ER beta) | Homo sapiens (human) | Potency | 15.3553 | 1 | 1 |
| estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 17.7966 | 2 | 2 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 7.5309 | 1 | 5 |
| EWS/FLI fusion protein | Homo sapiens (human) | Potency | 16.3600 | 3 | 3 |
| G | Vesicular stomatitis virus | Potency | 13.8029 | 1 | 1 |
| GABA theta subunit | Rattus norvegicus (Norway rat) | Potency | 20.4839 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit alpha-1 | Rattus norvegicus (Norway rat) | Potency | 20.4839 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | Potency | 20.4839 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | Potency | 20.4839 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | Potency | 20.4839 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit alpha-5 | Rattus norvegicus (Norway rat) | Potency | 20.4839 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | Potency | 20.4839 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit beta-1 | Rattus norvegicus (Norway rat) | Potency | 20.4839 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit beta-2 | Rattus norvegicus (Norway rat) | Potency | 20.4839 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit beta-3 | Rattus norvegicus (Norway rat) | Potency | 20.4839 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit delta | Rattus norvegicus (Norway rat) | Potency | 20.4839 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit epsilon | Rattus norvegicus (Norway rat) | Potency | 20.4839 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit gamma-1 | Rattus norvegicus (Norway rat) | Potency | 20.4839 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit gamma-2 | Rattus norvegicus (Norway rat) | Potency | 20.4839 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit gamma-3 | Rattus norvegicus (Norway rat) | Potency | 20.4839 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit pi | Rattus norvegicus (Norway rat) | Potency | 20.4839 | 1 | 2 |
| geminin | Homo sapiens (human) | Potency | 0.3362 | 2 | 2 |
| GLS protein | Homo sapiens (human) | Potency | 4.9316 | 1 | 3 |
| histone acetyltransferase KAT2A isoform 1 | Homo sapiens (human) | Potency | 17.7828 | 1 | 1 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 13.8029 | 1 | 1 |
| hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor) | Homo sapiens (human) | Potency | 3.9811 | 2 | 2 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 13.8029 | 1 | 2 |
| Inositol monophosphatase 1 | Rattus norvegicus (Norway rat) | Potency | 5.0119 | 1 | 1 |
| Interferon beta | Homo sapiens (human) | Potency | 7.9518 | 2 | 2 |
| interleukin 8 | Homo sapiens (human) | Potency | 66.8242 | 1 | 1 |
| lamin isoform A-delta10 | Homo sapiens (human) | Potency | 2.2049 | 1 | 5 |
| M-phase phosphoprotein 8 | Homo sapiens (human) | Potency | 33.5875 | 1 | 1 |
| muscarinic acetylcholine receptor M1 | Rattus norvegicus (Norway rat) | Potency | 7.9690 | 1 | 2 |
| NFKB1 protein, partial | Homo sapiens (human) | Potency | 0.7079 | 2 | 2 |
| nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 11.5788 | 1 | 1 |
| peripheral myelin protein 22 | Rattus norvegicus (Norway rat) | Potency | 4.9598 | 2 | 3 |
| peripheral myelin protein 22 isoform 1 | Homo sapiens (human) | Potency | 95.2834 | 1 | 1 |
| phosphopantetheinyl transferase | Bacillus subtilis | Potency | 54.6588 | 1 | 3 |
| progesterone receptor | Homo sapiens (human) | Potency | 14.9250 | 2 | 2 |
| RAR-related orphan receptor gamma | Mus musculus (house mouse) | Potency | 27.7635 | 2 | 3 |
| serine/threonine-protein kinase PLK1 | Homo sapiens (human) | Potency | 23.7781 | 1 | 1 |
| Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 17.7828 | 1 | 1 |
| survival motor neuron protein isoform d | Homo sapiens (human) | Potency | 8.9672 | 1 | 3 |
| TDP1 protein | Homo sapiens (human) | Potency | 33.4983 | 1 | 1 |
| thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 13.7170 | 2 | 6 |
| USP1 protein, partial | Homo sapiens (human) | Potency | 17.7828 | 1 | 1 |
| vitamin D (1,25- dihydroxyvitamin D3) receptor | Homo sapiens (human) | Potency | 24.3162 | 1 | 1 |
| vitamin D3 receptor isoform VDRA | Homo sapiens (human) | Potency | 22.3872 | 1 | 1 |
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Acetylcholinesterase | Homo sapiens (human) | IC50 | 5.6146 | 1 | 1 |
| Aldehyde oxidase | Homo sapiens (human) | Ki | 155.0000 | 1 | 1 |
| ATP-binding cassette sub-family C member 3 | Homo sapiens (human) | IC50 | 133.0000 | 1 | 2 |
| ATP-dependent translocase ABCB1 | Homo sapiens (human) | IC50 | 50.0000 | 3 | 3 |
| ATP-dependent translocase ABCB1 | Mus musculus (house mouse) | IC50 | 50.0000 | 4 | 4 |
| Bile salt export pump | Homo sapiens (human) | IC50 | 458.8750 | 4 | 8 |
| Bile salt export pump | Rattus norvegicus (Norway rat) | IC50 | 1,000.0000 | 1 | 1 |
| Canalicular multispecific organic anion transporter 1 | Homo sapiens (human) | IC50 | 133.0000 | 1 | 2 |
| Carbonic anhydrase 1 | Homo sapiens (human) | Ki | 28.4408 | 2 | 3 |
| Carbonic anhydrase 12 | Homo sapiens (human) | Ki | 0.0453 | 1 | 1 |
| Carbonic anhydrase 13 | Homo sapiens (human) | Ki | 0.1715 | 1 | 1 |
| Carbonic anhydrase 14 | Homo sapiens (human) | Ki | 0.6772 | 1 | 1 |
| Carbonic anhydrase 2 | Homo sapiens (human) | Ki | 28.1526 | 2 | 3 |
| Carbonic anhydrase 3 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| Carbonic anhydrase 4 | Homo sapiens (human) | Ki | 0.9388 | 1 | 1 |
| Carbonic anhydrase 5A, mitochondrial | Homo sapiens (human) | Ki | 1.4295 | 1 | 1 |
| Carbonic anhydrase 5B, mitochondrial | Homo sapiens (human) | Ki | 5.3282 | 1 | 1 |
| Carbonic anhydrase 6 | Homo sapiens (human) | Ki | 0.0982 | 1 | 1 |
| Carbonic anhydrase 7 | Homo sapiens (human) | Ki | 0.0030 | 1 | 1 |
| Carbonic anhydrase 9 | Homo sapiens (human) | Ki | 0.1263 | 1 | 1 |
| cGMP-specific 3',5'-cyclic phosphodiesterase | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| Cytochrome P450 2C9 | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| Cytochrome P450 2D6 | Homo sapiens (human) | Ki | 77.0000 | 1 | 1 |
| Cytochrome P450 2J2 | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| Cytochrome P450 3A4 | Homo sapiens (human) | IC50 | 507.5000 | 2 | 2 |
| Histamine H2 receptor | Cavia porcellus (domestic guinea pig) | IC50 | 1.0200 | 1 | 1 |
| Histamine H2 receptor | Homo sapiens (human) | IC50 | 1.0484 | 8 | 9 |
| Histamine H2 receptor | Cavia porcellus (domestic guinea pig) | Ki | 0.1559 | 1 | 2 |
| Histamine H2 receptor | Homo sapiens (human) | Ki | 0.9161 | 5 | 7 |
| Histamine H4 receptor | Homo sapiens (human) | Ki | 10.0000 | 1 | 4 |
| Multidrug and toxin extrusion protein 1 | Homo sapiens (human) | IC50 | 2.4650 | 3 | 4 |
| Multidrug and toxin extrusion protein 2 | Homo sapiens (human) | IC50 | 37.6000 | 2 | 2 |
| Multidrug resistance-associated protein 4 | Homo sapiens (human) | IC50 | 133.0000 | 1 | 2 |
| Potassium-transporting ATPase alpha chain 1 | Homo sapiens (human) | IC50 | 50.4100 | 2 | 2 |
| Potassium-transporting ATPase subunit beta | Homo sapiens (human) | IC50 | 50.4100 | 2 | 2 |
| Solute carrier family 22 member 1 | Mus musculus (house mouse) | IC50 | 0.5900 | 1 | 1 |
| Solute carrier family 22 member 1 | Rattus norvegicus (Norway rat) | IC50 | 329.0000 | 1 | 1 |
| Solute carrier family 22 member 1 | Rattus norvegicus (Norway rat) | Ki | 5.7000 | 1 | 1 |
| Solute carrier family 22 member 1 | Homo sapiens (human) | IC50 | 183.0000 | 3 | 3 |
| Solute carrier family 22 member 1 | Homo sapiens (human) | Ki | 166.0000 | 1 | 1 |
| Solute carrier family 22 member 11 | Homo sapiens (human) | IC50 | 2,000.0000 | 1 | 1 |
| Solute carrier family 22 member 2 | Homo sapiens (human) | IC50 | 29.5500 | 2 | 2 |
| Solute carrier family 22 member 2 | Mus musculus (house mouse) | IC50 | 8.0000 | 1 | 1 |
| Solute carrier family 22 member 2 | Rattus norvegicus (Norway rat) | IC50 | 373.0000 | 1 | 1 |
| Solute carrier family 22 member 2 | Homo sapiens (human) | Ki | 928.5000 | 1 | 2 |
| Solute carrier family 22 member 2 | Rattus norvegicus (Norway rat) | Ki | 103.7000 | 2 | 2 |
| Solute carrier family 22 member 3 | Homo sapiens (human) | IC50 | 10.7000 | 1 | 1 |
| Solute carrier family 22 member 4 | Rattus norvegicus (Norway rat) | IC50 | 1,500.0000 | 1 | 1 |
| Solute carrier family 22 member 6 | Homo sapiens (human) | IC50 | 492.0000 | 1 | 1 |
| Solute carrier family 22 member 6 | Rattus norvegicus (Norway rat) | IC50 | 2,000.0000 | 1 | 1 |
| Solute carrier family 22 member 6 | Rattus norvegicus (Norway rat) | Ki | 1,000.0000 | 1 | 1 |
| Solute carrier family 22 member 8 | Homo sapiens (human) | IC50 | 92.4000 | 1 | 1 |
| Solute carrier family 22 member 8 | Rattus norvegicus (Norway rat) | IC50 | 166.0000 | 1 | 1 |
| Solute carrier family 22 member 8 | Homo sapiens (human) | Ki | 176.5000 | 1 | 2 |
| Solute carrier family 22 member 8 | Rattus norvegicus (Norway rat) | Ki | 46.8000 | 1 | 1 |
Activation Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Histamine H1 receptor | Cavia porcellus (domestic guinea pig) | Kd | 0.9550 | 1 | 1 |
| Histamine H2 receptor | Cavia porcellus (domestic guinea pig) | Kd | 0.3126 | 4 | 9 |
Other Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| POU domain, class 2, transcription factor 1 | Homo sapiens (human) | Km | 35.7000 | 1 | 1 |
| Solute carrier family 22 member 2 | Homo sapiens (human) | Km | 60.0000 | 1 | 1 |
| Solute carrier family 22 member 8 | Homo sapiens (human) | Km | 110.1333 | 2 | 3 |