A histamine agonist that binds to and activates histamine H3-receptors.
ChEBI ID: 64154
| Member | Definition | Class |
|---|---|---|
| alpha-methylhistamine | An aralkylamino compound that is histamine bearing a methyl substituent at the alpha-position. | alpha-methylhistamine |
| alpha-methylhistamine | An aralkylamino compound that is histamine bearing a methyl substituent at the alpha-position (the R-enantiomer). | (R)-alpha-methylhistamine |
| imetit | An imidothiocarbamic ester that consists of isothiourea in which the thiol hydrogen is substituted by a 2-(imidazol-4-yl)ethyl group. An extremely potent, high affinity agonist at H3 and H4 receptors (Ki values are 0.3 and 2.7 nM respectively). Induces shape change in eosinophils with an EC50 of 25 nM. Centrally active following systemic administration. | imetit |
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 1 (0.31) | 18.7374 |
| 1990's | 164 (50.46) | 18.2507 |
| 2000's | 114 (35.08) | 29.6817 |
| 2010's | 38 (11.69) | 24.3611 |
| 2020's | 8 (2.46) | 2.80 |
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 3 (0.80%) | 5.53% |
| Reviews | 3 (0.80%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 367 (98.39%) | 84.16% |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| aldehyde dehydrogenase 1 family, member A1 | Homo sapiens (human) | Potency | 39.8107 | 1 | 2 |
| alpha-galactosidase | Homo sapiens (human) | Potency | 63.0957 | 1 | 1 |
| arylsulfatase A | Homo sapiens (human) | Potency | 33.8078 | 1 | 1 |
| ATAD5 protein, partial | Homo sapiens (human) | Potency | 2.9081 | 1 | 1 |
| Chain A, TYROSYL-DNA PHOSPHODIESTERASE | Homo sapiens (human) | Potency | 1.4125 | 1 | 1 |
| chromobox protein homolog 1 | Homo sapiens (human) | Potency | 28.5991 | 1 | 2 |
| cytochrome P450 2D6 isoform 1 | Homo sapiens (human) | Potency | 15.7142 | 1 | 2 |
| cytochrome P450 3A4 isoform 1 | Homo sapiens (human) | Potency | 27.8298 | 2 | 4 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 16.3191 | 1 | 2 |
| GABA theta subunit | Rattus norvegicus (Norway rat) | Potency | 27.8298 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit alpha-1 | Rattus norvegicus (Norway rat) | Potency | 27.8298 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | Potency | 27.8298 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | Potency | 27.8298 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | Potency | 27.8298 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit alpha-5 | Rattus norvegicus (Norway rat) | Potency | 27.8298 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | Potency | 27.8298 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit beta-1 | Rattus norvegicus (Norway rat) | Potency | 27.8298 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit beta-2 | Rattus norvegicus (Norway rat) | Potency | 27.8298 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit beta-3 | Rattus norvegicus (Norway rat) | Potency | 27.8298 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit delta | Rattus norvegicus (Norway rat) | Potency | 27.8298 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit epsilon | Rattus norvegicus (Norway rat) | Potency | 27.8298 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit gamma-1 | Rattus norvegicus (Norway rat) | Potency | 27.8298 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit gamma-2 | Rattus norvegicus (Norway rat) | Potency | 27.8298 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit gamma-3 | Rattus norvegicus (Norway rat) | Potency | 27.8298 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit pi | Rattus norvegicus (Norway rat) | Potency | 27.8298 | 1 | 2 |
| Histamine H2 receptor | Cavia porcellus (domestic guinea pig) | Potency | 15.8489 | 1 | 2 |
| histone acetyltransferase KAT2A isoform 1 | Homo sapiens (human) | Potency | 39.8107 | 1 | 1 |
| lethal factor (plasmid) | Bacillus anthracis str. A2012 | Potency | 12.5893 | 1 | 1 |
| Microtubule-associated protein tau | Homo sapiens (human) | Potency | 15.8489 | 1 | 1 |
| Polyunsaturated fatty acid lipoxygenase ALOX15B | Homo sapiens (human) | Potency | 15.8489 | 1 | 1 |
| TDP1 protein | Homo sapiens (human) | Potency | 26.1011 | 2 | 2 |
| thioredoxin reductase | Rattus norvegicus (Norway rat) | Potency | 6.6326 | 2 | 3 |
| Thrombopoietin | Homo sapiens (human) | Potency | 0.7943 | 2 | 2 |
| vitamin D3 receptor isoform VDRA | Homo sapiens (human) | Potency | 79.4328 | 1 | 1 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Histamine H1 receptor | Cavia porcellus (domestic guinea pig) | Ki | 10.0000 | 1 | 4 |
| Histamine H3 receptor | Homo sapiens (human) | IC50 | 0.0023 | 1 | 1 |
| Histamine H3 receptor | Rattus norvegicus (Norway rat) | IC50 | 0.0015 | 1 | 1 |
| Histamine H3 receptor | Cavia porcellus (domestic guinea pig) | Ki | 0.0008 | 2 | 2 |
| Histamine H3 receptor | Homo sapiens (human) | Ki | 0.0057 | 16 | 21 |
| Histamine H3 receptor | Mus musculus (house mouse) | Ki | 0.0020 | 1 | 1 |
| Histamine H4 receptor | Homo sapiens (human) | Ki | 378,971,818,181.8966 | 8 | 11 |
| Metabotropic glutamate receptor 5 | Rattus norvegicus (Norway rat) | Ki | 0.0006 | 1 | 2 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Histamine H3 receptor | Homo sapiens (human) | EC50 | 0.0064 | 6 | 8 |
| Histamine H4 receptor | Homo sapiens (human) | EC50 | 0.3658 | 4 | 5 |
| Metabotropic glutamate receptor 5 | Rattus norvegicus (Norway rat) | EC50 | 0.0026 | 1 | 4 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Histamine H3 receptor | Cavia porcellus (domestic guinea pig) | KH | 0.0043 | 1 | 1 |
| Histamine H3 receptor | Cavia porcellus (domestic guinea pig) | KL | 0.2200 | 1 | 1 |