Page last updated: 2024-08-05 15:23:33

histamine agonist

A drug that binds to and activates histamine receptors. Although they have been suggested for a variety of clinical applications, histamine agonists have so far been more widely used in research than therapeutically.

ChEBI ID: 35678

Members (6)

MemberDefinitionClass
2-(2-aminoethyl)pyridineAn aminoalkylpyridine that is pyridine substituted by a ethanamino group at position 2.2-pyridylethylamine
2-methylhistamineAn aralkylamino compound that is histamine bearing a methyl substituent at the 2 position on the ring.2-methylhistamine
4-methylhistamineAn aralkylamino compound that is histamine bearing a methyl substituent at the 5 position on the ring.4-methylhistamine
betazolePyrazole in which a hydrogen adjacent to one of the nitrogen atoms is substituted by a 2-aminoethyl group. It is a histamine H2-receptor agonist used clinically to test gastric secretory function.betazole
histamine phosphateA phosphate salt that is the diphosphate salt of histamine.histamine phosphate
mianserinA dibenzoazepine (specifically 1,2,3,4,10,14b-hexahydrodibenzo[c,f]pyrazino[1,2-a]azepine) methyl-substituted on N-2. Closely related to (and now mostly superseded by) the tetracyclic antidepressant mirtazapinean, it is an atypical antidepressant used in the treatment of depression throughout Europe and elsewhere.mianserin

Research

Studies (2,883)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-1990951 (32.99)18.7374
1990's573 (19.88)18.2507
2000's737 (25.56)29.6817
2010's579 (20.08)24.3611
2020's43 (1.49)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials561 (17.76%)5.53%
Reviews226 (7.15%)6.00%
Case Studies464 (14.69%)4.05%
Observational5 (0.16%)0.25%
Other1,903 (60.24%)84.16%

Protein Targets (147)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
acetylcholinesteraseHomo sapiens (human)Potency41.275222
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency37.650511
AR proteinHomo sapiens (human)Potency28.135977
arylsulfatase AHomo sapiens (human)Potency6.012011
ATAD5 protein, partialHomo sapiens (human)Potency29.081011
Ataxin-2Homo sapiens (human)Potency17.782811
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency23.934111
Cellular tumor antigen p53Homo sapiens (human)Potency33.491511
chromobox protein homolog 1Homo sapiens (human)Potency39.810711
cytochrome P450 2D6Homo sapiens (human)Potency2.754011
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency30.900811
D(1A) dopamine receptorHomo sapiens (human)Potency1.869222
Disintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)Potency5.011911
estrogen nuclear receptor alphaHomo sapiens (human)Potency27.975366
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency29.849311
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency31.670422
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency34.534422
EWS/FLI fusion proteinHomo sapiens (human)Potency20.493344
Fumarate hydrataseHomo sapiens (human)Potency37.221211
gemininHomo sapiens (human)Potency14.581011
GLI family zinc finger 3Homo sapiens (human)Potency27.311622
GLS proteinHomo sapiens (human)Potency11.220211
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency26.832533
heat shock 70kDa protein 5 (glucose-regulated protein, 78kDa)Homo sapiens (human)Potency35.481311
huntingtin isoform 2Homo sapiens (human)Potency35.481311
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency1.995311
lamin isoform A-delta10Homo sapiens (human)Potency0.640312
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency26.603211
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency0.077511
phosphopantetheinyl transferaseBacillus subtilisPotency70.524633
polyproteinZika virusPotency37.221211
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency14.125411
pregnane X nuclear receptorHomo sapiens (human)Potency33.491511
progesterone receptorHomo sapiens (human)Potency10.590911
ras-related protein Rab-9AHomo sapiens (human)Potency58.047911
regulator of G-protein signaling 4Homo sapiens (human)Potency8.436811
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency33.491511
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency39.810711
TDP1 proteinHomo sapiens (human)Potency19.952611
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency24.173922
ubiquitin carboxyl-terminal hydrolase 2 isoform aHomo sapiens (human)Potency5.011911
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency14.015422
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency39.810711

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
5-hydroxytryptamine receptor 1AHomo sapiens (human)IC500.398122
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)IC502.936022
5-hydroxytryptamine receptor 1AHomo sapiens (human)Ki0.500011
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Ki0.726033
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)IC502.936022
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)Ki1.719544
5-hydroxytryptamine receptor 1DHomo sapiens (human)IC500.380222
5-hydroxytryptamine receptor 1DRattus norvegicus (Norway rat)IC505.000011
5-hydroxytryptamine receptor 1DRattus norvegicus (Norway rat)Ki0.840022
5-hydroxytryptamine receptor 1FRattus norvegicus (Norway rat)IC505.000011
5-hydroxytryptamine receptor 1FRattus norvegicus (Norway rat)Ki0.840022
5-hydroxytryptamine receptor 2AHomo sapiens (human)IC500.011033
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)IC505.000011
5-hydroxytryptamine receptor 2AHomo sapiens (human)Ki0.00701113
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)Ki0.006555
5-hydroxytryptamine receptor 2BHomo sapiens (human)IC500.007311
5-hydroxytryptamine receptor 2BRattus norvegicus (Norway rat)IC505.000011
5-hydroxytryptamine receptor 2BHomo sapiens (human)Ki0.004611
5-hydroxytryptamine receptor 2BRattus norvegicus (Norway rat)Ki0.004233
5-hydroxytryptamine receptor 2CHomo sapiens (human)IC500.004322
5-hydroxytryptamine receptor 2CRattus norvegicus (Norway rat)IC505.000011
5-hydroxytryptamine receptor 2CHomo sapiens (human)Ki0.004868
5-hydroxytryptamine receptor 2CRattus norvegicus (Norway rat)Ki0.003544
5-hydroxytryptamine receptor 3AHomo sapiens (human)IC501.412522
5-hydroxytryptamine receptor 3AMus musculus (house mouse)IC501.412511
5-hydroxytryptamine receptor 3ARattus norvegicus (Norway rat)IC505.000011
5-hydroxytryptamine receptor 3AMus musculus (house mouse)Ki0.252011
5-hydroxytryptamine receptor 3ARattus norvegicus (Norway rat)Ki0.070011
5-hydroxytryptamine receptor 3BHomo sapiens (human)IC501.412522
5-hydroxytryptamine receptor 3BMus musculus (house mouse)IC501.412511
5-hydroxytryptamine receptor 3BRattus norvegicus (Norway rat)IC505.000011
5-hydroxytryptamine receptor 3BMus musculus (house mouse)Ki0.252011
5-hydroxytryptamine receptor 3BRattus norvegicus (Norway rat)Ki0.070011
5-hydroxytryptamine receptor 3CHomo sapiens (human)IC501.412522
5-hydroxytryptamine receptor 3DHomo sapiens (human)IC501.412522
5-hydroxytryptamine receptor 3EHomo sapiens (human)IC501.412522
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)IC500.001211
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)Ki0.000611
5-hydroxytryptamine receptor 4 Rattus norvegicus (Norway rat)IC505.000011
5-hydroxytryptamine receptor 5ARattus norvegicus (Norway rat)IC505.000011
5-hydroxytryptamine receptor 5BRattus norvegicus (Norway rat)IC505.000011
5-hydroxytryptamine receptor 6Homo sapiens (human)IC500.085011
5-hydroxytryptamine receptor 6Rattus norvegicus (Norway rat)IC505.000011
5-hydroxytryptamine receptor 6Homo sapiens (human)Ki0.047522
5-hydroxytryptamine receptor 7Homo sapiens (human)IC500.114811
5-hydroxytryptamine receptor 7Homo sapiens (human)Ki2.709733
5-hydroxytryptamine receptor 7 Rattus norvegicus (Norway rat)IC505.000011
5-hydroxytryptamine receptor 7 Rattus norvegicus (Norway rat)Ki0.081622
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)IC500.163011
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)Ki0.161011
Alpha-1A adrenergic receptorHomo sapiens (human)IC500.407422
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)IC500.190022
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)Ki0.075034
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)IC500.380011
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)Ki0.075034
Alpha-1D adrenergic receptorHomo sapiens (human)IC500.083011
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)IC500.380011
Alpha-1D adrenergic receptorHomo sapiens (human)Ki0.041011
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)Ki0.075034
Alpha-2A adrenergic receptorHomo sapiens (human)IC500.021333
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)IC500.210011
Alpha-2A adrenergic receptorHomo sapiens (human)Ki0.010422
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)Ki0.062011
Alpha-2B adrenergic receptorHomo sapiens (human)IC500.026022
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)IC500.210011
Alpha-2B adrenergic receptorHomo sapiens (human)Ki0.024011
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)Ki0.062011
Alpha-2C adrenergic receptorHomo sapiens (human)IC500.066144
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)IC500.210011
Alpha-2C adrenergic receptorHomo sapiens (human)Ki0.014922
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)Ki0.062011
Angiotensin-converting enzymeRattus norvegicus (Norway rat)Ki0.500013
Bile salt export pumpHomo sapiens (human)IC5046.820011
DRattus norvegicus (Norway rat)Ki1.420011
D(1A) dopamine receptorHomo sapiens (human)IC500.543011
D(1A) dopamine receptorHomo sapiens (human)Ki0.271011
D(2) dopamine receptorHomo sapiens (human)IC507.079522
D(2) dopamine receptorRattus norvegicus (Norway rat)IC503.548122
D(2) dopamine receptorHomo sapiens (human)Ki2.197011
D(2) dopamine receptorRattus norvegicus (Norway rat)Ki0.942723
D(3) dopamine receptorHomo sapiens (human)IC503.890422
D(3) dopamine receptorHomo sapiens (human)Ki2.841011
D(3) dopamine receptorRattus norvegicus (Norway rat)Ki1.524011
D(4) dopamine receptorHomo sapiens (human)IC503.311322
Endothelin receptor type BHomo sapiens (human)Ki0.063122
Endothelin receptor type BRattus norvegicus (Norway rat)Ki0.063111
Endothelin-1 receptorHomo sapiens (human)IC500.114811
G-protein coupled receptor Apis mellifera (honey bee)IC5073.000011
Histamine H1 receptorHomo sapiens (human)IC500.630734
Histamine H1 receptorRattus norvegicus (Norway rat)IC500.755425
Histamine H1 receptorHomo sapiens (human)Ki2,103,190,000.000633
Histamine H1 receptorRattus norvegicus (Norway rat)Ki6,309,570,000.000011
Histamine H2 receptorCavia porcellus (domestic guinea pig)IC500.880011
Histamine H2 receptorHomo sapiens (human)IC501.008011
Histamine H2 receptorHomo sapiens (human)Ki4.467622
Histamine H3 receptorHomo sapiens (human)Ki6.309611
Histamine H4 receptorHomo sapiens (human)Ki2.337725
Muscarinic acetylcholine receptor M1Homo sapiens (human)IC501.423011
Muscarinic acetylcholine receptor M1Homo sapiens (human)Ki0.343011
Muscarinic acetylcholine receptor M2Homo sapiens (human)IC501.078011
Muscarinic acetylcholine receptor M2Homo sapiens (human)Ki0.383011
Muscarinic acetylcholine receptor M3Homo sapiens (human)IC501.405011
Muscarinic acetylcholine receptor M3Homo sapiens (human)Ki0.298011
Muscarinic acetylcholine receptor M4Homo sapiens (human)IC502.066011
Muscarinic acetylcholine receptor M4Homo sapiens (human)Ki0.288011
Muscarinic acetylcholine receptor M5Homo sapiens (human)IC500.320011
Muscarinic acetylcholine receptor M5Rattus norvegicus (Norway rat)IC501.900011
Muscarinic acetylcholine receptor M5Homo sapiens (human)Ki0.230011
Sodium-dependent noradrenaline transporter Homo sapiens (human)IC500.163011
Sodium-dependent noradrenaline transporter Homo sapiens (human)Ki0.161011
Sodium-dependent serotonin transporterHomo sapiens (human)IC502.068011
Sodium-dependent serotonin transporterRattus norvegicus (Norway rat)IC502.900011
Sodium-dependent serotonin transporterHomo sapiens (human)Ki1.098011
TransporterRattus norvegicus (Norway rat)IC500.022012
TransporterRattus norvegicus (Norway rat)Ki0.101011
Type-2 angiotensin II receptorRattus norvegicus (Norway rat)IC500.210011
Type-2 angiotensin II receptorRattus norvegicus (Norway rat)Ki0.500011

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
5-hydroxytryptamine receptor 1AHomo sapiens (human)Kd0.398111
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)Kd1.974022
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)Kd1.974022
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)Kd1.974022
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)Kd1.095822
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)Kd1.095822
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)Kd1.095822
Histamine H1 receptorHomo sapiens (human)EC508.321622
Histamine H2 receptorHomo sapiens (human)EC503.023222
Histamine H3 receptorCavia porcellus (domestic guinea pig)EC501.584911
Histamine H3 receptorHomo sapiens (human)EC5012.400011
Histamine H4 receptorHomo sapiens (human)EC501.030834
Histamine H4 receptorMus musculus (house mouse)EC501.584911
Histamine H4 receptorRattus norvegicus (Norway rat)EC502.511911

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
5-hydroxytryptamine receptor 6Homo sapiens (human)Kb0.030011
Adenosine receptor A1Rattus norvegicus (Norway rat)KA15.000011
Adenosine receptor A2aRattus norvegicus (Norway rat)KA15.000012
Carbonic anhydraseCandida albicans SC5314KA30.200011
Carbonic anhydraseMethanosarcina thermophilaKA24.000011
Carbonic anhydraseMethanothermobacter thermautotrophicus str. Delta HKa40.000011
Carbonic anhydraseSaccharomyces cerevisiae S288CKa11.200022
Carbonic anhydrase Cryptococcus neoformans var. grubiiKA46.300011
Carbonic anhydrase Nakaseomyces glabratus CBS 138Ka16.300011
Carbonic anhydrase 1Homo sapiens (human)KA13.00001111
Carbonic anhydrase 12Homo sapiens (human)KA0.690011
Carbonic anhydrase 13Mus musculus (house mouse)KA46.000011
Carbonic anhydrase 14Homo sapiens (human)KA6.900011
Carbonic anhydrase 15Mus musculus (house mouse)KA11.900011
Carbonic anhydrase 2Homo sapiens (human)KA15.00001313
Carbonic anhydrase 3Homo sapiens (human)Ka1.100022
Carbonic anhydrase 4Homo sapiens (human)KA7.130022
Carbonic anhydrase 5A, mitochondrialHomo sapiens (human)KA7.620011
Carbonic anhydrase 5B, mitochondrialHomo sapiens (human)KA0.094011
Carbonic anhydrase 6Homo sapiens (human)Ka18.000022
Carbonic anhydrase 7Homo sapiens (human)KA27.800011
Carbonic anhydrase 9Homo sapiens (human)KA0.013011
Carbonic anhydrase-like protein, putativeTrypanosoma cruzi strain CL BrenerKA100.000011
Glutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)KA27.800011
Glutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)KA27.800011
Glutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)KA27.800011
Glutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)KA27.800011
Glutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)KA27.800011
Glutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)KA27.800011
Glutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)KA27.800011
Histamine H2 receptorCavia porcellus (domestic guinea pig)K0.50.000312
Plasma kallikreinHomo sapiens (human)KA0.094011