Histamine

Identification

Summary

Histamine is an ingredient of topical drugs for the relief of joint pain or muscle aches and pains.

Brand Names
Activon Arthritis, Ceplene, Rematex
Generic Name
Histamine
DrugBank Accession Number
DB05381
Background

A depressor amine derived by enzymatic decarboxylation of histidine. It is a powerful stimulant of gastric secretion, a constrictor of bronchial smooth muscle, a vasodilator, and also a centrally acting neurotransmitter.

Type
Small Molecule
Groups
Approved, Investigational
Structure
Weight
Average: 111.1451
Monoisotopic: 111.079647303
Chemical Formula
C5H9N3
Synonyms
  • 1H-Imidazole-4-ethanamine
  • 2-(4-imidazolyl)ethylamine
  • 4-imidazoleethylamine
  • 5-imidazoleethylamine
  • beta-aminoethylglyoxaline
  • beta-aminoethylimidazole
External IDs
  • NSC-33792

Pharmacology

Indication

Histamine phosphate is indicated as a diagnostic aid for the evaluation of gastric acid secretory function.

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Prophylaxis ofMigraine••• ••••••••••••••
Contraindications & Blackbox Warnings
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Pharmacodynamics

Histamine stimulates gastric gland secretion, causing an increased secretion of gastric juice of high acidity. This action is probably due mainly to a direct action on parietal and chief gland cells.

Mechanism of action

Histamine acts directly on the blood vessels to dilate arteries and capillaries; this action is mediated by both H 1- and H 2-receptors. Capillary dilatation may produce flushing of the face, a decrease in systemic blood pressure, and gastric gland secretion, causing an increased secretion of gastric juice of high acidity. Increased capillary permeability accompanies capillary dilatation, producing an outward passage of plasma protein and fluid into the extracellular spaces, an increase in lymph flow and protein content, and the formation of edema. In addition, histamine has a direct stimulant action on smooth muscle, producing contraction if H 1-receptors are activated, or mostly relaxation if H 2-receptors are activated. Also in humans, the stimulant effect of histamine may cause contraction of the intestinal muscle. However, little effect is noticed on the uterus, bladder, or gallbladder. Histamine has some stimulant effect on duodenal, salivary, pancreatic, bronchial, and lacrimal glands. Histamine also can bind to H3 and H4 receptors which are involved in the CNS/PNS neurotransmitter release and immune system chemotaxis, respectively.

TargetActionsOrganism
AHistamine H1 receptor
agonist
Humans
AHistamine H2 receptor
agonist
Humans
AHistamine H3 receptor
agonist
Humans
UHistamine H4 receptor
agonist
Humans
USynaptic vesicular amine transporterNot AvailableHumans
Absorption

Readily absorbed after parenteral administration.

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism

Primarily hepatic. Histamine is rapidly metabolized by methylation and oxidation. Methylation involves ring methylation and catalyzation by the enzyme histamine-N-methyltransferase, producing N-methylhistamine, which is mostly converted to N-methyl imidazole acetic acid. 2 to 3% excreted as free histamine, 4 to 8% as N-methylhistamine, 42 to 47% as N-methyl imidazole acetic acid, 9 to 11% as imidazole acetic acid, and 16 to 23% as imidazole acetic acid riboside.

Route of elimination

Not Available

Half-life

Not Available

Clearance

Not Available

Adverse Effects
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Toxicity

LD50=807 mg/kg (mouse, oral). Side effects can lead to hypertension, hypotension, headache, dizziness, nervousness and tachycardia. Large overdoses can lead to seizures.

Pathways
Not Available
Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
Not Available

Interactions

Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AcyclovirThe risk or severity of adverse effects can be increased when Acyclovir is combined with Histamine.
AmantadineThe serum concentration of Histamine can be increased when it is combined with Amantadine.
AmilorideThe serum concentration of Histamine can be increased when it is combined with Amiloride.
Aminohippuric acidThe serum concentration of Histamine can be increased when it is combined with Aminohippuric acid.
AmiodaroneThe serum concentration of Histamine can be increased when it is combined with Amiodarone.
Food Interactions
No interactions found.

Products

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Product Ingredients
IngredientUNIICASInChI Key
Histamine dihydrochloride3POA0Q644U56-92-8PPZMYIBUHIPZOS-UHFFFAOYSA-N
Histamine phosphateQWB37T4WZZ51-74-1ZHIBQGJKHVBLJJ-UHFFFAOYSA-N
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
CepleneInjection, solution0.5 mg/0.5mlSubcutaneousLaboratoires Delbert2016-09-20Not applicableEU flag
Histamine Phosphate Injection USP Liq ScLiquid1 mg / mLSubcutaneousBioniche Pharma (Canada) Ltd1994-12-312014-11-24Canada flag
Histamine Phosphate Injection USP, 1mg/mlLiquid1 mg / mLSubcutaneousAlveda Pharmaceuticals IncNot applicableNot applicableCanada flag
Histamine Positive Skin Test ControlSolution2.75 mg/1mLPercutaneousALK-Abello, Inc.1989-10-23Not applicableUS flag
Histamine Positive Skin Test ControlInjection, solution0.275 mg/1mLIntradermalALK-Abello, Inc.1989-10-23Not applicableUS flag
Over the Counter Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
AMINO ACTIVE Topical Analgesic CreamCream0.25 mg/1mLTopicalVIREO SYSTEMS, INC.2022-08-08Not applicableUS flag
Arthritis Pain ReliefCream0.025 g/100gTopicalWalgreens2022-11-01Not applicableUS flag
Arthritis Pain ReliefCream0.03 g/100gTopicalPainX LLC2022-11-07Not applicableUS flag
Arthritis Pain Relief CreamCream.00025 g/1gTopicalSombra Cosmetics, Inc.2019-12-09Not applicableUS flag
Australian Dream Back PainCream0.05 g/100gTopicalNature's Health Connection2014-07-102019-12-03US flag
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
Abee MedHistamine dihydrochloride (0.5 mg/1g) + Menthol (15 mg/1g)CreamTopicalCrossover Telecom Llc2016-05-25Not applicableUS flag
ActivOn Ultra Strength ArthritisHistamine dihydrochloride (0.00028 g/1g) + Menthol (0.04574 g/1g)StickTopicalFamily First Pharmaceuticals, Inc.2011-09-01Not applicableUS flag
Alo Therapeutic MassageHistamine dihydrochloride (1 mg/1mL) + Menthol (30 mg/1mL)CreamTopicalCmi Therapy Solutions2016-11-10Not applicableUS flag
Alo Therapeutic MassageHistamine dihydrochloride (0.1 g/100g) + Menthol (3 g/100g)CreamTopicalTheraplex Solutions2012-06-07Not applicableUS flag
Alo Therapeutic MassageHistamine dihydrochloride (1 mg/1mL) + Menthol (30 mg/1mL)CreamTopicalCmi Therapy Solutions2016-11-10Not applicableUS flag
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
CamphomexHistamine (0.03 mg/1mL) + Camphor (3.6 mg/1mL) + Menthol (12 mg/1mL)SprayTopical1st Class Pharmaceuticals2014-03-242016-01-15US flag
SimanixHistamine dihydrochloride (0.035 g/100g) + Capsaicin (0.0375 g/100g) + Menthol (3 g/100g)CreamTopicalHome Aide Diagnostics, Inc.2015-07-08Not applicableUS flag
SimanixHistamine dihydrochloride (0.035 g/100g) + Capsaicin (0.0357 g/100g) + Menthol (3 g/100g)CreamTopicalHome Aide Diagnostics, Inc.2015-07-08Not applicableUS flag

Categories

ATC Codes
L03AX14 — Histamine dihydrochlorideV04CG03 — Histamine phosphate
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as 2-arylethylamines. These are primary amines that have the general formula RCCNH2, where R is an organic group.
Kingdom
Organic compounds
Super Class
Organic nitrogen compounds
Class
Organonitrogen compounds
Sub Class
Amines
Direct Parent
2-arylethylamines
Alternative Parents
Aralkylamines / Imidazoles / Heteroaromatic compounds / Azacyclic compounds / Organopnictogen compounds / Monoalkylamines / Hydrocarbon derivatives
Substituents
2-arylethylamine / Aralkylamine / Aromatic heteromonocyclic compound / Azacycle / Azole / Heteroaromatic compound / Hydrocarbon derivative / Imidazole / Organoheterocyclic compound / Organopnictogen compound
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
imidazoles, aralkylamino compound (CHEBI:18295) / Biogenic amines, Histamine (C00388)
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
820484N8I3
CAS number
51-45-6
InChI Key
NTYJJOPFIAHURM-UHFFFAOYSA-N
InChI
InChI=1S/C5H9N3/c6-2-1-5-3-7-4-8-5/h3-4H,1-2,6H2,(H,7,8)
IUPAC Name
2-(1H-imidazol-4-yl)ethan-1-amine
SMILES
NCCC1=CNC=N1

References

General References
  1. Middleton M, Sarno M, Agarwala SS, Glaspy J, Laurent A, McMasters K, Naredi P, O'Day S, Whitman E, Danson S, Cosford R, Gehlsen K: Pharmacokinetics of histamine dihydrochloride in healthy volunteers and cancer patients: implications for combined immunotherapy with interleukin-2. J Clin Pharmacol. 2002 Jul;42(7):774-81. [Article]
  2. Silberstein SD: Preventive Migraine Treatment. Continuum (Minneap Minn). 2015 Aug;21(4 Headache):973-89. doi: 10.1212/CON.0000000000000199. [Article]
  3. DailyMed: Histamine positive test control injection [Link]
  4. BASG: ALK Prick Positiv Kontrolle (Histamine) Intradermal Solution [Link]
Human Metabolome Database
HMDB0060263
KEGG Drug
D08040
KEGG Compound
C00388
PubChem Compound
774
PubChem Substance
175426988
ChemSpider
753
BindingDB
7966
RxNav
5333
ChEBI
18295
ChEMBL
CHEMBL90
ZINC
ZINC000000388081
PharmGKB
PA449880
PDBe Ligand
HSM
Drugs.com
Drugs.com Drug Page
Wikipedia
Histamine
PDB Entries
1avn / 1ike / 1jqd / 1kar / 1np1 / 1qft / 1qfv / 1u18 / 2qeb / 2x45
show 21 more
MSDS
Download (49.5 KB)

Clinical Trials

Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
PhaseStatusPurposeConditionsCount
4CompletedTreatmentAcute Myeloid Leukemia1
4RecruitingBasic ScienceNormal Skin / Skin Photoaging1
3CompletedTreatmentLeukemias1
3CompletedTreatmentOsteoarthritis of the Knee1
3Unknown StatusTreatmentMelanoma / Metastatic Cancer1

Pharmacoeconomics

Manufacturers
  • Eli lilly and co
Packagers
  • ALK-Abello Inc.
  • Hollister-Stier Laboratories LLC
  • Medisca Inc.
  • Professional Co.
Dosage Forms
FormRouteStrength
StickTopical
SolutionIntradermal
SolutionIntradermal10 mg/ml
SolutionTopical1.7 mg/ml
CreamTopical0.03 g/100g
LiquidTopical
CreamTopical.0005 g/1g
CreamTopical0.25 mg/1g
CreamTopical0.3 mg/1g
SprayTopical
Injection, solutionSubcutaneous0.5 MG/0.5ML
CreamTopical.025 g/100g
CreamTopical0.25 mg/1mL
CreamTopical0.05 g/100g
CreamTopical.00025 g/1g
SprayTopical0.1 g/100mL
LiquidSubcutaneous1 mg / mL
Injection, solutionIntradermal0.275 mg/1mL
SolutionPercutaneous2.75 mg/1mL
SolutionIntradermal0.275 mg / mL
SolutionPercutaneous2.75 mg / mL
Solution
LotionTopical0.6 mg/1mL
OintmentTopical
CreamTopical0.3 mg/1mL
GelTopical0.5 mg/1mL
GelTopical0.25 mg/1mL
CreamTopical0.025 g/100g
CreamTopical
InjectionPercutaneous6 mg/1mL
SolutionPercutaneous6 mg / mL
CreamTopical0.4 mg/1mL
CreamTopical0.05 mg/100mg
CreamTopical0.00025 g/1g
Solution10 mg/1ml
Prices
Unit descriptionCostUnit
Histamine phosphate 100% cryst14.38USD g
Histatrol 1:10000 vial13.18USD ml
Histamine di-hcl powder12.6USD g
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)139 °C (phosphate salt)Not Available
Predicted Properties
PropertyValueSource
Water Solubility169.0 mg/mLALOGPS
logP-0.69ALOGPS
logP-0.7Chemaxon
logS0.18ALOGPS
pKa (Strongest Acidic)14.46Chemaxon
pKa (Strongest Basic)9.58Chemaxon
Physiological Charge1Chemaxon
Hydrogen Acceptor Count2Chemaxon
Hydrogen Donor Count2Chemaxon
Polar Surface Area54.7 Å2Chemaxon
Rotatable Bond Count2Chemaxon
Refractivity31.66 m3·mol-1Chemaxon
Polarizability12.08 Å3Chemaxon
Number of Rings1Chemaxon
Bioavailability1Chemaxon
Rule of FiveYesChemaxon
Ghose FilterNoChemaxon
Veber's RuleNoChemaxon
MDDR-like RuleNoChemaxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption+0.9931
Blood Brain Barrier+0.8784
Caco-2 permeable-0.5409
P-glycoprotein substrateNon-substrate0.6136
P-glycoprotein inhibitor INon-inhibitor0.9639
P-glycoprotein inhibitor IINon-inhibitor0.9013
Renal organic cation transporterNon-inhibitor0.529
CYP450 2C9 substrateNon-substrate0.8735
CYP450 2D6 substrateNon-substrate0.7217
CYP450 3A4 substrateNon-substrate0.7528
CYP450 1A2 substrateNon-inhibitor0.8045
CYP450 2C9 inhibitorNon-inhibitor0.8396
CYP450 2D6 inhibitorNon-inhibitor0.8574
CYP450 2C19 inhibitorNon-inhibitor0.9187
CYP450 3A4 inhibitorNon-inhibitor0.7351
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8404
Ames testNon AMES toxic0.7103
CarcinogenicityNon-carcinogens0.8747
BiodegradationNot ready biodegradable0.9377
Rat acute toxicity2.4808 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9413
hERG inhibition (predictor II)Non-inhibitor0.8061
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
GC-MS Spectrum - GC-EI-TOF (Pegasus III TOF-MS system, Leco; GC 6890, Agilent Technologies) (3 TMS)GC-MSsplash10-0f79-5910000000-9946e1707fcaf5562f88
GC-MS Spectrum - GC-EI-TOF (Pegasus III TOF-MS system, Leco; GC 6890, Agilent Technologies)GC-MSsplash10-00di-2910000000-8c243055df15d6ce8116
GC-MS Spectrum - GC-EI-TOF (Pegasus III TOF-MS system, Leco; GC 6890, Agilent Technologies) (3 TMS)GC-MSsplash10-00di-9710000000-bf79b524c104e1cc94ba
GC-MS Spectrum - GC-MS (2 TMS)GC-MSsplash10-0udi-2900000000-a40a3d0aed04ccfe9365
GC-MS Spectrum - GC-MS (3 TMS)GC-MSsplash10-00dr-3910000000-44d8fb649d4e75eba66c
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSsplash10-001i-9100000000-3de6a14d8a45af6c9d66
GC-MS Spectrum - GC-EI-TOFGC-MSsplash10-0f79-5910000000-9946e1707fcaf5562f88
GC-MS Spectrum - GC-EI-TOFGC-MSsplash10-00di-2910000000-8c243055df15d6ce8116
GC-MS Spectrum - GC-EI-TOFGC-MSsplash10-00di-9710000000-bf79b524c104e1cc94ba
GC-MS Spectrum - GC-MSGC-MSsplash10-0udi-2900000000-a40a3d0aed04ccfe9365
GC-MS Spectrum - GC-MSGC-MSsplash10-00dr-3910000000-44d8fb649d4e75eba66c
GC-MS Spectrum - GC-MSGC-MSsplash10-0udi-2900000000-a40a3d0aed04ccfe9365
GC-MS Spectrum - GC-MSGC-MSsplash10-00dr-3910000000-44d8fb649d4e75eba66c
Mass Spectrum (Electron Ionization)MSsplash10-001i-9000000000-9d57c893be8c75ce8178
MS/MS Spectrum - Quattro_QQQ 10V, Positive (Annotated)LC-MS/MSsplash10-01ot-9600000000-06c58d75770dfd76aeab
MS/MS Spectrum - Quattro_QQQ 25V, Positive (Annotated)LC-MS/MSsplash10-00kf-9000000000-0135b8f0628e592abc22
MS/MS Spectrum - Quattro_QQQ 40V, Positive (Annotated)LC-MS/MSsplash10-000x-9000000000-6fccc177582b320a48ae
LC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 10V, PositiveLC-MS/MSsplash10-03di-1900000000-6cda8885da689473fb42
LC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 20V, PositiveLC-MS/MSsplash10-0002-9100000000-37450d9969c24ad44ad7
LC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 30V, PositiveLC-MS/MSsplash10-0002-9000000000-e9e368926d3146437e13
LC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 40V, PositiveLC-MS/MSsplash10-015a-9000000000-f51ad8a8259595600938
LC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 50V, PositiveLC-MS/MSsplash10-00lu-9000000000-3e02d5b58a7c9f77ec53
LC-MS/MS Spectrum - LC-ESI-QTOF (UPLC Q-Tof Premier, Waters) , PositiveLC-MS/MSsplash10-03di-0900000000-046407320168835599f0
MS/MS Spectrum - , negativeLC-MS/MSsplash10-03di-3900000000-29ccabc0b6f5396168f2
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-03di-1900000000-6cda8885da689473fb42
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-0002-9100000000-37450d9969c24ad44ad7
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-0002-9000000000-e9e368926d3146437e13
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-015a-9000000000-f51ad8a8259595600938
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-00lu-9000000000-77394d92ed9170d75b98
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-03di-0900000000-046407320168835599f0
MS/MS Spectrum - , positiveLC-MS/MSsplash10-01ot-9400000000-a19fc5e555afd53dafe7
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSsplash10-0002-9100000000-1873790d720343035c25
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSsplash10-03di-7900000000-96b9ab6a11b3319a1863
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSsplash10-0002-9000000000-7e2955a3344f73d743c3
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSsplash10-03yi-9300000000-23e8d88e453b3c010e57
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSsplash10-016u-9000000000-710090a55ca7a9dfc50a
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSsplash10-0006-9000000000-aef65835787ed382bf9f
13C NMR Spectrum1D NMRNot Applicable
1H NMR Spectrum1D NMRNot Applicable
1H NMR Spectrum1D NMRNot Applicable
13C NMR Spectrum1D NMRNot Applicable
1H NMR Spectrum1D NMRNot Applicable
13C NMR Spectrum1D NMRNot Applicable
Predicted 1H NMR Spectrum1D NMRNot Applicable
Predicted 13C NMR Spectrum1D NMRNot Applicable
[1H,13C] 2D NMR Spectrum2D NMRNot Applicable
Chromatographic Properties
Collision Cross Sections (CCS)
AdductCCS Value (Å2)Source typeSource
[M-H]-119.0188967
predicted
DarkChem Lite v0.1.0
[M-H]-118.7227967
predicted
DarkChem Lite v0.1.0
[M-H]-119.1770967
predicted
DarkChem Lite v0.1.0
[M-H]-121.41139
predicted
DeepCCS 1.0 (2019)
[M+H]+119.5835967
predicted
DarkChem Lite v0.1.0
[M+H]+119.9786967
predicted
DarkChem Lite v0.1.0
[M+H]+119.5310967
predicted
DarkChem Lite v0.1.0
[M+H]+123.68864
predicted
DeepCCS 1.0 (2019)
[M+Na]+119.2326967
predicted
DarkChem Lite v0.1.0
[M+Na]+119.2957967
predicted
DarkChem Lite v0.1.0
[M+Na]+119.2931967
predicted
DarkChem Lite v0.1.0
[M+Na]+131.81657
predicted
DeepCCS 1.0 (2019)

Targets

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Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
General Function
Histamine receptor activity
Specific Function
In peripheral tissues, the H1 subclass of histamine receptors mediates the contraction of smooth muscles, increase in capillary permeability due to contraction of terminal venules, and catecholamin...
Gene Name
HRH1
Uniprot ID
P35367
Uniprot Name
Histamine H1 receptor
Molecular Weight
55783.61 Da
References
  1. Miyoshi K, Das AK, Fujimoto K, Horio S, Fukui H: Recent advances in molecular pharmacology of the histamine systems: regulation of histamine H1 receptor signaling by changing its expression level. J Pharmacol Sci. 2006 May;101(1):3-6. Epub 2006 Apr 28. [Article]
  2. Han SK, Mancino V, Simon MI: Phospholipase Cbeta 3 mediates the scratching response activated by the histamine H1 receptor on C-fiber nociceptive neurons. Neuron. 2006 Nov 22;52(4):691-703. [Article]
  3. Spahr L, Coeytaux A, Giostra E, Hadengue A, Annoni JM: Histamine H1 blocker hydroxyzine improves sleep in patients with cirrhosis and minimal hepatic encephalopathy: a randomized controlled pilot trial. Am J Gastroenterol. 2007 Apr;102(4):744-53. Epub 2007 Jan 11. [Article]
  4. Suzuki K, Morokata T, Morihira K, Sato I, Takizawa S, Kaneko M, Takahashi K, Shimizu Y: A dual antagonist for chemokine CCR3 receptor and histamine H1 receptor. Eur J Pharmacol. 2007 Jun 1;563(1-3):224-32. Epub 2007 Feb 8. [Article]
  5. Tanimoto A, Wang KY, Murata Y, Kimura S, Nomaguchi M, Nakata S, Tsutsui M, Sasaguri Y: Histamine upregulates the expression of inducible nitric oxide synthase in human intimal smooth muscle cells via histamine H1 receptor and NF-kappaB signaling pathway. Arterioscler Thromb Vasc Biol. 2007 Jul;27(7):1556-61. Epub 2007 May 3. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
General Function
Histamine receptor activity
Specific Function
The H2 subclass of histamine receptors mediates gastric acid secretion. Also appears to regulate gastrointestinal motility and intestinal secretion. Possible role in regulating cell growth and diff...
Gene Name
HRH2
Uniprot ID
P25021
Uniprot Name
Histamine H2 receptor
Molecular Weight
40097.65 Da
References
  1. Francis H, Franchitto A, Ueno Y, Glaser S, DeMorrow S, Venter J, Gaudio E, Alvaro D, Fava G, Marzioni M, Vaculin B, Alpini G: H3 histamine receptor agonist inhibits biliary growth of BDL rats by downregulation of the cAMP-dependent PKA/ERK1/2/ELK-1 pathway. Lab Invest. 2007 May;87(5):473-87. Epub 2007 Mar 5. [Article]
  2. Soga F, Katoh N, Kishimoto S: Histamine prevents apoptosis in human monocytes. Clin Exp Allergy. 2007 Mar;37(3):323-30. [Article]
  3. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
General Function
Histamine receptor activity
Specific Function
The H3 subclass of histamine receptors could mediate the histamine signals in CNS and peripheral nervous system. Signals through the inhibition of adenylate cyclase and displays high constitutive a...
Gene Name
HRH3
Uniprot ID
Q9Y5N1
Uniprot Name
Histamine H3 receptor
Molecular Weight
48670.81 Da
References
  1. Petroianu G, Arafat K, Sasse BC, Stark H: Multiple enzyme inhibitions by histamine H3 receptor antagonists as potential procognitive agents. Pharmazie. 2006 Mar;61(3):179-82. [Article]
  2. Garduno-Torres B, Arias-Montano JA: Homologous down-regulation of histamine H3 receptors in rat striatal slices. Synapse. 2006 Aug;60(2):165-71. [Article]
  3. Minick DJ, Copley RC, Szewczyk JR, Rutkowske RD, Miller LA: An investigation of the absolute configuration of the potent histamine H3 receptor antagonist GT-2331 using vibrational circular dichroism. Chirality. 2007 Sep;19(9):731-40. [Article]
  4. Arrang JM: [The histamine H3 receptor: a new target for the treatment of arousal and cognitive disorders]. Ann Pharm Fr. 2007 Jul;65(4):275-84. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Agonist
General Function
Histamine receptor activity
Specific Function
The H4 subclass of histamine receptors could mediate the histamine signals in peripheral tissues. Displays a significant level of constitutive activity (spontaneous activity in the absence of agoni...
Gene Name
HRH4
Uniprot ID
Q9H3N8
Uniprot Name
Histamine H4 receptor
Molecular Weight
44495.375 Da
References
  1. Blaya B, Nicolau-Galmes F, Jangi SM, Ortega-Martinez I, Alonso-Tejerina E, Burgos-Bretones J, Perez-Yarza G, Asumendi A, Boyano MD: Histamine and histamine receptor antagonists in cancer biology. Inflamm Allergy Drug Targets. 2010 Jul;9(3):146-57. [Article]
  2. Yu B, Shao Y, Li P, Zhang J, Zhong Q, Yang H, Hu X, Chen B, Peng X, Wu Q, Chen Y, Guan M, Wan J, Zhang W: Copy number variations of the human histamine H4 receptor gene are associated with systemic lupus erythematosus. Br J Dermatol. 2010 Nov;163(5):935-40. doi: 10.1111/j.1365-2133.2010.09928.x. [Article]
  3. Cowden JM, Riley JP, Ma JY, Thurmond RL, Dunford PJ: Histamine H4 receptor antagonism diminishes existing airway inflammation and dysfunction via modulation of Th2 cytokines. Respir Res. 2010 Jun 24;11:86. doi: 10.1186/1465-9921-11-86. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Monoamine transmembrane transporter activity
Specific Function
Involved in the ATP-dependent vesicular transport of biogenic amine neurotransmitters. Pumps cytosolic monoamines including dopamine, norepinephrine, serotonin, and histamine into synaptic vesicles...
Gene Name
SLC18A2
Uniprot ID
Q05940
Uniprot Name
Synaptic vesicular amine transporter
Molecular Weight
55712.075 Da
References
  1. Gonzalez AM, Walther D, Pazos A, Uhl GR: Synaptic vesicular monoamine transporter expression: distribution and pharmacologic profile. Brain Res Mol Brain Res. 1994 Mar;22(1-4):219-26. [Article]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Histamine n-methyltransferase activity
Specific Function
Inactivates histamine by N-methylation. Plays an important role in degrading histamine and in regulating the airway response to histamine.
Gene Name
HNMT
Uniprot ID
P50135
Uniprot Name
Histamine N-methyltransferase
Molecular Weight
33294.765 Da
References
  1. Garcia-Martin E, Ayuso P, Martinez C, Blanca M, Agundez JA: Histamine pharmacogenomics. Pharmacogenomics. 2009 May;10(5):867-83. doi: 10.2217/pgs.09.26. [Article]
  2. Okinaga S, Ohrui T, Nakazawa H, Yamauchi K, Sakurai E, Watanabe T, Sekizawa K, Sasaki H: The role of HMT (histamine N-methyltransferase) in airways: a review. Methods Find Exp Clin Pharmacol. 1995 Nov;17 Suppl C:16-20. [Article]

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Quaternary ammonium group transmembrane transporter activity
Specific Function
Mediates tubular uptake of organic compounds from circulation. Mediates the influx of agmatine, dopamine, noradrenaline (norepinephrine), serotonin, choline, famotidine, ranitidine, histamin, creat...
Gene Name
SLC22A2
Uniprot ID
O15244
Uniprot Name
Solute carrier family 22 member 2
Molecular Weight
62579.99 Da
References
  1. Urakami Y, Akazawa M, Saito H, Okuda M, Inui K: cDNA cloning, functional characterization, and tissue distribution of an alternatively spliced variant of organic cation transporter hOCT2 predominantly expressed in the human kidney. J Am Soc Nephrol. 2002 Jul;13(7):1703-10. [Article]
  2. Grundemann D, Liebich G, Kiefer N, Koster S, Schomig E: Selective substrates for non-neuronal monoamine transporters. Mol Pharmacol. 1999 Jul;56(1):1-10. [Article]
  3. Urakami Y, Okuda M, Masuda S, Akazawa M, Saito H, Inui K: Distinct characteristics of organic cation transporters, OCT1 and OCT2, in the basolateral membrane of renal tubules. Pharm Res. 2001 Nov;18(11):1528-34. [Article]
  4. Busch AE, Karbach U, Miska D, Gorboulev V, Akhoundova A, Volk C, Arndt P, Ulzheimer JC, Sonders MS, Baumann C, Waldegger S, Lang F, Koepsell H: Human neurons express the polyspecific cation transporter hOCT2, which translocates monoamine neurotransmitters, amantadine, and memantine. Mol Pharmacol. 1998 Aug;54(2):342-52. [Article]
  5. Arndt P, Volk C, Gorboulev V, Budiman T, Popp C, Ulzheimer-Teuber I, Akhoundova A, Koppatz S, Bamberg E, Nagel G, Koepsell H: Interaction of cations, anions, and weak base quinine with rat renal cation transporter rOCT2 compared with rOCT1. Am J Physiol Renal Physiol. 2001 Sep;281(3):F454-68. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Secondary active organic cation transmembrane transporter activity
Specific Function
Translocates a broad array of organic cations with various structures and molecular weights including the model compounds 1-methyl-4-phenylpyridinium (MPP), tetraethylammonium (TEA), N-1-methylnico...
Gene Name
SLC22A1
Uniprot ID
O15245
Uniprot Name
Solute carrier family 22 member 1
Molecular Weight
61153.345 Da
References
  1. Grundemann D, Liebich G, Kiefer N, Koster S, Schomig E: Selective substrates for non-neuronal monoamine transporters. Mol Pharmacol. 1999 Jul;56(1):1-10. [Article]
  2. Urakami Y, Okuda M, Masuda S, Akazawa M, Saito H, Inui K: Distinct characteristics of organic cation transporters, OCT1 and OCT2, in the basolateral membrane of renal tubules. Pharm Res. 2001 Nov;18(11):1528-34. [Article]
  3. Busch AE, Quester S, Ulzheimer JC, Gorboulev V, Akhoundova A, Waldegger S, Lang F, Koepsell H: Monoamine neurotransmitter transport mediated by the polyspecific cation transporter rOCT1. FEBS Lett. 1996 Oct 21;395(2-3):153-6. [Article]
  4. Arndt P, Volk C, Gorboulev V, Budiman T, Popp C, Ulzheimer-Teuber I, Akhoundova A, Koppatz S, Bamberg E, Nagel G, Koepsell H: Interaction of cations, anions, and weak base quinine with rat renal cation transporter rOCT2 compared with rOCT1. Am J Physiol Renal Physiol. 2001 Sep;281(3):F454-68. [Article]
  5. Yee SW, Lin L, Merski M, Keiser MJ, Gupta A, Zhang Y, Chien HC, Shoichet BK, Giacomini KM: Prediction and validation of enzyme and transporter off-targets for metformin. J Pharmacokinet Pharmacodyn. 2015 Oct;42(5):463-75. doi: 10.1007/s10928-015-9436-y. Epub 2015 Sep 3. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Toxin transporter activity
Specific Function
Mediates potential-dependent transport of a variety of organic cations. May play a significant role in the disposition of cationic neurotoxins and neurotransmitters in the brain.
Gene Name
SLC22A3
Uniprot ID
O75751
Uniprot Name
Solute carrier family 22 member 3
Molecular Weight
61279.485 Da
References
  1. Grundemann D, Liebich G, Kiefer N, Koster S, Schomig E: Selective substrates for non-neuronal monoamine transporters. Mol Pharmacol. 1999 Jul;56(1):1-10. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Symporter activity
Specific Function
Sodium-ion dependent, high affinity carnitine transporter. Involved in the active cellular uptake of carnitine. Transports one sodium ion with one molecule of carnitine. Also transports organic cat...
Gene Name
SLC22A5
Uniprot ID
O76082
Uniprot Name
Solute carrier family 22 member 5
Molecular Weight
62751.08 Da
References
  1. Ohashi R, Tamai I, Nezu Ji J, Nikaido H, Hashimoto N, Oku A, Sai Y, Shimane M, Tsuji A: Molecular and physiological evidence for multifunctionality of carnitine/organic cation transporter OCTN2. Mol Pharmacol. 2001 Feb;59(2):358-66. [Article]

Drug created at November 18, 2007 18:24 / Updated at February 20, 2024 23:55