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
Structure for Histamine (DB05381)
- 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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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Prophylaxis of Migraine ••• ••••• ••••••••• - Contraindications & Blackbox Warnings
Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- 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.
Target Actions Organism AHistamine H1 receptor agonistHumans AHistamine H2 receptor agonistHumans AHistamine H3 receptor agonistHumans UHistamine H4 receptor agonistHumans USynaptic vesicular amine transporter Not Available Humans - 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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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.
Drug Interaction Integrate drug-drug
interactions in your softwareAcyclovir The risk or severity of adverse effects can be increased when Acyclovir is combined with Histamine. Amantadine The serum concentration of Histamine can be increased when it is combined with Amantadine. Amiloride The serum concentration of Histamine can be increased when it is combined with Amiloride. Aminohippuric acid The serum concentration of Histamine can be increased when it is combined with Aminohippuric acid. Amiodarone The serum concentration of Histamine can be increased when it is combined with Amiodarone. - Food Interactions
- No interactions found.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Product Ingredients
Ingredient UNII CAS InChI Key Histamine dihydrochloride 3POA0Q644U 56-92-8 PPZMYIBUHIPZOS-UHFFFAOYSA-N Histamine phosphate QWB37T4WZZ 51-74-1 ZHIBQGJKHVBLJJ-UHFFFAOYSA-N - Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Ceplene Injection, solution 0.5 mg/0.5ml Subcutaneous Laboratoires Delbert 2016-09-20 Not applicable EU 
Histamine Phosphate Injection USP Liq Sc Liquid 1 mg / mL Subcutaneous Bioniche Pharma (Canada) Ltd 1994-12-31 2014-11-24 Canada 
Histamine Phosphate Injection USP, 1mg/ml Liquid 1 mg / mL Subcutaneous Alveda Pharmaceuticals Inc Not applicable Not applicable Canada Histamine Positive Skin Test Control Solution 2.75 mg/1mL Percutaneous ALK-Abello, Inc. 1989-10-23 Not applicable US 
Histamine Positive Skin Test Control Injection, solution 0.275 mg/1mL Intradermal ALK-Abello, Inc. 1989-10-23 Not applicable US - Over the Counter Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image AMINO ACTIVE Topical Analgesic Cream Cream 0.25 mg/1mL Topical VIREO SYSTEMS, INC. 2022-08-08 Not applicable US Arthritis Pain Relief Cream 0.025 g/100g Topical Walgreens 2022-11-01 Not applicable US Arthritis Pain Relief Cream 0.03 g/100g Topical PainX LLC 2022-11-07 Not applicable US Arthritis Pain Relief Cream Cream .00025 g/1g Topical Sombra Cosmetics, Inc. 2019-12-09 Not applicable US Australian Dream Back Pain Cream 0.05 g/100g Topical Nature's Health Connection 2014-07-10 2019-12-03 US - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Abee Med Histamine dihydrochloride (0.5 mg/1g) + Menthol (15 mg/1g) Cream Topical Crossover Telecom Llc 2016-05-25 Not applicable US ActivOn Ultra Strength Arthritis Histamine dihydrochloride (0.00028 g/1g) + Menthol (0.04574 g/1g) Stick Topical Family First Pharmaceuticals, Inc. 2011-09-01 Not applicable US Alo Therapeutic Massage Histamine dihydrochloride (1 mg/1mL) + Menthol (30 mg/1mL) Cream Topical Cmi Therapy Solutions 2016-11-10 Not applicable US Alo Therapeutic Massage Histamine dihydrochloride (0.1 g/100g) + Menthol (3 g/100g) Cream Topical Theraplex Solutions 2012-06-07 Not applicable US Alo Therapeutic Massage Histamine dihydrochloride (1 mg/1mL) + Menthol (30 mg/1mL) Cream Topical Cmi Therapy Solutions 2016-11-10 Not applicable US - Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Camphomex Histamine (0.03 mg/1mL) + Camphor (3.6 mg/1mL) + Menthol (12 mg/1mL) Spray Topical 1st Class Pharmaceuticals 2014-03-24 2016-01-15 US Simanix Histamine dihydrochloride (0.035 g/100g) + Capsaicin (0.0375 g/100g) + Menthol (3 g/100g) Cream Topical Home Aide Diagnostics, Inc. 2015-07-08 Not applicable US Simanix Histamine dihydrochloride (0.035 g/100g) + Capsaicin (0.0357 g/100g) + Menthol (3 g/100g) Cream Topical Home Aide Diagnostics, Inc. 2015-07-08 Not applicable US
Categories
- ATC Codes
- L03AX14 — Histamine dihydrochloride
- L03AX — Other immunostimulants
- L03A — IMMUNOSTIMULANTS
- L03 — IMMUNOSTIMULANTS
- L — ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
- Drug Categories
- Adjuvants, Immunologic
- Amines
- Antineoplastic and Immunomodulating Agents
- Autacoids
- Biogenic Amines
- Biogenic Monoamines
- Biological Factors
- Cytochrome P-450 CYP3A Inhibitors
- Cytochrome P-450 Enzyme Inhibitors
- Diagnostic Agents
- Ethylamines
- Gastric Function
- Histamine Agents
- Histamine Agonists
- Imidazoles
- Inflammation Mediators
- Neurotransmitter Agents
- OCT1 substrates
- OCT2 Inhibitors
- OCT2 Substrates
- Other Diagnostics
- Tests for Gastric Secretion
- 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
- 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]
- Silberstein SD: Preventive Migraine Treatment. Continuum (Minneap Minn). 2015 Aug;21(4 Headache):973-89. doi: 10.1212/CON.0000000000000199. [Article]
- DailyMed: Histamine positive test control injection [Link]
- BASG: ALK Prick Positiv Kontrolle (Histamine) Intradermal Solution [Link]
- External Links
- Human Metabolome Database
- HMDB0060263
- KEGG Drug
- D08040
- KEGG Compound
- C00388
- PubChem Compound
- 774
- PubChem Substance
- 175426988
- ChemSpider
- 753
- BindingDB
- 7966
- 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);">
Phase Status Purpose Conditions Count 4 Completed Treatment Acute Myeloid Leukemia 1 4 Recruiting Basic Science Normal Skin / Skin Photoaging 1 3 Completed Treatment Leukemias 1 3 Completed Treatment Osteoarthritis of the Knee 1 3 Unknown Status Treatment Melanoma / Metastatic Cancer 1
Pharmacoeconomics
- Manufacturers
- Eli lilly and co
- Packagers
- ALK-Abello Inc.
- Hollister-Stier Laboratories LLC
- Medisca Inc.
- Professional Co.
- Dosage Forms
Form Route Strength Stick Topical Solution Intradermal Solution Intradermal 10 mg/ml Solution Topical 1.7 mg/ml Cream Topical 0.03 g/100g Liquid Topical Cream Topical .0005 g/1g Cream Topical 0.25 mg/1g Cream Topical 0.3 mg/1g Spray Topical Injection, solution Subcutaneous 0.5 MG/0.5ML Cream Topical .025 g/100g Cream Topical 0.25 mg/1mL Cream Topical 0.05 g/100g Cream Topical .00025 g/1g Spray Topical 0.1 g/100mL Liquid Subcutaneous 1 mg / mL Injection, solution Intradermal 0.275 mg/1mL Solution Percutaneous 2.75 mg/1mL Solution Intradermal 0.275 mg / mL Solution Percutaneous 2.75 mg / mL Solution Lotion Topical 0.6 mg/1mL Ointment Topical Cream Topical 0.3 mg/1mL Gel Topical 0.5 mg/1mL Gel Topical 0.25 mg/1mL Cream Topical 0.025 g/100g Cream Topical Injection Percutaneous 6 mg/1mL Solution Percutaneous 6 mg / mL Cream Topical 0.4 mg/1mL Cream Topical 0.05 mg/100mg Cream Topical 0.00025 g/1g Solution 10 mg/1ml - Prices
Unit description Cost Unit Histamine phosphate 100% cryst 14.38USD g Histatrol 1:10000 vial 13.18USD ml Histamine di-hcl powder 12.6USD g DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 139 °C (phosphate salt) Not Available - Predicted Properties
Property Value Source Water Solubility 169.0 mg/mL ALOGPS logP -0.69 ALOGPS logP -0.7 Chemaxon logS 0.18 ALOGPS pKa (Strongest Acidic) 14.46 Chemaxon pKa (Strongest Basic) 9.58 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 2 Chemaxon Hydrogen Donor Count 2 Chemaxon Polar Surface Area 54.7 Å2 Chemaxon Rotatable Bond Count 2 Chemaxon Refractivity 31.66 m3·mol-1 Chemaxon Polarizability 12.08 Å3 Chemaxon Number of Rings 1 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter No Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.9931 Blood Brain Barrier + 0.8784 Caco-2 permeable - 0.5409 P-glycoprotein substrate Non-substrate 0.6136 P-glycoprotein inhibitor I Non-inhibitor 0.9639 P-glycoprotein inhibitor II Non-inhibitor 0.9013 Renal organic cation transporter Non-inhibitor 0.529 CYP450 2C9 substrate Non-substrate 0.8735 CYP450 2D6 substrate Non-substrate 0.7217 CYP450 3A4 substrate Non-substrate 0.7528 CYP450 1A2 substrate Non-inhibitor 0.8045 CYP450 2C9 inhibitor Non-inhibitor 0.8396 CYP450 2D6 inhibitor Non-inhibitor 0.8574 CYP450 2C19 inhibitor Non-inhibitor 0.9187 CYP450 3A4 inhibitor Non-inhibitor 0.7351 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.8404 Ames test Non AMES toxic 0.7103 Carcinogenicity Non-carcinogens 0.8747 Biodegradation Not ready biodegradable 0.9377 Rat acute toxicity 2.4808 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9413 hERG inhibition (predictor II) Non-inhibitor 0.8061
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 119.0188967 predictedDarkChem Lite v0.1.0 [M-H]- 118.7227967 predictedDarkChem Lite v0.1.0 [M-H]- 119.1770967 predictedDarkChem Lite v0.1.0 [M-H]- 121.41139 predictedDeepCCS 1.0 (2019) [M+H]+ 119.5835967 predictedDarkChem Lite v0.1.0 [M+H]+ 119.9786967 predictedDarkChem Lite v0.1.0 [M+H]+ 119.5310967 predictedDarkChem Lite v0.1.0 [M+H]+ 123.68864 predictedDeepCCS 1.0 (2019) [M+Na]+ 119.2326967 predictedDarkChem Lite v0.1.0 [M+Na]+ 119.2957967 predictedDarkChem Lite v0.1.0 [M+Na]+ 119.2931967 predictedDarkChem Lite v0.1.0 [M+Na]+ 131.81657 predictedDeepCCS 1.0 (2019)
Targets
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Use our structured and evidence-based datasets to unlock newinsights and accelerate drug research.
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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
- 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]
- 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]
- 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]
- 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]
- 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
- 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]
- Soga F, Katoh N, Kishimoto S: Histamine prevents apoptosis in human monocytes. Clin Exp Allergy. 2007 Mar;37(3):323-30. [Article]
- 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
- 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]
- 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]
- 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]
- 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
- 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]
- 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]
- 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
- 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
- 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]
- 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
- SubstrateInhibitor
- 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
- 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]
- 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]
- 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]
- 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]
- 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
- 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]
- 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]
- 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]
- 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]
- 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
- 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
- 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