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Identification
- Summary
Choline is a nutrient found in a wide variety of vitamins including pre-natal formulations.
- Generic Name
- Choline
- DrugBank Accession Number
- DB00122
- Background
A basic constituent of lecithin that is found in many plants and animal organs. It is important as a precursor of acetylcholine, as a methyl donor in various metabolic processes, and in lipid metabolism.
- Type
- Small Molecule
- Groups
- Approved, Nutraceutical
- Structure
Structure for Choline (DB00122)
- Weight
- Average: 104.1708
Monoisotopic: 104.107539075 - Chemical Formula
- C5H14NO
- Synonyms
- Bilineurine
- Choline ion
- N-trimethylethanolamine
- N,N,N-trimethylethanol-ammonium
- trimethylethanolamine
- Vitamin J
Pharmacology
- Indication
For nutritional supplementation, also for treating dietary shortage or imbalance
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- Contraindications & Blackbox Warnings
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This compound is needed for good nerve conduction throughout the CNS (central nervous system) as it is a precursor to acetylcholine (ACh). Choline is also needed for gallbladder regulation, liver function and lecithin (a key lipid) formation. Choline also aids in fat and cholesterol metabolism and prevents excessive fat build up in the liver. Choline has been used to mitigate the effects of Parkinsonism and tardive dyskinesia. Choline deficiencies may result in excessive build-up of fat in the liver, high blood pressure, gastric ulcers, kidney and liver dysfunction and stunted growth.
- Mechanism of action
Choline is a major part of the polar head group of phosphatidylcholine. Phosphatidylcholine's role in the maintenance of cell membrane integrity is vital to all of the basic biological processes: information flow, intracellular communication and bioenergetics. Inadequate choline intake would negatively affect all these processes. Choline is also a major part of another membrane phospholipid, sphingomyelin, also important for the maintenance of cell structure and function. It is noteworthy and not surprising that choline deficiency in cell culture causes apoptosis or programmed cell death. This appears to be due to abnormalities in cell membrane phosphatidylcholine content and an increase in ceramide, a precursor, as well as a metabolite, of sphingomyelin. Ceramide accumulation, which is caused by choline deficiency, appears to activate Caspase, a type of enzyme that mediates apoptosis. Betaine or trimethylglycine is derived from choline via an oxidation reaction. Betaine is one of the factors that maintains low levels of homocysteine by resynthesizing L-methionine from homocysteine. Elevated homocysteine levels are a significant risk factor for atherosclerosis, as well as other cardiovascular and neurological disorders. Acetylcholine is one of the major neurotransmitters and requires choline for its synthesis. Adequate acetylcholine levels in the brain are believed to be protective against certain types of dementia, including Alzheimer's disease.
Target Actions Organism ANeuronal acetylcholine receptor subunit alpha-2 inhibitorHumans UNeuronal acetylcholine receptor subunit alpha-7 Not Available Humans UCholine-phosphate cytidylyltransferase B product ofHumans UAcetylcholinesterase product ofHumans UCholine-phosphate cytidylyltransferase A product ofHumans UPhospholipase D2 product ofHumans UCholinesterase product ofHumans UPhospholipase D1 product ofHumans UPhosphoethanolamine/phosphocholine phosphatase product ofHumans - Absorption
Not Available
- Volume of distribution
Not Available
- Protein binding
Not Available
- Metabolism
- Not Available
- Route of elimination
Not Available
- Half-life
Not Available
- Clearance
Not Available
- Adverse Effects
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Oral rat LD50: 3400 mg/kg
- Pathways
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- 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 softwareAcetylcholine The risk or severity of adverse effects can be increased when Choline is combined with Acetylcholine. Acyclovir The risk or severity of adverse effects can be increased when Choline is combined with Acyclovir. Amantadine The serum concentration of Amantadine can be increased when it is combined with Choline. Amiloride The serum concentration of Choline can be increased when it is combined with Amiloride. Aminohippuric acid The serum concentration of Choline can be increased when it is combined with Aminohippuric acid. - 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 Choline bitartrate 6K2W7T9V6Y 87-67-2 QWJSAWXRUVVRLH-LREBCSMRSA-M Choline chloride 45I14D8O27 67-48-1 Not applicable - Over the Counter Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Choline 250 mg Tablet 250 mg Oral Swiss Herbal Remedies Ltd. 1971-12-31 2004-09-03 Canada 
Choline 250mg Tablet 250 mg Oral Great Earth Companies, Inc. 1998-08-25 2002-10-02 Canada Choline 250mg Tablet 250 mg Oral General Nutrition Canada Inc. 1997-04-18 2005-08-05 Canada Choline Bitartrate 100mg-tab Tablet 100 mg / tab Oral International Nutrition Ltd. 1996-07-26 2001-08-17 Canada Choline Bitartrate 500 Mg - Tablet Tablet 500 mg / tab Oral Health Wise Nutrition Inc. 1997-08-15 1998-08-25 Canada - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image 24 Multivitamins + Minerals Choline bitartrate (25 mg) + Ascorbic acid (150 mg) + Beta carotene (10000 unit) + Biotin (25 mcg) + Calcium (130 mg) + Cholecalciferol (400 unit) + Chromium (20 mcg) + Copper (1 mg) + Cyanocobalamin (25 mcg) + Ferrous fumarate (15 mg) + Folic acid (.8 mg) + Inositol (25 mg) + Magnesium (65 mg) + Manganese cation (2 mg) + Molybdenum (20 mcg) + Niacin (25 mg) + Calcium pantothenate (25 mg) + Potassium (15 mg) + Potassium Iodide (.1 mg) + Pyridoxine hydrochloride (25 mg) + Racemethionine (25 mg) + Riboflavin (25 mg) + Selenium (20 mcg) + Thiamine hydrochloride (25 mg) + Vanadium (20 mcg) + Vitamin A palmitate (5000 unit) + Vitamin E (50 unit) + Zinc (10 mg) Tablet Oral Stanley Pharmaceuticals, A Division Of Vita Health Products Inc. 1997-04-30 2002-07-31 Canada 50 Plus Choline bitartrate (20 mg) + Ascorbic acid (200 mg) + Biotin (20 mcg) + Cyanocobalamin (20 mcg) + Folic acid (.2 mg) + Inositol (20 mg) + Niacin (20 mg) + Calcium pantothenate (20 mg) + Pyridoxine hydrochloride (20 mg) + Racemethionine (20 mg) + Riboflavin (20 mg) + Thiamine hydrochloride (20 mg) + Vitamin A palmitate (10000 unit) + Vitamin D (400 unit) + Vitamin E (20 unit) Tablet Oral Quest Vitamins A Div Of Purity Life Health Products 1998-08-04 2001-07-06 Canada Advanced 2000 Capsules Choline (15 mg) + Chromium (50 mcg) + Inositol (15 mg) + Manganese cation (1 mg) + Pantothenic acid (15 mg) + Pyridoxine hydrochloride (4 mg) Capsule Oral Body Gold, A Division Of Pep Products, Inc. 2000-01-01 2002-08-22 Canada Alertonic Choline (2.222 mg / mL) + Inositol (2.222 mg / mL) + Nicotinamide (1.111 mg / mL) + Pipradrol hydrochloride (.044 mg / mL) + Pyridoxine hydrochloride (.042 mg / mL) + Riboflavin (.111 mg / mL) + Thiamine hydrochloride (.222 mg / mL) Liquid Oral Merrell Pharms Inc., Division Of Merrell Dow (Can) 1967-12-31 1996-09-09 Canada Alertonic Choline (2.222 mg / mL) + Inositol (2.222 mg / mL) + Nicotinamide (1.111 mg / mL) + Pipradrol hydrochloride (0.044 mg / mL) + Pyridoxine hydrochloride (0.042 mg / mL) + Riboflavin (0.111 mg / mL) + Thiamine hydrochloride (0.222 mg / mL) Elixir Oral Odan Laboratories Ltd 1995-12-31 2020-06-04 Canada - Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Cavan Prenatal Choline bitartrate (55 mg/1) + Ascorbic acid (120 mg/1) + Calcium carbonate (200 mg/1) + Cholecalciferol (420 [iU]/1) + Cyanocobalamin (8 ug/1) + Ferrous fumarate (28 mg/1) + Folic acid (1 mg/1) + Niacin (20 mg/1) + Potassium Iodide (150 ug/1) + Pyridoxine hydrochloride (50 mg/1) + Riboflavin (3 mg/1) + Thiamine mononitrate (3 mg/1) + Vitamin E (30 [iU]/1) + Zinc oxide (15 ug/1) Tablet Oral Seton Pharmaceuticals 2009-07-09 2009-07-22 US 
Duet DHA Balanced Choline (55 mg/1) + Ascorbic acid (120 mg/1) + Beta carotene (2800 [iU]/1) + Calcium carbonate (215 mg/1) + Cholecalciferol (640 [iU]/1) + Cupric oxide (1.8 mg/1) + Cyanocobalamin (12 ug/1) + D-alpha-Tocopherol acetate (15 mg/1) + Folic acid (1 mg/1) + Iodine (210 ug/1) + Iron (25 mg/1) + Magnesium (25 mg/1) + Nicotinamide (20 mg/1) + Omega-3 fatty acids (267 mg/1) + Pyridoxine hydrochloride (50 mg/1) + Riboflavin (2 mg/1) + Sodium selenate (65 ug/1) + Thiamine mononitrate (1.5 mg/1) + Zinc oxide (25 mg/1) Capsule, gelatin coated; Kit; Tablet Oral Eckson Labs, LLC 2012-10-30 Not applicable US Gabavale-5 Choline (125 mg/1) + Diazepam (5 mg/1) Kit Oral Physician Therapeutics Llc 2011-05-07 Not applicable US Gabazolamine Choline (125 mg/1) + Alprazolam (0.25 mg/1) Kit Oral Physician Therapeutics Llc 2011-07-07 Not applicable US Gabazolamine-0.5 Choline (125 mg/1) + Alprazolam (0.5 mg/1) Kit Oral Physician Therapeutics Llc 2011-07-07 Not applicable US
Categories
- Drug Categories
- Alcohols
- Amines
- Amino Alcohols
- Analgesics
- Antimetabolites
- Central Nervous System Agents
- Dietary Supplements
- Ethanolamines
- Gastrointestinal Agents
- Hypolipidemic Agents
- Lipid Regulating Agents
- Lipotropic Agents
- Nervous System
- Nootropic Agents
- OCT1 inhibitors
- OCT1 substrates
- OCT2 Inhibitors
- OCT2 Substrates
- Onium Compounds
- Other Nutritional Agents
- Quaternary Ammonium Compounds
- Salicylic Acid and Derivatives
- Supplements
- Trimethyl Ammonium Compounds
- Vitamin B Complex
- Vitamins
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as cholines. These are organic compounds containing a N,N,N-trimethylethanolammonium cation.
- Kingdom
- Organic compounds
- Super Class
- Organic nitrogen compounds
- Class
- Organonitrogen compounds
- Sub Class
- Quaternary ammonium salts
- Direct Parent
- Cholines
- Alternative Parents
- Tetraalkylammonium salts / 1,2-aminoalcohols / Primary alcohols / Organopnictogen compounds / Organic salts / Hydrocarbon derivatives / Organic cations
- Substituents
- 1,2-aminoalcohol / Alcohol / Aliphatic acyclic compound / Alkanolamine / Amine / Choline / Hydrocarbon derivative / Organic cation / Organic oxygen compound / Organic salt
- Molecular Framework
- Aliphatic acyclic compounds
- External Descriptors
- cholines (CHEBI:15354) / Pesticides (C00114) / a small molecule (CHOLINE)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- N91BDP6H0X
- CAS number
- 62-49-7
- InChI Key
- OEYIOHPDSNJKLS-UHFFFAOYSA-N
- InChI
- InChI=1S/C5H14NO/c1-6(2,3)4-5-7/h7H,4-5H2,1-3H3/q+1
- IUPAC Name
- (2-hydroxyethyl)trimethylazanium
- SMILES
- C[N+](C)(C)CCO
References
- Synthesis Reference
Satishchandra P. Patel, Vinayak T. Bhalani, "Solid choline magnesium salicylate composition and method of preparing same." U.S. Patent US5043168, issued May, 1954.
US5043168- General References
- Not Available
- External Links
- Human Metabolome Database
- HMDB0000097
- KEGG Drug
- D07690
- KEGG Compound
- C00114
- PubChem Compound
- 305
- PubChem Substance
- 46508132
- ChemSpider
- 299
- BindingDB
- 50026220
- 2449
- ChEBI
- 15354
- ChEMBL
- CHEMBL920
- ZINC
- ZINC000003079337
- PharmGKB
- PA448976
- PDBe Ligand
- CHT
- PDRhealth
- PDRhealth Drug Page
- Wikipedia
- Choline
- PDB Entries
- 1gvm / 1h8g / 1hcx / 1oba / 1p0m / 2fy3 / 2ha3 / 2reg / 2v04 / 2v05 … show 56 more
- MSDS
- Download (73.6 KB)
Clinical Trials
- Clinical Trials
Clinical Trial & Rare Diseases Add-on Data Package
Explore 4,000+ rare diseases, orphan drugs & condition pairs, clinical trial why stopped data, & more. Preview package Phase Status Purpose Conditions Count Start Date Why Stopped 100+ additional columns Unlock 175K+ rows when you subscribe.View sample dataNot Available Active Not Recruiting Treatment Under Nutrition 1 somestatus stop reason just information to hide Not Available Approved for Marketing Not Available Prostate Cancer 1 somestatus stop reason just information to hide Not Available Completed Diagnostic Latent Cancer (Prostate) 1 somestatus stop reason just information to hide Not Available Completed Treatment Cystic Fibrosis (CF) 1 somestatus stop reason just information to hide Not Available Completed Treatment Cystic Fibrosis Liver Disease 1 somestatus stop reason just information to hide
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Abbott Laboratories Ltd.
- Amend
- Caraco Pharmaceutical Labs
- Cypress Pharmaceutical Inc.
- Dispensing Solutions
- Diversified Healthcare Services Inc.
- Fournier Pharma Inc.
- Heartland Repack Services LLC
- Kaiser Foundation Hospital
- Key Co.
- Major Pharmaceuticals
- PD-Rx Pharmaceuticals Inc.
- Pharmaceutical Utilization Management Program VA Inc.
- Pliva Inc.
- Purdue Pharma LP
- Sandhills Packaging Inc.
- Silarx Pharmaceuticals
- United Research Laboratories Inc.
- Dosage Forms
Form Route Strength Elixir Oral Liquid Oral Solution Oral Tablet Oral Tablet Oral 250 mg Tablet Oral 100 mg / tab Tablet Oral 500 mg / tab Capsule Oral 350 mg / cap Tablet, extended release Oral 400 mg / tab Tablet Oral 250 mg / tab Tablet Oral 200 mg Tablet, film coated Tablet, delayed release Oral Injection Intramuscular Capsule, gelatin coated; kit; tablet Oral Tablet, film coated Oral Emulsion Parenteral Capsule, liquid filled; kit; tablet Oral Capsule Oral Tablet, extended release Oral Powder, for solution Oral Tablet, coated Oral Tablet, chewable Oral Capsule, gelatin coated Oral Kit Oral - Prices
Unit description Cost Unit Trilipix dr 135 mg capsule 4.38USD capsule Trilipix dr 45 mg capsule 1.46USD capsule Choline-10 tablet 0.06USD tablet Choline bitartrate crystals 0.03USD g DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
- Not Available
Properties
- State
- Liquid
- Experimental Properties
Property Value Source melting point (°C) 244-247 °C (as chloride salt) Not Available boiling point (°C) 113 °C Not Available water solubility Soluble Not Available - Predicted Properties
Property Value Source Water Solubility 3.61 mg/mL ALOGPS logP -3.6 ALOGPS logP -4.7 Chemaxon logS -1.6 ALOGPS pKa (Strongest Acidic) 13.97 Chemaxon pKa (Strongest Basic) -3.2 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 1 Chemaxon Hydrogen Donor Count 1 Chemaxon Polar Surface Area 20.23 Å2 Chemaxon Rotatable Bond Count 2 Chemaxon Refractivity 42.19 m3·mol-1 Chemaxon Polarizability 12.57 Å3 Chemaxon Number of Rings 0 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter No Chemaxon Veber's Rule Yes Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption - 0.964 Blood Brain Barrier + 0.9214 Caco-2 permeable + 0.8867 P-glycoprotein substrate Non-substrate 0.5169 P-glycoprotein inhibitor I Non-inhibitor 0.9881 P-glycoprotein inhibitor II Non-inhibitor 0.9543 Renal organic cation transporter Non-inhibitor 0.7651 CYP450 2C9 substrate Non-substrate 0.7719 CYP450 2D6 substrate Non-substrate 0.5882 CYP450 3A4 substrate Non-substrate 0.5505 CYP450 1A2 substrate Non-inhibitor 0.9193 CYP450 2C9 inhibitor Non-inhibitor 0.9496 CYP450 2D6 inhibitor Non-inhibitor 0.9231 CYP450 2C19 inhibitor Non-inhibitor 0.9497 CYP450 3A4 inhibitor Non-inhibitor 0.9904 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.9936 Ames test Non AMES toxic 0.9387 Carcinogenicity Carcinogens 0.5996 Biodegradation Ready biodegradable 0.7211 Rat acute toxicity 2.0491 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.8202 hERG inhibition (predictor II) Non-inhibitor 0.8071
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (â„«2) Source type Source [M-H]- 119.19381 predictedDeepCCS 1.0 (2019) [M+H]+ 122.34346 predictedDeepCCS 1.0 (2019) [M+Na]+ 131.11252 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
- Inhibitor
- General Function
- After binding acetylcholine, the AChR responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane
- Specific Function
- acetylcholine receptor activity
- Gene Name
- CHRNA2
- Uniprot ID
- Q15822
- Uniprot Name
- Neuronal acetylcholine receptor subunit alpha-2
- Molecular Weight
- 59764.82 Da
References
- Zhou Y, Zhang Y, Zhao D, Yu X, Shen X, Zhou Y, Wang S, Qiu Y, Chen Y, Zhu F: TTD: Therapeutic Target Database describing target druggability information. Nucleic Acids Res. 2024 Jan 5;52(D1):D1465-D1477. doi: 10.1093/nar/gkad751. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- After binding acetylcholine, the AChR responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane. The channel is blocked by alpha-bungarotoxin
- Specific Function
- acetylcholine binding
- Gene Name
- CHRNA7
- Uniprot ID
- P36544
- Uniprot Name
- Neuronal acetylcholine receptor subunit alpha-7
- Molecular Weight
- 56448.925 Da
References
- Zhao L, Kuo YP, George AA, Peng JH, Purandare MS, Schroeder KM, Lukas RJ, Wu J: Functional properties of homomeric, human alpha 7-nicotinic acetylcholine receptors heterologously expressed in the SH-EP1 human epithelial cell line. J Pharmacol Exp Ther. 2003 Jun;305(3):1132-41. Epub 2003 Mar 6. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Product of
- General Function
- Catalyzes the key rate-limiting step in the CDP-choline pathway for phosphatidylcholine biosynthesis
- Specific Function
- choline-phosphate cytidylyltransferase activity
- Gene Name
- PCYT1B
- Uniprot ID
- Q9Y5K3
- Uniprot Name
- Choline-phosphate cytidylyltransferase B
- Molecular Weight
- 41939.76 Da
References
- Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
- Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
- Wang L, Magdaleno S, Tabas I, Jackowski S: Early embryonic lethality in mice with targeted deletion of the CTP:phosphocholine cytidylyltransferase alpha gene (Pcyt1a). Mol Cell Biol. 2005 Apr;25(8):3357-63. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Product of
- General Function
- Hydrolyzes rapidly the acetylcholine neurotransmitter released into the synaptic cleft allowing to terminate the signal transduction at the neuromuscular junction. Role in neuronal apoptosis
- Specific Function
- acetylcholine binding
- Gene Name
- ACHE
- Uniprot ID
- P22303
- Uniprot Name
- Acetylcholinesterase
- Molecular Weight
- 67795.525 Da
References
- Amenta F, Tayebati SK, Vitali D, Di Tullio MA: Association with the cholinergic precursor choline alphoscerate and the cholinesterase inhibitor rivastigmine: an approach for enhancing cholinergic neurotransmission. Mech Ageing Dev. 2006 Feb;127(2):173-9. Epub 2005 Nov 16. [Article]
- Longobardi F, Solfrizzo M, Compagnone D, Del Carlo M, Visconti A: Use of electrochemical biosensor and gas chromatography for determination of dichlorvos in wheat. J Agric Food Chem. 2005 Nov 30;53(24):9389-94. [Article]
- Durcan N, Costello RW, McLean WG, Blusztajn J, Madziar B, Fenech AG, Hall IP, Gleich GJ, McGarvey L, Walsh MT: Eosinophil-mediated cholinergic nerve remodeling. Am J Respir Cell Mol Biol. 2006 Jun;34(6):775-86. Epub 2006 Feb 2. [Article]
- Alkondon M, Albuquerque EX: Subtype-specific inhibition of nicotinic acetylcholine receptors by choline: a regulatory pathway. J Pharmacol Exp Ther. 2006 Jul;318(1):268-75. Epub 2006 Mar 24. [Article]
- Anzai J: [Use of biosensors for detecting organophosphorus agents]. Yakugaku Zasshi. 2006 Dec;126(12):1301-8. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Product of
- General Function
- Catalyzes the key rate-limiting step in the CDP-choline pathway for phosphatidylcholine biosynthesis
- Specific Function
- calmodulin binding
- Gene Name
- PCYT1A
- Uniprot ID
- P49585
- Uniprot Name
- Choline-phosphate cytidylyltransferase A
- Molecular Weight
- 41730.67 Da
References
- Enaw JO, Zhu H, Yang W, Lu W, Shaw GM, Lammer EJ, Finnell RH: CHKA and PCYT1A gene polymorphisms, choline intake and spina bifida risk in a California population. BMC Med. 2006 Dec 21;4:36. [Article]
- Li L, She H, Yue SJ, Qin XQ, Guan CX, Liu HJ, Luo ZQ: Role of c-fos gene in vasoactive intestinal peptide promoted synthesis of pulmonary surfactant phospholipids. Regul Pept. 2007 May 3;140(3):117-24. Epub 2007 Jan 10. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Product of
- General Function
- Function as phospholipase selective for phosphatidylcholine (PubMed:9582313). May have a role in signal-induced cytoskeletal regulation and/or endocytosis (By similarity)
- Specific Function
- phosphatidylinositol binding
- Gene Name
- PLD2
- Uniprot ID
- O14939
- Uniprot Name
- Phospholipase D2
- Molecular Weight
- 105986.1 Da
References
- Lee JS, Kim JH, Jang IH, Kim HS, Han JM, Kazlauskas A, Yagisawa H, Suh PG, Ryu SH: Phosphatidylinositol (3,4,5)-trisphosphate specifically interacts with the phox homology domain of phospholipase D1 and stimulates its activity. J Cell Sci. 2005 Oct 1;118(Pt 19):4405-13. [Article]
- Singh AT, Frohman MA, Stern PH: Parathyroid hormone stimulates phosphatidylethanolamine hydrolysis by phospholipase D in osteoblastic cells. Lipids. 2005 Nov;40(11):1135-40. [Article]
- Paruch S, Heinis M, Lemay J, Hoeffel G, Maranon C, Hosmalin A, Perianin A: CCR5 signaling through phospholipase D involves p44/42 MAP-kinases and promotes HIV-1 LTR-directed gene expression. FASEB J. 2007 Dec;21(14):4038-46. Epub 2007 Jul 12. [Article]
- Szumilo M, Rahden-Staron I: [Phospholipase D in mammalian cells: structure, properties, physiological and pathological role]. Postepy Hig Med Dosw (Online). 2006;60:421-30. [Article]
- Fensome-Green A, Cockcroft S: Reconstitution system based on cytosol-depleted cells to study the regulation of phospholipase D. Methods Mol Biol. 2006;332:299-310. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Product of
- General Function
- Esterase with broad substrate specificity. Contributes to the inactivation of the neurotransmitter acetylcholine. Can degrade neurotoxic organophosphate esters
- Specific Function
- acetylcholinesterase activity
- Gene Name
- BCHE
- Uniprot ID
- P06276
- Uniprot Name
- Cholinesterase
- Molecular Weight
- 68417.575 Da
References
- Hsieh BC, Matsumoto K, Cheng TJ, Yuu G, Chen RL: Choline biosensor constructed with chitinous membrane from soldier crab and its application in measuring cholinesterase inhibitory activities. J Pharm Biomed Anal. 2007 Nov 30;45(4):673-8. Epub 2007 Jan 24. [Article]
- Amenta F, Tayebati SK, Vitali D, Di Tullio MA: Association with the cholinergic precursor choline alphoscerate and the cholinesterase inhibitor rivastigmine: an approach for enhancing cholinergic neurotransmission. Mech Ageing Dev. 2006 Feb;127(2):173-9. Epub 2005 Nov 16. [Article]
- Lurie S, Sadan O, Oron G, Fux A, Boaz M, Ezri T, Golan A, Bar J: Reduced pseudocholinesterase activity in patients with HELLP syndrome. Reprod Sci. 2007 Feb;14(2):192-6. [Article]
- Calaf GM, Roy D: Gene expression signature of parathion-transformed human breast epithelial cells. Int J Mol Med. 2007 May;19(5):741-50. [Article]
- Stoytcheva M, Zlatev R, Valdez B, Magnin JP, Velkova Z: Electrochemical sensor based on Arthrobacter globiformis for cholinesterase activity determination. Biosens Bioelectron. 2006 Jul 15;22(1):1-9. Epub 2005 Dec 20. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Product of
- General Function
- Function as phospholipase selective for phosphatidylcholine (PubMed:25936805, PubMed:8530346, PubMed:9582313). Implicated as a critical step in numerous cellular pathways, including signal transduction, membrane trafficking, and the regulation of mitosis. May be involved in the regulation of perinuclear intravesicular membrane traffic (By similarity)
- Specific Function
- phosphatidylinositol binding
- Gene Name
- PLD1
- Uniprot ID
- Q13393
- Uniprot Name
- Phospholipase D1
- Molecular Weight
- 124183.135 Da
References
- Lee JS, Kim JH, Jang IH, Kim HS, Han JM, Kazlauskas A, Yagisawa H, Suh PG, Ryu SH: Phosphatidylinositol (3,4,5)-trisphosphate specifically interacts with the phox homology domain of phospholipase D1 and stimulates its activity. J Cell Sci. 2005 Oct 1;118(Pt 19):4405-13. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Product of
- General Function
- Phosphatase that has a high activity toward phosphoethanolamine (PEA) and phosphocholine (PCho) (PubMed:15175005). Involved in the generation of inorganic phosphate for bone mineralization (By similarity). Acts in a non-redundant manner with PHOSPHO1 in skeletal mineralization: while PHOSPHO1 mediates the initiation of hydroxyapatite crystallization in the matrix vesicles (MVs), ALPL/TNAP catalyzes the spread of hydroxyapatite crystallization in the extracellular matrix (By similarity)
- Specific Function
- metal ion binding
- Gene Name
- PHOSPHO1
- Uniprot ID
- Q8TCT1
- Uniprot Name
- Phosphoethanolamine/phosphocholine phosphatase
- Molecular Weight
- 29712.54 Da
References
- Sahashi K, Yamada-Kato N, Maeda T, Kito K, Cha-Um S, Rai V, Tanaka Y, Takabe T: Expression and functional characterization of sugar beet phosphoethanolamine/phosphocholine phosphatase under salt stress. Plant Physiol Biochem. 2019 Sep;142:211-216. doi: 10.1016/j.plaphy.2019.07.011. Epub 2019 Jul 9. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Catalyzes both phosphatidylcholine and phosphatidylethanolamine biosynthesis from CDP-choline and CDP-ethanolamine, respectively (PubMed:10191259, PubMed:10893425, PubMed:12216837, PubMed:37137909). Involved in protein-dependent process of phospholipid transport to distribute phosphatidyl choline to the lumenal surface (PubMed:10191259, PubMed:10893425, PubMed:12216837). Has a higher cholinephosphotransferase activity than ethanolaminephosphotransferase activity (PubMed:10191259, PubMed:12216837)
- Specific Function
- 1-alkenyl-2-acylglycerol choline phosphotransferase activity
- Gene Name
- CEPT1
- Uniprot ID
- Q9Y6K0
- Uniprot Name
- Choline/ethanolaminephosphotransferase 1
- Molecular Weight
- 46553.135 Da
References
- Wright MM, McMaster CR: PC and PE synthesis: mixed micellar analysis of the cholinephosphotransferase and ethanolaminephosphotransferase activities of human choline/ethanolamine phosphotransferase 1 (CEPT1). Lipids. 2002 Jul;37(7):663-72. [Article]
- Henneberry AL, Wistow G, McMaster CR: Cloning, genomic organization, and characterization of a human cholinephosphotransferase. J Biol Chem. 2000 Sep 22;275(38):29808-15. [Article]
- Henneberry AL, McMaster CR: Cloning and expression of a human choline/ethanolaminephosphotransferase: synthesis of phosphatidylcholine and phosphatidylethanolamine. Biochem J. 1999 Apr 15;339 ( Pt 2):291-8. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Has a key role in phospholipid metabolism, and catalyzes the first step of phosphatidylethanolamine and phosphatidylcholine biosynthesis
- Specific Function
- ATP binding
- Gene Name
- CHKB
- Uniprot ID
- Q9Y259
- Uniprot Name
- Choline/ethanolamine kinase
- Molecular Weight
- 45270.99 Da
References
- Sher RB, Aoyama C, Huebsch KA, Ji S, Kerner J, Yang Y, Frankel WN, Hoppel CL, Wood PA, Vance DE, Cox GA: A rostrocaudal muscular dystrophy caused by a defect in choline kinase beta, the first enzyme in phosphatidylcholine biosynthesis. J Biol Chem. 2006 Feb 24;281(8):4938-48. Epub 2005 Dec 21. [Article]
- Eliyahu G, Kreizman T, Degani H: Phosphocholine as a biomarker of breast cancer: molecular and biochemical studies. Int J Cancer. 2007 Apr 15;120(8):1721-30. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Catalyzes the reversible synthesis of acetylcholine (ACh) from acetyl CoA and choline at cholinergic synapses
- Specific Function
- choline O-acetyltransferase activity
- Gene Name
- CHAT
- Uniprot ID
- P28329
- Uniprot Name
- Choline O-acetyltransferase
- Molecular Weight
- 82535.025 Da
References
- Kim AR, Dobransky T, Rylett RJ, Shilton BH: Surface-entropy reduction used in the crystallization of human choline acetyltransferase. Acta Crystallogr D Biol Crystallogr. 2005 Sep;61(Pt 9):1306-10. Epub 2005 Aug 16. [Article]
- Bikopoulos GJ, Hoque T, Webb RA: Infection with the cestode Hymenolepis diminuta induces changes in acetylcholine metabolism and muscarinic receptor mRNA expression in the rat jejunum. Parasitol Res. 2006 Aug;99(3):231-7. Epub 2006 Mar 16. [Article]
- Opazo P, Saud K, de Saint Pierre M, Cardenas AM, Allen DD, Segura-Aguilar J, Caviedes R, Caviedes P: Knockdown of amyloid precursor protein normalizes cholinergic function in a cell line derived from the cerebral cortex of a trisomy 16 mouse: An animal model of down syndrome. J Neurosci Res. 2006 Nov 1;84(6):1303-10. [Article]
- Kim AR, Rylett RJ, Shilton BH: Substrate binding and catalytic mechanism of human choline acetyltransferase. Biochemistry. 2006 Dec 12;45(49):14621-31. [Article]
- Mehl A, Schanke TM, Torvik A, Fonnum F: The effect of trichlorfon and methylazoxymethanol on the development of guinea pig cerebellum. Toxicol Appl Pharmacol. 2007 Mar;219(2-3):128-35. Epub 2006 Nov 1. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Plays a key role in phospholipid biosynthesis by catalyzing the phosphorylation of free choline to phosphocholine, the first step in phosphatidylcholine biosynthesis (PubMed:17007874, PubMed:19915674, PubMed:23416529, PubMed:34077757). Also phosphorylates ethanolamine, thereby contributing to phosphatidylethanolamine biosynthesis (PubMed:17007874, PubMed:19915674). Has higher activity with choline (PubMed:17007874, PubMed:19915674). May contribute to tumor cell growth (PubMed:19915674)
- Specific Function
- ATP binding
- Gene Name
- CHKA
- Uniprot ID
- P35790
- Uniprot Name
- Choline kinase alpha
- Molecular Weight
- 52248.53 Da
References
- Li Z, Agellon LB, Vance DE: Phosphatidylcholine homeostasis and liver failure. J Biol Chem. 2005 Nov 11;280(45):37798-802. Epub 2005 Sep 6. [Article]
- Glunde K, Raman V, Mori N, Bhujwalla ZM: RNA interference-mediated choline kinase suppression in breast cancer cells induces differentiation and reduces proliferation. Cancer Res. 2005 Dec 1;65(23):11034-43. [Article]
- Malito E, Sekulic N, Too WC, Konrad M, Lavie A: Elucidation of human choline kinase crystal structures in complex with the products ADP or phosphocholine. J Mol Biol. 2006 Nov 24;364(2):136-51. Epub 2006 Sep 3. [Article]
- Eliyahu G, Kreizman T, Degani H: Phosphocholine as a biomarker of breast cancer: molecular and biochemical studies. Int J Cancer. 2007 Apr 15;120(8):1721-30. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Not Available
- Specific Function
- choline dehydrogenase activity
- Gene Name
- CHDH
- Uniprot ID
- Q8NE62
- Uniprot Name
- Choline dehydrogenase, mitochondrial
- Molecular Weight
- 65358.005 Da
References
- Slow S, Garrow TA: Liver choline dehydrogenase and kidney betaine-homocysteine methyltransferase expression are not affected by methionine or choline intake in growing rats. J Nutr. 2006 Sep;136(9):2279-83. [Article]
- Bidulescu A, Chambless LE, Siega-Riz AM, Zeisel SH, Heiss G: Usual choline and betaine dietary intake and incident coronary heart disease: the Atherosclerosis Risk in Communities (ARIC) study. BMC Cardiovasc Disord. 2007 Jul 13;7:20. [Article]
- Quan R, Shang M, Zhang H, Zhao Y, Zhang J: Engineering of enhanced glycine betaine synthesis improves drought tolerance in maize. Plant Biotechnol J. 2004 Nov;2(6):477-86. [Article]
- Dalmeijer GW, Olthof MR, Verhoef P, Bots ML, van der Schouw YT: Prospective study on dietary intakes of folate, betaine, and choline and cardiovascular disease risk in women. Eur J Clin Nutr. 2008 Mar;62(3):386-94. Epub 2007 Mar 21. [Article]
- da Costa KA, Kozyreva OG, Song J, Galanko JA, Fischer LM, Zeisel SH: Common genetic polymorphisms affect the human requirement for the nutrient choline. FASEB J. 2006 Jul;20(9):1336-44. [Article]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- General Function
- Electrogenic voltage-dependent transporter that mediates the transport of a variety of organic cations such as endogenous bioactive amines, cationic drugs and xenobiotics (PubMed:9260930, PubMed:9687576). Functions as a Na(+)-independent, bidirectional uniporter (PubMed:21128598, PubMed:9687576). Cation cellular uptake or release is driven by the electrochemical potential, i.e. membrane potential and concentration gradient (PubMed:15212162, PubMed:9260930, PubMed:9687576). However, may also engage electroneutral cation exchange when saturating concentrations of cation substrates are reached (By similarity). Predominantly expressed at the basolateral membrane of hepatocytes and proximal tubules and involved in the uptake and disposition of cationic compounds by hepatic and renal clearance from the blood flow (PubMed:15783073). Implicated in monoamine neurotransmitters uptake such as histamine, dopamine, adrenaline/epinephrine, noradrenaline/norepinephrine, serotonin and tyramine, thereby supporting a physiological role in the central nervous system by regulating interstitial concentrations of neurotransmitters (PubMed:16581093, PubMed:17460754, PubMed:9687576). Also capable of transporting dopaminergic neuromodulators cyclo(his-pro), salsolinol and N-methyl-salsolinol, thereby involved in the maintenance of dopaminergic cell integrity in the central nervous system (PubMed:17460754). Mediates the bidirectional transport of acetylcholine (ACh) at the apical membrane of ciliated cell in airway epithelium, thereby playing a role in luminal release of ACh from bronchial epithelium (PubMed:15817714). Also transports guanidine and endogenous monoamines such as vitamin B1/thiamine, creatinine and N-1-methylnicotinamide (NMN) (PubMed:12089365, PubMed:15212162, PubMed:17072098, PubMed:24961373, PubMed:9260930). Mediates the uptake and efflux of quaternary ammonium compound choline (PubMed:9260930). Mediates the bidirectional transport of polyamine agmatine and the uptake of polyamines putrescine and spermidine (PubMed:12538837, PubMed:21128598). Able to transport non-amine endogenous compounds such as prostaglandin E2 (PGE2) and prostaglandin F2-alpha (PGF2-alpha) (PubMed:11907186). Also involved in the uptake of xenobiotic 4-(4-(dimethylamino)styryl)-N-methylpyridinium (ASP) (PubMed:12395288, PubMed:16394027). May contribute to regulate the transport of organic compounds in testis across the blood-testis-barrier (Probable)
- Specific Function
- acetylcholine transmembrane transporter activity
- Gene Name
- SLC22A2
- Uniprot ID
- O15244
- Uniprot Name
- Solute carrier family 22 member 2
- Molecular Weight
- 62579.99 Da
References
- Sweet DH, Miller DS, Pritchard JB: Ventricular choline transport: a role for organic cation transporter 2 expressed in choroid plexus. J Biol Chem. 2001 Nov 9;276(45):41611-9. Epub 2001 Sep 11. [Article]
- 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]
- Kakehi M, Koyabu N, Nakamura T, Uchiumi T, Kuwano M, Ohtani H, Sawada Y: Functional characterization of mouse cation transporter mOCT2 compared with mOCT1. Biochem Biophys Res Commun. 2002 Aug 23;296(3):644-50. [Article]
- Okuda M, Urakami Y, Saito H, Inui K: Molecular mechanisms of organic cation transport in OCT2-expressing Xenopus oocytes. Biochim Biophys Acta. 1999 Mar 4;1417(2):224-31. [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]
- Gorboulev V, Ulzheimer JC, Akhoundova A, Ulzheimer-Teuber I, Karbach U, Quester S, Baumann C, Lang F, Busch AE, Koepsell H: Cloning and characterization of two human polyspecific organic cation transporters. DNA Cell Biol. 1997 Jul;16(7):871-81. [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]
- Budiman T, Bamberg E, Koepsell H, Nagel G: Mechanism of electrogenic cation transport by the cloned organic cation transporter 2 from rat. J Biol Chem. 2000 Sep 22;275(38):29413-20. [Article]
- Pan G, Winter TN, Roberts JC, Fairbanks CA, Elmquist WF: Organic cation uptake is enhanced in bcrp1-transfected MDCKII cells. Mol Pharm. 2010 Feb 1;7(1):138-45. doi: 10.1021/mp900177r. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- General Function
- Electrogenic voltage-dependent transporter that mediates the transport of a variety of organic cations such as endogenous bioactive amines, cationic drugs and xenobiotics (PubMed:11388889, PubMed:11408531, PubMed:12439218, PubMed:12719534, PubMed:15389554, PubMed:16263091, PubMed:16272756, PubMed:16581093, PubMed:19536068, PubMed:21128598, PubMed:23680637, PubMed:24961373, PubMed:34040533, PubMed:9187257, PubMed:9260930, PubMed:9655880). Functions as a pH- and Na(+)-independent, bidirectional transporter (By similarity). Cation cellular uptake or release is driven by the electrochemical potential (i.e. membrane potential and concentration gradient) and substrate selectivity (By similarity). Hydrophobicity is a major requirement for recognition in polyvalent substrates and inhibitors (By similarity). Primarily expressed at the basolateral membrane of hepatocytes and proximal tubules and involved in the uptake and disposition of cationic compounds by hepatic and renal clearance from the blood flow (By similarity). Most likely functions as an uptake carrier in enterocytes contributing to the intestinal elimination of organic cations from the systemic circulation (PubMed:16263091). Transports endogenous monoamines such as N-1-methylnicotinamide (NMN), guanidine, histamine, neurotransmitters dopamine, serotonin and adrenaline (PubMed:12439218, PubMed:24961373, PubMed:35469921, PubMed:9260930). Also transports natural polyamines such as spermidine, agmatine and putrescine at low affinity, but relatively high turnover (PubMed:21128598). Involved in the hepatic uptake of vitamin B1/thiamine, hence regulating hepatic lipid and energy metabolism (PubMed:24961373). Mediates the bidirectional transport of acetylcholine (ACh) at the apical membrane of ciliated cell in airway epithelium, thereby playing a role in luminal release of ACh from bronchial epithelium (PubMed:15817714). Transports dopaminergic neuromodulators cyclo(his-pro) and salsolinol with lower efficency (PubMed:17460754). Also capable of transporting non-amine endogenous compounds such as prostaglandin E2 (PGE2) and prostaglandin F2-alpha (PGF2-alpha) (PubMed:11907186). May contribute to the transport of cationic compounds in testes across the blood-testis-barrier (Probable). Also involved in the uptake of xenobiotics tributylmethylammonium (TBuMA), quinidine, N-methyl-quinine (NMQ), N-methyl-quinidine (NMQD) N-(4,4-azo-n-pentyl)-quinuclidine (APQ), azidoprocainamide methoiodide (AMP), N-(4,4-azo-n-pentyl)-21-deoxyajmalinium (APDA) and 4-(4-(dimethylamino)styryl)-N-methylpyridinium (ASP) (PubMed:11408531, PubMed:15389554, PubMed:35469921, PubMed:9260930)
- Specific Function
- (R)-carnitine transmembrane transporter activity
- Gene Name
- SLC22A1
- Uniprot ID
- O15245
- Uniprot Name
- Solute carrier family 22 member 1
- Molecular Weight
- 61153.345 Da
References
- Kakehi M, Koyabu N, Nakamura T, Uchiumi T, Kuwano M, Ohtani H, Sawada Y: Functional characterization of mouse cation transporter mOCT2 compared with mOCT1. Biochem Biophys Res Commun. 2002 Aug 23;296(3):644-50. [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]
- Jonker JW, Wagenaar E, Mol CA, Buitelaar M, Koepsell H, Smit JW, Schinkel AH: Reduced hepatic uptake and intestinal excretion of organic cations in mice with a targeted disruption of the organic cation transporter 1 (Oct1 [Slc22a1]) gene. Mol Cell Biol. 2001 Aug;21(16):5471-7. [Article]
- Sinclair CJ, Chi KD, Subramanian V, Ward KL, Green RM: Functional expression of a high affinity mammalian hepatic choline/organic cation transporter. J Lipid Res. 2000 Nov;41(11):1841-8. [Article]
- Green RM, Lo K, Sterritt C, Beier DR: Cloning and functional expression of a mouse liver organic cation transporter. Hepatology. 1999 May;29(5):1556-62. [Article]
- Busch AE, Quester S, Ulzheimer JC, Waldegger S, Gorboulev V, Arndt P, Lang F, Koepsell H: Electrogenic properties and substrate specificity of the polyspecific rat cation transporter rOCT1. J Biol Chem. 1996 Dec 20;271(51):32599-604. [Article]
- Sweet DH, Miller DS, Pritchard JB: Ventricular choline transport: a role for organic cation transporter 2 expressed in choroid plexus. J Biol Chem. 2001 Nov 9;276(45):41611-9. Epub 2001 Sep 11. [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]
- Gorboulev V, Volk C, Arndt P, Akhoundova A, Koepsell H: Selectivity of the polyspecific cation transporter rOCT1 is changed by mutation of aspartate 475 to glutamate. Mol Pharmacol. 1999 Dec;56(6):1254-61. [Article]
- Friedrich A, George RL, Bridges CC, Prasad PD, Ganapathy V: Transport of choline and its relationship to the expression of the organic cation transporters in a rat brain microvessel endothelial cell line (RBE4). Biochim Biophys Acta. 2001 Jun 6;1512(2):299-307. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Electrogenic voltage-dependent transporter that mediates the transport of a variety of organic cations such as endogenous bioactive amines, cationic drugs and xenobiotics (PubMed:10196521, PubMed:10966924, PubMed:12538837, PubMed:17460754, PubMed:20858707). Cation cellular uptake or release is driven by the electrochemical potential, i.e. membrane potential and concentration gradient (PubMed:10966924). Functions as a Na(+)- and Cl(-)-independent, bidirectional uniporter (PubMed:12538837). Implicated in monoamine neurotransmitters uptake such as dopamine, adrenaline/epinephrine, noradrenaline/norepinephrine, histamine, serotonin and tyramine, thereby supporting a role in homeostatic regulation of aminergic neurotransmission in the brain (PubMed:10196521, PubMed:16581093, PubMed:20858707). Transports dopaminergic neuromodulators cyclo(his-pro) and salsolinol with low efficiency (PubMed:17460754). May be involved in the uptake and disposition of cationic compounds by renal clearance from the blood flow (PubMed:10966924). May contribute to regulate the transport of cationic compounds in testis across the blood-testis-barrier (Probable). Mediates the transport of polyamine spermidine and putrescine (By similarity). Mediates the bidirectional transport of polyamine agmatine (PubMed:12538837). Also transports guanidine (PubMed:10966924). May also mediate intracellular transport of organic cations, thereby playing a role in amine metabolism and intracellular signaling (By similarity)
- Specific Function
- monoamine transmembrane transporter activity
- Gene Name
- SLC22A3
- Uniprot ID
- O75751
- Uniprot Name
- Solute carrier family 22 member 3
- Molecular Weight
- 61279.485 Da
References
- Kekuda R, Prasad PD, Wu X, Wang H, Fei YJ, Leibach FH, Ganapathy V: Cloning and functional characterization of a potential-sensitive, polyspecific organic cation transporter (OCT3) most abundantly expressed in placenta. J Biol Chem. 1998 Jun 26;273(26):15971-9. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General 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 (PubMed:10454528, PubMed:10525100, PubMed:10966938, PubMed:17509700, PubMed:20722056, PubMed:33124720). Also transports organic cations such as tetraethylammonium (TEA) without the involvement of sodium. Relative uptake activity ratio of carnitine to TEA is 11.3 (PubMed:10454528, PubMed:10525100, PubMed:10966938). In intestinal epithelia, transports the quorum-sensing pentapeptide CSF (competence and sporulation factor) from Bacillus Subtilis wich induces cytoprotective heat shock proteins contributing to intestinal homeostasis (PubMed:18005709). May also contribute to regulate the transport of organic compounds in testis across the blood-testis-barrier (Probable)
- Specific Function
- (R)-carnitine transmembrane transporter activity
- Gene Name
- SLC22A5
- Uniprot ID
- O76082
- Uniprot Name
- Organic cation/carnitine transporter 2
- Molecular Weight
- 62751.08 Da
References
- Wu X, Prasad PD, Leibach FH, Ganapathy V: cDNA sequence, transport function, and genomic organization of human OCTN2, a new member of the organic cation transporter family. Biochem Biophys Res Commun. 1998 May 29;246(3):589-95. [Article]
- Wu X, Huang W, Prasad PD, Seth P, Rajan DP, Leibach FH, Chen J, Conway SJ, Ganapathy V: Functional characteristics and tissue distribution pattern of organic cation transporter 2 (OCTN2), an organic cation/carnitine transporter. J Pharmacol Exp Ther. 1999 Sep;290(3):1482-92. [Article]
- Tamai I, Ohashi R, Nezu JI, Sai Y, Kobayashi D, Oku A, Shimane M, Tsuji A: Molecular and functional characterization of organic cation/carnitine transporter family in mice. J Biol Chem. 2000 Dec 22;275(51):40064-72. [Article]
- 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]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Transporter that mediates the transport of endogenous and microbial zwitterions and organic cations (PubMed:10215651, PubMed:15107849, PubMed:15795384, PubMed:16729965, PubMed:20601551, PubMed:22206629, PubMed:22569296, PubMed:29530864). Functions as a Na(+)-dependent and pH-dependent high affinity microbial symporter of potent food-derived antioxidant ergothioeine (PubMed:15795384, PubMed:29530864, PubMed:33124720). Transports one sodium ion with one ergothioeine molecule (By similarity). Involved in the absorption of ergothioneine from the luminal/apical side of the small intestine and renal tubular cells, and into non-parenchymal liver cells, thereby contributing to maintain steady-state ergothioneine level in the body (PubMed:20601551). Also mediates the bidirectional transport of acetycholine, although the exact transport mechanism has not been fully identified yet (PubMed:22206629). Most likely exports anti-inflammatory acetylcholine in non-neuronal tissues, thereby contributing to the non-neuronal cholinergic system (PubMed:22206629, PubMed:22569296). Displays a general physiological role linked to better survival by controlling inflammation and oxidative stress, which may be related to ergothioneine and acetycholine transports (PubMed:15795384, PubMed:22206629). May also function as a low-affinity Na(+)-dependent transporter of L-carnitine through the mitochondrial membrane, thereby maintaining intracellular carnitine homeostasis (PubMed:10215651, PubMed:15107849, PubMed:16729965). May contribute to regulate the transport of cationic compounds in testis across the blood-testis-barrier (PubMed:35307651)
- Specific Function
- acetylcholine transmembrane transporter activity
- Gene Name
- SLC22A4
- Uniprot ID
- Q9H015
- Uniprot Name
- Solute carrier family 22 member 4
- Molecular Weight
- 62154.48 Da
References
- Yabuuchi H, Tamai I, Nezu J, Sakamoto K, Oku A, Shimane M, Sai Y, Tsuji A: Novel membrane transporter OCTN1 mediates multispecific, bidirectional, and pH-dependent transport of organic cations. J Pharmacol Exp Ther. 1999 May;289(2):768-73. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Choline/H+ antiporter (PubMed:19357133, PubMed:23651124, PubMed:31855247, PubMed:33789160). Also acts as a high-affinity ethanolamine/H+ antiporter, regulating the supply of extracellular ethanolamine (Etn) for the CDP-Etn pathway, redistribute intracellular Etn and balance the CDP-Cho and CDP-Etn arms of the Kennedy pathway (PubMed:33789160). Involved in membrane synthesis and myelin production (PubMed:31855247)
- Specific Function
- antiporter activity
- Gene Name
- SLC44A1
- Uniprot ID
- Q8WWI5
- Uniprot Name
- Choline transporter-like protein 1
- Molecular Weight
- 73301.28 Da
References
- Inazu M, Takeda H, Matsumiya T: Molecular and functional characterization of an Na+-independent choline transporter in rat astrocytes. J Neurochem. 2005 Sep;94(5):1427-37. Epub 2005 Jul 5. [Article]
- Fullerton MD, Wagner L, Yuan Z, Bakovic M: Impaired trafficking of choline transporter-like protein-1 at plasma membrane and inhibition of choline transport in THP-1 monocyte-derived macrophages. Am J Physiol Cell Physiol. 2006 Apr;290(4):C1230-8. Epub 2005 Nov 30. [Article]
- Tomi M, Arai K, Tachikawa M, Hosoya K: Na(+)-independent choline transport in rat retinal capillary endothelial cells. Neurochem Res. 2007 Nov;32(11):1833-42. Epub 2007 May 23. [Article]
- Ishiguro N, Oyabu M, Sato T, Maeda T, Minami H, Tamai I: Decreased biosynthesis of lung surfactant constituent phosphatidylcholine due to inhibition of choline transporter by gefitinib in lung alveolar cells. Pharm Res. 2008 Feb;25(2):417-27. Epub 2007 Jul 12. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Choline transporter that plays a role in the choline-acetylcholine system and is required to the efferent innervation of hair cells in the olivocochlear bundle for the maintenance of physiological function of outer hair cells and the protection of hair cells from acoustic injury (By similarity) (PubMed:23651124, PubMed:28013291). Also described as a thiamine pyrophosphate transporter in colon, may mediate the absorption of microbiota-generated thiamine pyrophosphate and contribute to host thiamine (vitamin B1) homeostasis (PubMed:24379411, PubMed:26741288)
- Specific Function
- antiporter activity
- Gene Name
- SLC44A4
- Uniprot ID
- Q53GD3
- Uniprot Name
- Choline transporter-like protein 4
- Molecular Weight
- 79252.975 Da
References
- Tomi M, Arai K, Tachikawa M, Hosoya K: Na(+)-independent choline transport in rat retinal capillary endothelial cells. Neurochem Res. 2007 Nov;32(11):1833-42. Epub 2007 May 23. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Choline/H+ antiporter, mainly in mitochodria (PubMed:10677542, PubMed:20665236, PubMed:23651124, PubMed:33789160). Also acts as a low-affinity ethanolamine/H+ antiporter, regulating the supply of extracellular ethanolamine (Etn) for the CDP-Etn pathway, redistribute intracellular Etn and balance the CDP-Cho and CDP-Etn arms of the Kennedy pathway (PubMed:33789160)
- Specific Function
- antiporter activity
- Gene Name
- SLC44A2
- Uniprot ID
- Q8IWA5
- Uniprot Name
- Choline transporter-like protein 2
- Molecular Weight
- 80122.695 Da
References
- Nair TS, Kommareddi PK, Galano MM, Miller DM, Kakaraparthi BN, Telian SA, Arts HA, El-Kashlan H, Kilijanczyk A, Lassig AA, Graham MP, Fisher SG, Stoll SW, Nair RP, Elder JT, Carey TE: SLC44A2 single nucleotide polymorphisms, isoforms, and expression: Association with severity of Meniere's disease? Genomics. 2016 Dec;108(5-6):201-208. doi: 10.1016/j.ygeno.2016.11.002. Epub 2016 Nov 6. [Article]
- Inazu M: Functional Expression of Choline Transporters in the Blood-Brain Barrier. Nutrients. 2019 Sep 20;11(10). pii: nu11102265. doi: 10.3390/nu11102265. [Article]
- Iwao B, Yara M, Hara N, Kawai Y, Yamanaka T, Nishihara H, Inoue T, Inazu M: Functional expression of choline transporter like-protein 1 (CTL1) and CTL2 in human brain microvascular endothelial cells. Neurochem Int. 2016 Feb;93:40-50. doi: 10.1016/j.neuint.2015.12.011. Epub 2015 Dec 31. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Not Available
- Specific Function
- choline transmembrane transporter activity
- Gene Name
- SLC44A3
- Uniprot ID
- Q8N4M1
- Uniprot Name
- Choline transporter-like protein 3
- Molecular Weight
- 73782.63 Da
References
- Tomi M, Arai K, Tachikawa M, Hosoya K: Na(+)-independent choline transport in rat retinal capillary endothelial cells. Neurochem Res. 2007 Nov;32(11):1833-42. Epub 2007 May 23. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- High-affinity Na(+)-coupled choline transmembrane symporter (PubMed:11027560, PubMed:11068039, PubMed:12237312, PubMed:12969261, PubMed:17005849, PubMed:23132865, PubMed:23141292, PubMed:27569547). Functions as an electrogenic, voltage-dependent transporter with variable charge/choline stoichiometry (PubMed:17005849). Choline uptake and choline-induced current is also Cl(-)-dependent where Cl(-) is likely a regulatory ion rather than cotransported ion (PubMed:11068039, PubMed:12237312, PubMed:17005849). Plays a critical role in acetylcholine (ACh) synthesis by taking up the substrate choline from the synaptic cleft into the presynaptic nerve terminals after neurotransmitter release (PubMed:27569547). SLC5A7/CHT1-mediated choline high-affinity transport in cholinergic neurons is the rate-limiting step for production of ACh, thereby facilitating communication by subsequent action potentials (PubMed:11027560). Localized predominantly in presynaptic terminal intracellular organelles, and translocated to the plasma membrane in active form in response to neuronal activity (PubMed:12969261, PubMed:15953352)
- Specific Function
- choline binding
- Gene Name
- SLC5A7
- Uniprot ID
- Q9GZV3
- Uniprot Name
- High affinity choline transporter 1
- Molecular Weight
- 63202.985 Da
References
- Ribeiro FM, Black SA, Cregan SP, Prado VF, Prado MA, Rylett RJ, Ferguson SS: Constitutive high-affinity choline transporter endocytosis is determined by a carboxyl-terminal tail dileucine motif. J Neurochem. 2005 Jul;94(1):86-96. [Article]
- Geldenhuys WJ, Lockman PR, Philip AE, McAfee JH, Miller BL, McCurdy CR, Allen DD: Inhibition of choline uptake by N-cyclohexylcholine, a high affinity ligand for the choline transporter at the blood-brain barrier. J Drug Target. 2005 May;13(4):259-66. [Article]
- Guidry G, Willison BD, Blakely RD, Landis SC, Habecker BA: Developmental expression of the high affinity choline transporter in cholinergic sympathetic neurons. Auton Neurosci. 2005 Dec 30;123(1-2):54-61. Epub 2005 Nov 8. [Article]
- Parikh V, Sarter M: Cortical choline transporter function measured in vivo using choline-sensitive microelectrodes: clearance of endogenous and exogenous choline and effects of removal of cholinergic terminals. J Neurochem. 2006 Apr;97(2):488-503. Epub 2006 Mar 15. [Article]
- Parikh V, Apparsundaram S, Kozak R, Richards JB, Sarter M: Reduced expression and capacity of the striatal high-affinity choline transporter in hyperdopaminergic mice. Neuroscience. 2006 Aug 11;141(1):379-89. Epub 2006 May 3. [Article]
Drug created at June 13, 2005 13:24 / Updated at October 15, 2024 05:47