Identification

Name
Choline
Accession Number
DB00122  (NUTR00020)
Type
Small Molecule
Groups
Approved, Nutraceutical
Description

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. [PubChem]

Structure
Thumb
Synonyms
  • Bilineurine
  • Choline
  • Choline ion
  • N-trimethylethanolamine
  • N,N,N-trimethylethanol-ammonium
  • trimethylethanolamine
Product Ingredients
IngredientUNIICASInChI Key
Choline bitartrate6K2W7T9V6Y87-67-2QWJSAWXRUVVRLH-LREBCSMRSA-M
Choline salicylateKD510K1IQW2016-36-6UDKCHVLMFQVBAA-UHFFFAOYSA-M
Over the Counter Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Choline 250 mgTablet250 mgOralSwiss Herbal Remedies Ltd.1971-12-312004-09-03Canada
Choline 250mgTablet250 mgOralGeneral Nutrition Canada Inc.1997-04-182005-08-05Canada
Choline 250mgTablet250 mgOralGreat Earth Companies, Inc.1998-08-252002-10-02Canada
Choline Bitartrate 100mg-tabTablet100 mgOralInternational Nutrition Ltd.1996-07-262001-08-17Canada
Choline Bitartrate 500 Mg - TabletTablet500 mgOralHealth Wise Nutrition Inc.1997-08-151998-08-25Canada
Choline Caps 350mgCapsule350 mgOralTwin Laboratories Inc.1995-12-311999-11-10Canada
Choline Ctr Srt 400mgTablet, extended release400 mgOralBioenergy Inc.1979-12-311998-06-03Canada
Choline Tab 250mgTablet250 mgOralGahler Enterprises Ltd.1984-12-312000-08-01Canada
Choline Tab 250mgTablet250 mgOralJamieson Laboratories Ltd1963-12-312000-09-08Canada
Choline Tab 250mgTablet250 mgOralVita Health Products Inc1976-12-311998-07-22Canada
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
Advanced 2000 CapsulesCholine (15 mg) + Chromium (50 mcg) + Inositol nicotinate (15 mg) + Manganese (1 mg) + Pantothenic acid (15 mg) + Pyridoxine hydrochloride (4 mg)CapsuleOralBody Gold, A Division Of Pep Products, Inc.2000-01-012002-08-22Canada
AlertonicCholine (2.222 mg) + Inositol nicotinate (2.222 mg) + Nicotinamide (1.111 mg) + Pipradrol hydrochloride (.044 mg) + Pyridoxine hydrochloride (.042 mg) + Riboflavin (.111 mg) + Thiamine Hydrochloride (.222 mg)LiquidOralMerrell Pharms Inc., Division Of Merrell Dow (Can)1967-12-311996-09-09Canada
AlertonicCholine (2.222 mg) + Inositol nicotinate (2.222 mg) + Nicotinamide (1.111 mg) + Pipradrol hydrochloride (0.044 mg) + Pyridoxine hydrochloride (0.042 mg) + Riboflavin (0.111 mg) + Thiamine Hydrochloride (0.222 mg)ElixirOralOdan Laboratories Ltd1995-12-31Not applicableCanada
American Eagle Energizer Plus Vitamin Supplement DrinkCholine (50 mg) + Cyanocobalamin (5 mg) + Inositol nicotinate (50 mg) + Niacin (20 mg) + Pantothenic acid (5 mg) + Pyridoxine (3 mg)LiquidOralP.S.W.C. Co., Inc.Not applicableNot applicableCanada
American Plus Energy & Vitamin DrinkCholine (50 mg) + Cyanocobalamin (5 mcg) + Inositol nicotinate (50 mg) + Niacin (20 mg) + Pantothenic acid (5 mg) + Pyridoxine (3 mg)LiquidOralP.S.W.C. Co., Inc.Not applicableNot applicableCanada
B 50 CapsulesCholine bitartrate (50 mg) + Biotin (50 mcg) + Cyanocobalamin (50 mcg) + Folic Acid (.4 mg) + Inositol nicotinate (50 mg) + Nicotinamide (50 mg) + Calcium pantothenate (50 mg) + Pyridoxine hydrochloride (50 mg) + Riboflavin (50 mg) + Thiamine mononitrate (50 mg)CapsuleOralRheingold Food International Ltd.1987-12-312007-07-26Canada
B Complex 25mg Vitamin SupplementCholine bitartrate (25 mg) + Biotin (25 mcg) + Cyanocobalamin (25 mcg) + Folic Acid (0.4 mg) + Inositol nicotinate (25 mg) + Nicotinamide (25 mg) + Pantothenic acid (25 mg) + Pyridoxine hydrochloride (25 mg) + Riboflavin (25 mg) + Thiamine Hydrochloride (25 mg)TabletOralGarden State Nutritionals1998-08-312000-06-07Canada
B Complex 50 Vitamin CapCholine bitartrate (50 mg) + Biotin (50 mcg) + Cyanocobalamin (55 mcg) + Folic Acid (.4 mg) + Inositol nicotinate (50 mg) + Nicotinamide (50 mg) + Pantothenic acid (50 mg) + Pyridoxine (50 mg) + Riboflavin (50 mg) + Thiamine (50 mg)CapsuleOralBioforce Canada Inc.1994-12-311997-07-22Canada
B Complex 50+ CapletCholine (50 mg) + Biotin (50 mcg) + Cyanocobalamin (100 mcg) + Folic Acid (1 mg) + Inositol nicotinate (50 mg) + Nicotinamide (50 mg) + Calcium pantothenate (100 mg) + Pyridoxine hydrochloride (50 mg) + Riboflavin (50 mg) + Thiamine mononitrate (50 mg)TabletOralHealth Wise Nutrition Inc.1994-12-312002-07-18Canada
B Compound 50mg TabCholine bitartrate (50 mg) + Biotin (50 mcg) + Cyanocobalamin (50 mcg) + Folic Acid (1 mg) + Inositol nicotinate (50 mg) + Nicotinamide (50 mg) + Pantothenic acid (50 mg) + Pyridoxine hydrochloride (50 mg) + Riboflavin (50 mg) + Thiamine Hydrochloride (50 mg)TabletOralGahler Enterprises Ltd.1987-12-312009-09-28Canada
Categories
UNII
N91BDP6H0X
CAS number
62-49-7
Weight
Average: 104.1708
Monoisotopic: 104.107539075
Chemical Formula
C5H14NO
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

Pharmacology

Indication

For nutritional supplementation, also for treating dietary shortage or imbalance

Structured Indications
Not Available
Pharmacodynamics

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.

TargetActionsOrganism
UCholine-phosphate cytidylyltransferase B
product of
Human
UAcetylcholinesterase
product of
Human
UCholine-phosphate cytidylyltransferase A
product of
Human
UPhospholipase D2
product of
Human
UCholinesterase
product of
Human
UPhospholipase D1
product of
Human
UPhosphoethanolamine/phosphocholine phosphatase
product of
Human
UNeuronal acetylcholine receptor subunit alpha-7Not AvailableHuman
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
Toxicity

Oral rat LD50: 3400 mg/kg

Affected organisms
  • Humans and other mammals
Pathways
PathwayCategory
Homocystinuria-megaloblastic anemia due to defect in cobalamin metabolism, cblG complementation typeDisease
Phosphatidylcholine Biosynthesis PC(14:0/22:1(13Z))Metabolic
Phosphatidylcholine Biosynthesis PC(14:1(9Z)/16:1(9Z))Metabolic
Phosphatidylcholine Biosynthesis PC(14:1(9Z)/18:1(9Z))Metabolic
Phosphatidylcholine Biosynthesis PC(14:1(9Z)/20:5(5Z,8Z,11Z,14Z,17Z))Metabolic
Phosphatidylcholine Biosynthesis PC(15:0/15:0)Metabolic
Phosphatidylcholine Biosynthesis PC(15:0/20:4(8Z,11Z,14Z,17Z))Metabolic
Phosphatidylcholine Biosynthesis PC(15:0/20:5(5Z,8Z,11Z,14Z,17Z))Metabolic
Phosphatidylcholine Biosynthesis PC(15:0/24:0)Metabolic
Phosphatidylcholine Biosynthesis PC(16:0/14:1(9Z))Metabolic
Phosphatidylcholine Biosynthesis PC(16:0/16:1(9Z))Metabolic
Phosphatidylcholine Biosynthesis PC(16:0/18:1(9Z))Metabolic
Phosphatidylcholine Biosynthesis PC(16:0/20:1(11Z))Metabolic
Phosphatidylcholine Biosynthesis PC(16:0/20:4(8Z,11Z,14Z,17Z))Metabolic
Phosphatidylcholine Biosynthesis PC(16:0/20:5(5Z,8Z,11Z,14Z,17Z))Metabolic
Phosphatidylcholine Biosynthesis PC(16:1(9Z)/14:0)Metabolic
Phosphatidylcholine Biosynthesis PC(16:1(9Z)/20:3(5Z,8Z,11Z))Metabolic
Phosphatidylcholine Biosynthesis PC(16:1(9Z)/20:3(8Z,11Z,14Z))Metabolic
Phosphatidylcholine Biosynthesis PC(16:1(9Z)/22:1(13Z))Metabolic
Phosphatidylcholine Biosynthesis PC(16:1(9Z)/22:4(7Z,10Z,13Z,16Z))Metabolic
Phosphatidylcholine Biosynthesis PC(18:0/16:1(9Z))Metabolic
Phosphatidylcholine Biosynthesis PC(18:0/18:0)Metabolic
Phosphatidylcholine Biosynthesis PC(18:0/20:1(11Z))Metabolic
Phosphatidylcholine Biosynthesis PC(18:0/24:0)Metabolic
Phosphatidylcholine Biosynthesis PC(18:1(11Z)/16:0)Metabolic
Phosphatidylcholine Biosynthesis PC(18:1(11Z)/18:2(9Z,12Z))Metabolic
Phosphatidylcholine Biosynthesis PC(18:1(11Z)/18:3(6Z,9Z,12Z))Metabolic
Phosphatidylcholine Biosynthesis PC(18:1(11Z)/18:3(9Z,12Z,15Z))Metabolic
Phosphatidylcholine Biosynthesis PC(18:1(11Z)/20:3(5Z,8Z,11Z))Metabolic
Phosphatidylcholine Biosynthesis PC(18:1(11Z)/20:3(8Z,11Z,14Z))Metabolic
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
BupropionThe serum concentration of Choline can be increased when it is combined with Bupropion.Approved
Food Interactions
Not Available

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
HMDB00097
KEGG Compound
C00114
PubChem Compound
305
PubChem Substance
46508132
ChemSpider
299
BindingDB
50026220
ChEBI
15354
ChEMBL
CHEMBL920
PharmGKB
PA448976
HET
CHT
PDRhealth
PDRhealth Drug Page
Wikipedia
Choline
ATC Codes
N02BA03 — Choline salicylate
AHFS Codes
  • 56:24.00 — Lipotropic Agents
  • 88:30.00* — Other Nutritional Agents
  • 88:08.00 — Vitamin B Complex
PDB Entries
1gvm / 1h8g / 1hcx / 1oba / 1p0m / 2fy3 / 2ha3 / 2reg / 2v04 / 2v05
show 27 more
MSDS
Download (73.6 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0Enrolling by InvitationBasic ScienceDietary Modifications / Nutrition1
1CompletedTreatmentChild's Development / Pregnancy1
1Not Yet RecruitingTreatmentChild's Development / Prenatal Stress1
1, 2CompletedTreatmentAlcohol Related Neurodevelopmental Disorder / Fetal Alcohol Spectrum Disorders / Fetal Alcohol Syndrome (FAS) / Partial Fetal Alcohol Syndrome / Prenatal Alcohol Exposure1
2RecruitingTreatmentFetal Alcohol Spectrum Disorders1
3RecruitingTreatmentType 2 Diabetes Mellitus1
4CompletedPreventionArsenic Metabolites Measured in Urine1
4CompletedTreatmentDiabetic Peripheral Neuropathic Pain1
4RecruitingTreatmentAutism, Early Infantile1
4TerminatedTreatmentInflammatory Reaction / Postoperative pain1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Dosage forms
FormRouteStrength
ElixirOral
CapsuleOral
Tablet, extended releaseOral
TabletOral250 mg
TabletOral100 mg
TabletOral500 mg
CapsuleOral350 mg
Tablet, extended releaseOral400 mg
TabletOral200 mg
SolutionOral
LiquidOral
TabletOral
Kit
KitOral
GelDental; Topical
Prices
Unit descriptionCostUnit
Trilipix dr 135 mg capsule4.38USD capsule
Trilipix dr 45 mg capsule1.46USD capsule
Choline-10 tablet0.06USD tablet
Choline bitartrate crystals0.03USD g
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Not Available

Properties

State
Liquid
Experimental Properties
PropertyValueSource
melting point (°C)244-247 °C (as chloride salt)Not Available
boiling point (°C)113 °CNot Available
water solubilitySolubleNot Available
Predicted Properties
PropertyValueSource
Water Solubility3.61 mg/mLALOGPS
logP-3.6ALOGPS
logP-4.7ChemAxon
logS-1.6ALOGPS
pKa (Strongest Acidic)13.97ChemAxon
pKa (Strongest Basic)-3.2ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count1ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area20.23 Å2ChemAxon
Rotatable Bond Count2ChemAxon
Refractivity42.19 m3·mol-1ChemAxon
Polarizability12.57 Å3ChemAxon
Number of Rings0ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterNoChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption-0.964
Blood Brain Barrier+0.9214
Caco-2 permeable+0.8867
P-glycoprotein substrateNon-substrate0.5169
P-glycoprotein inhibitor INon-inhibitor0.9881
P-glycoprotein inhibitor IINon-inhibitor0.9543
Renal organic cation transporterNon-inhibitor0.7651
CYP450 2C9 substrateNon-substrate0.7719
CYP450 2D6 substrateNon-substrate0.5882
CYP450 3A4 substrateNon-substrate0.5505
CYP450 1A2 substrateNon-inhibitor0.9193
CYP450 2C9 inhibitorNon-inhibitor0.9496
CYP450 2D6 inhibitorNon-inhibitor0.9231
CYP450 2C19 inhibitorNon-inhibitor0.9497
CYP450 3A4 inhibitorNon-inhibitor0.9904
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9936
Ames testNon AMES toxic0.9387
CarcinogenicityCarcinogens 0.5996
BiodegradationReady biodegradable0.7211
Rat acute toxicity2.0491 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8202
hERG inhibition (predictor II)Non-inhibitor0.8071
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
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
MS/MS Spectrum - Quattro_QQQ 10V, PositiveLC-MS/MSsplash10-0a4i-0900000000-ea6f9c1150759c5be6c7
MS/MS Spectrum - Quattro_QQQ 25V, PositiveLC-MS/MSsplash10-0a4i-1900000000-cadf16d18f093e9b19d6
MS/MS Spectrum - Quattro_QQQ 40V, PositiveLC-MS/MSsplash10-0bt9-9100000000-a2c328b7da5435b8e467
LC-MS/MS Spectrum - LC-ESI-QTOF (UPLC Q-Tof Premier, Waters) , PositiveLC-MS/MSsplash10-0udi-0900000000-6a7b57dbdf4560721722
LC-MS/MS Spectrum - LC-ESI-QTOF (UPLC Q-Tof Premier, Waters) 30V, PositiveLC-MS/MSsplash10-0udi-5900000000-87fdeef5275a74e78348
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-0w29-5900000000-9b79cc5ff3b1ce17deb1
LC-MS/MS Spectrum - LC-ESI-QQ , positiveLC-MS/MSsplash10-03di-9200000000-fe62d5a4fbf492493d60
LC-MS/MS Spectrum - LC-ESI-IT , positiveLC-MS/MSsplash10-0udi-3900000000-0b37e63e9c6b14a2e397
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-0udi-0900000000-6a7b57dbdf4560721722
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-0udi-5900000000-87fdeef5275a74e78348
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0pb9-1900000000-391c1b7859a03e776123
1H NMR Spectrum1D NMRNot Applicable
13C NMR Spectrum1D NMRNot Applicable
[1H,1H] 2D NMR Spectrum2D NMRNot Applicable
[1H,13C] 2D NMR Spectrum2D NMRNot Applicable

Taxonomy

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
Choline / Tetraalkylammonium salt / 1,2-aminoalcohol / Alkanolamine / Organic oxygen compound / Organopnictogen compound / Hydrocarbon derivative / Organic salt / Primary alcohol / Organooxygen compound
Molecular Framework
Aliphatic acyclic compounds
External Descriptors
cholines (CHEBI:15354) / Pesticides (C00114) / a small molecule (CHOLINE)

Targets

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Product of
General Function
Choline-phosphate cytidylyltransferase activity
Specific Function
Controls phosphatidylcholine synthesis.
Gene Name
PCYT1B
Uniprot ID
Q9Y5K3
Uniprot Name
Choline-phosphate cytidylyltransferase B
Molecular Weight
41939.76 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. 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. [PubMed:17016423]
  3. 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. [PubMed:15798219]
Details
2. Acetylcholinesterase
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Product of
General Function
Serine hydrolase activity
Specific Function
Terminates signal transduction at the neuromuscular junction by rapid hydrolysis of the acetylcholine released into the synaptic cleft. Role in neuronal apoptosis.
Gene Name
ACHE
Uniprot ID
P22303
Uniprot Name
Acetylcholinesterase
Molecular Weight
67795.525 Da
References
  1. 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. [PubMed:16297435]
  2. 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. [PubMed:16302752]
  3. 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. [PubMed:16456188]
  4. 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. [PubMed:16565162]
  5. Anzai J: [Use of biosensors for detecting organophosphorus agents]. Yakugaku Zasshi. 2006 Dec;126(12):1301-8. [PubMed:17139155]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Product of
General Function
Lipid binding
Specific Function
Controls phosphatidylcholine synthesis.
Gene Name
PCYT1A
Uniprot ID
P49585
Uniprot Name
Choline-phosphate cytidylyltransferase A
Molecular Weight
41730.67 Da
References
  1. 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. [PubMed:17184542]
  2. 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. [PubMed:17218027]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Product of
General Function
Phospholipase d activity
Specific Function
May have a role in signal-induced cytoskeletal regulation and/or endocytosis.
Gene Name
PLD2
Uniprot ID
O14939
Uniprot Name
Phospholipase D2
Molecular Weight
105986.1 Da
References
  1. 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. [PubMed:16179605]
  2. Singh AT, Frohman MA, Stern PH: Parathyroid hormone stimulates phosphatidylethanolamine hydrolysis by phospholipase D in osteoblastic cells. Lipids. 2005 Nov;40(11):1135-40. [PubMed:16459925]
  3. 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. [PubMed:17627030]
  4. 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. [PubMed:16921342]
  5. 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. [PubMed:16878701]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Product of
General Function
Identical protein binding
Specific Function
Esterase with broad substrate specificity. Contributes to the inactivation of the neurotransmitter acetylcholine. Can degrade neurotoxic organophosphate esters.
Gene Name
BCHE
Uniprot ID
P06276
Uniprot Name
Cholinesterase
Molecular Weight
68417.575 Da
References
  1. 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. [PubMed:17329059]
  2. 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. [PubMed:16297435]
  3. 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. [PubMed:17636231]
  4. Calaf GM, Roy D: Gene expression signature of parathion-transformed human breast epithelial cells. Int J Mol Med. 2007 May;19(5):741-50. [PubMed:17390078]
  5. 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. [PubMed:16376069]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Product of
General Function
Phospholipase d activity
Specific Function
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 int...
Gene Name
PLD1
Uniprot ID
Q13393
Uniprot Name
Phospholipase D1
Molecular Weight
124183.135 Da
References
  1. 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. [PubMed:16179605]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Product of
General Function
Pyrophosphatase activity
Specific Function
Phosphatase that has a high activity toward phosphoethanolamine (PEA) and phosphocholine (PCho). Involved in the generation of inorganic phosphate for bone mineralization.
Gene Name
PHOSPHO1
Uniprot ID
Q8TCT1
Uniprot Name
Phosphoethanolamine/phosphocholine phosphatase
Molecular Weight
29712.54 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. 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. [PubMed:17016423]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Toxic substance binding
Specific 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 cha...
Gene Name
CHRNA7
Uniprot ID
P36544
Uniprot Name
Neuronal acetylcholine receptor subunit alpha-7
Molecular Weight
56448.925 Da
References
  1. 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. [PubMed:12626641]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Metal ion binding
Specific Function
Catalyzes both phosphatidylcholine and phosphatidylethanolamine biosynthesis from CDP-choline and CDP-ethanolamine, respectively. Involved in protein-dependent process of phospholipid transport to ...
Gene Name
CEPT1
Uniprot ID
Q9Y6K0
Uniprot Name
Choline/ethanolaminephosphotransferase 1
Molecular Weight
46553.135 Da
References
  1. 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. [PubMed:12216837]
  2. 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. [PubMed:10893425]
  3. 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. [PubMed:10191259]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Ethanolamine kinase activity
Specific Function
Has a key role in phospholipid biosynthesis. Catalyzes the first step in phosphatidylethanolamine biosynthesis. Phosphorylates ethanolamine, and can also act on choline (in vitro). Has higher activ...
Gene Name
CHKB
Uniprot ID
Q9Y259
Uniprot Name
Choline/ethanolamine kinase
Molecular Weight
45270.99 Da
References
  1. 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. [PubMed:16371353]
  2. 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. [PubMed:17236204]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Choline o-acetyltransferase activity
Specific Function
Catalyzes the reversible synthesis of acetylcholine (ACh) from acetyl CoA and choline at cholinergic synapses.
Gene Name
CHAT
Uniprot ID
P28329
Uniprot Name
Choline O-acetyltransferase
Molecular Weight
82535.025 Da
References
  1. 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. [PubMed:16131766]
  2. 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. [PubMed:16541262]
  3. 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. [PubMed:16941497]
  4. Kim AR, Rylett RJ, Shilton BH: Substrate binding and catalytic mechanism of human choline acetyltransferase. Biochemistry. 2006 Dec 12;45(49):14621-31. [PubMed:17144655]
  5. 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. [PubMed:17150236]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Signal transducer activity
Specific Function
Has a key role in phospholipid biosynthesis and may contribute to tumor cell growth. Catalyzes the first step in phosphatidylcholine biosynthesis. Contributes to phosphatidylethanolamine biosynthes...
Gene Name
CHKA
Uniprot ID
P35790
Uniprot Name
Choline kinase alpha
Molecular Weight
52248.53 Da
References
  1. 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. [PubMed:16144842]
  2. 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. [PubMed:16322253]
  3. 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. [PubMed:17007874]
  4. 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. [PubMed:17236204]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Flavin adenine dinucleotide binding
Specific Function
Not Available
Gene Name
CHDH
Uniprot ID
Q8NE62
Uniprot Name
Choline dehydrogenase, mitochondrial
Molecular Weight
65358.005 Da
References
  1. 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. [PubMed:16920841]
  2. 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. [PubMed:17629908]
  3. 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. [PubMed:17147620]
  4. 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. [PubMed:17375117]
  5. 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. [PubMed:16816108]

Transporters

Kind
Protein
Organism
Human
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. 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. [PubMed:11553644]
  2. 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. [PubMed:12089365]
  3. 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. [PubMed:12176030]
  4. 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. [PubMed:10082798]
  5. 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. [PubMed:11758759]
  6. 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. [PubMed:9260930]
  7. 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. [PubMed:11502595]
  8. 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. [PubMed:10889205]
  9. 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. [PubMed:19886673]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
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. Bednarczyk D, Ekins S, Wikel JH, Wright SH: Influence of molecular structure on substrate binding to the human organic cation transporter, hOCT1. Mol Pharmacol. 2003 Mar;63(3):489-98. [PubMed:12606755]
  2. Zhang L, Dresser MJ, Gray AT, Yost SC, Terashita S, Giacomini KM: Cloning and functional expression of a human liver organic cation transporter. Mol Pharmacol. 1997 Jun;51(6):913-21. [PubMed:9187257]
  3. Zhang L, Schaner ME, Giacomini KM: Functional characterization of an organic cation transporter (hOCT1) in a transiently transfected human cell line (HeLa). J Pharmacol Exp Ther. 1998 Jul;286(1):354-61. [PubMed:9655880]
  4. 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. [PubMed:12176030]
  5. Zhang L, Dresser MJ, Chun JK, Babbitt PC, Giacomini KM: Cloning and functional characterization of a rat renal organic cation transporter isoform (rOCT1A). J Biol Chem. 1997 Jun 27;272(26):16548-54. [PubMed:9195965]
  6. 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. [PubMed:10082798]
  7. 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. [PubMed:11758759]
  8. 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. [PubMed:11463829]
  9. 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. [PubMed:11060354]
  10. 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. [PubMed:10216142]
  11. 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. [PubMed:8955087]
  12. 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. [PubMed:11553644]
  13. 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. [PubMed:10385678]
  14. 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. [PubMed:10570053]
Kind
Protein
Organism
Human
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. 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. [PubMed:9632645]
Kind
Protein
Organism
Human
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. 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. [PubMed:9618255]
  2. 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. [PubMed:10454528]
  3. 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. [PubMed:11010964]
  4. 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. [PubMed:11160873]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Symporter activity
Specific Function
Sodium-ion dependent, low affinity carnitine transporter. Probably transports one sodium ion with one molecule of carnitine. Also transports organic cations such as tetraethylammonium (TEA) without...
Gene Name
SLC22A4
Uniprot ID
Q9H015
Uniprot Name
Solute carrier family 22 member 4
Molecular Weight
62154.48 Da
References
  1. 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. [PubMed:10215651]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Choline transmembrane transporter activity
Specific Function
Choline transporter. May be involved in membrane synthesis and myelin production.
Gene Name
SLC44A1
Uniprot ID
Q8WWI5
Uniprot Name
Choline transporter-like protein 1
Molecular Weight
73301.28 Da
References
  1. 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. [PubMed:16000150]
  2. 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. [PubMed:16319125]
  3. 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. [PubMed:17520363]
  4. 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. [PubMed:17624579]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Not Available
Specific Function
Not Available
Gene Name
SLC44A4
Uniprot ID
Q53GD3
Uniprot Name
Choline transporter-like protein 4
Molecular Weight
79252.975 Da
References
  1. 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. [PubMed:17520363]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Signal transducer activity
Specific Function
Isoform 1, but not isoform 3, exhibits some choline transporter activity.
Gene Name
SLC44A2
Uniprot ID
Q8IWA5
Uniprot Name
Choline transporter-like protein 2
Molecular Weight
80122.695 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. 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. [PubMed:17016423]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Not Available
Specific Function
Not Available
Gene Name
SLC44A3
Uniprot ID
Q8N4M1
Uniprot Name
Choline transporter-like protein 3
Molecular Weight
73782.63 Da
References
  1. 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. [PubMed:17520363]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Choline:sodium symporter activity
Specific Function
Imports choline from the extracellular space to the neuron with high affinity. Choline uptake is the rate-limiting step in acetylcholine synthesis. Sodium ion- and chloride ion-dependent.
Gene Name
SLC5A7
Uniprot ID
Q9GZV3
Uniprot Name
High affinity choline transporter 1
Molecular Weight
63202.985 Da
References
  1. 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. [PubMed:15953352]
  2. 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. [PubMed:16051538]
  3. 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. [PubMed:16278103]
  4. 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. [PubMed:16539662]
  5. 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. [PubMed:16675138]

Drug created on June 13, 2005 07:24 / Updated on December 04, 2017 13:13