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Identification
NameCholine
Accession NumberDB00122  (NUTR00020)
Typesmall molecule
Groupsapproved, 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
SynonymLanguageCode
BilineurineNot AvailableNot Available
Choline ionNot AvailableNot Available
N-trimethylethanolamineNot AvailableNot Available
N,N,N-trimethylethanol-ammoniumNot AvailableNot Available
trimethylethanolamineNot AvailableNot Available
SaltsNot Available
Brand namesNot Available
Brand mixturesNot Available
Categories
CAS number62-49-7
WeightAverage: 104.1708
Monoisotopic: 104.107539075
Chemical FormulaC5H14NO
InChI KeyOEYIOHPDSNJKLS-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
Mass SpecNot Available
Taxonomy
KingdomOrganic Compounds
SuperclassOrganonitrogen Compounds
ClassQuaternary Ammonium Salts
SubclassCholines
Direct parentCholines
Alternative parentsPrimary Alcohols; Polyamines
Substituentspolyamine; primary alcohol; amine; alcohol
Classification descriptionThis compound belongs to the cholines. These are organic compounds containing a N,N,N-trimethylethanolammonium cation.
Pharmacology
IndicationFor nutritional supplementation, also for treating dietary shortage or imbalance
PharmacodynamicsThis 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 actionCholine 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.
AbsorptionNot Available
Volume of distributionNot Available
Protein bindingNot Available
Metabolism
Route of eliminationNot Available
Half lifeNot Available
ClearanceNot Available
ToxicityOral rat LD50: 3400 mg/kg
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
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 substrate Non-inhibitor 0.9496
CYP450 2D6 substrate Non-inhibitor 0.9231
CYP450 2C19 substrate Non-inhibitor 0.9497
CYP450 3A4 substrate 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
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
TabletOral
Prices
Unit descriptionCostUnit
Trilipix dr 135 mg capsule4.38USDcapsule
Trilipix dr 45 mg capsule1.46USDcapsule
Choline-10 tablet0.06USDtablet
Choline bitartrate crystals0.03USDg
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
Stateliquid
Experimental Properties
PropertyValueSource
melting point244-247 °C (as chloride salt)Not Available
boiling point113 °CNot Available
water solubilitySolubleNot Available
Predicted Properties
PropertyValueSource
water solubility3.61e+00 g/lALOGPS
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 area20.23ChemAxon
rotatable bond count2ChemAxon
refractivity42.19ChemAxon
polarizability12.57ChemAxon
number of rings0ChemAxon
bioavailability1ChemAxon
rule of fiveYesChemAxon
Ghose filterNoChemAxon
Veber's ruleYesChemAxon
MDDR-like ruleNoChemAxon
Spectra
SpectraMS/MSLC-MS1D NMR2D NMR
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 ReferenceNot Available
External Links
ResourceLink
KEGG CompoundC00114
ChEBI15354
ChEMBLCHEMBL920
PharmGKBPA448976
HETCHT
PDRhealthhttp://www.pdrhealth.com/drug_info/nmdrugprofiles/nutsupdrugs/cho_0283.shtml
WikipediaCholine
ATC CodesN02BA03N07AX02R03DA02V03AB29S01EB09
AHFS Codes
  • 88:30.00*
  • 56:24.00
  • 88:08.00
PDB Entries
FDA labelNot Available
MSDSshow(73.6 KB)
Interactions
Drug InteractionsNot Available
Food InteractionsNot Available

Targets

1. Choline-phosphate cytidylyltransferase B

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: product of

Components

Name UniProt ID Details
Choline-phosphate cytidylyltransferase B Q9Y5K3 Details

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
  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
  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

2. Acetylcholinesterase

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: product of

Components

Name UniProt ID Details
Acetylcholinesterase P22303 Details

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
  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
  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
  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
  5. Anzai J: [Use of biosensors for detecting organophosphorus agents] Yakugaku Zasshi. 2006 Dec;126(12):1301-8. Pubmed

3. Choline-phosphate cytidylyltransferase A

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: product of

Components

Name UniProt ID Details
Choline-phosphate cytidylyltransferase A P49585 Details

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
  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

4. Phospholipase D2

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: product of

Components

Name UniProt ID Details
Phospholipase D2 O14939 Details

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
  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
  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 Jul 12;. Pubmed
  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
  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

5. Cholinesterase

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: product of

Components

Name UniProt ID Details
Cholinesterase P06276 Details

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 Jan 24;. Pubmed
  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
  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
  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
  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

6. Phospholipase D1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: product of

Components

Name UniProt ID Details
Phospholipase D1 Q13393 Details

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

7. Phosphoethanolamine/phosphocholine phosphatase

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: product of

Components

Name UniProt ID Details
Phosphoethanolamine/phosphocholine phosphatase Q8TCT1 Details

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
  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

Enzymes

1. Choline/ethanolaminephosphotransferase 1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Choline/ethanolaminephosphotransferase 1 Q9Y6K0 Details

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
  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
  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

2. Choline/ethanolamine kinase

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Choline/ethanolamine kinase Q9Y259 Details

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
  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

3. Choline O-acetyltransferase

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Choline O-acetyltransferase P28329 Details

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
  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
  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
  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
  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

4. Choline kinase alpha

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Choline kinase alpha P35790 Details

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
  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
  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
  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

5. Choline dehydrogenase, mitochondrial

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Choline dehydrogenase, mitochondrial Q8NE62 Details

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
  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
  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
  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. 2007 Mar 21;. Pubmed
  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

Transporters

1. Solute carrier family 22 member 2

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate inhibitor

Components

Name UniProt ID Details
Solute carrier family 22 member 2 O15244 Details

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
  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
  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
  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
  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
  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
  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
  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
  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. Pubmed

2. Solute carrier family 22 member 1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate inhibitor

Components

Name UniProt ID Details
Solute carrier family 22 member 1 O15245 Details

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
  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
  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
  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
  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
  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
  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
  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
  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
  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
  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
  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
  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
  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

3. Solute carrier family 22 member 3

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Solute carrier family 22 member 3 O75751 Details

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

4. Solute carrier family 22 member 5

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Solute carrier family 22 member 5 O76082 Details

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
  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
  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
  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

5. Solute carrier family 22 member 4

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Solute carrier family 22 member 4 Q9H015 Details

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

6. Choline transporter-like protein 1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Choline transporter-like protein 1 Q8WWI5 Details

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
  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
  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
  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. 2007 Jul 12;. Pubmed

7. Choline transporter-like protein 4

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Choline transporter-like protein 4 Q53GD3 Details

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

8. Choline transporter-like protein 2

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Choline transporter-like protein 2 Q8IWA5 Details

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
  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

9. Choline transporter-like protein 3

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Choline transporter-like protein 3 Q8N4M1 Details

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

10. High affinity choline transporter 1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
High affinity choline transporter 1 Q9GZV3 Details

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
  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
  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
  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
  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

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Drug created on June 13, 2005 07:24 / Updated on February 26, 2014 16:09