Choline salicylate 21.61% / Glycerol 12.62% ear drops
Choline salicylate is an anti-inflammatory pain reliever agent that is related to aspirin.
Active ingredients:
Choline salicylate + Glycerol
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MHRA alerts for Choline salicylate + Glycerol
Source: MHRA Products DatabaseOGL 3.0
Updated 3 months ago(18 Jan 2026)Safety monitoring data
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1 branded products available
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Part of the Earex brand family (generic: Choline salicylate + Glycerol)
1 products
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Similarity based on WHO Anatomical Therapeutic Chemical (ATC) classification and NHS BNF section grouping. Source data: NHS dm+d via TRUD (OGL v3.0), WHO ATC/DDD Index.
NHS prescribing volume and spending trends
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Clinical guidelines and formulary information
British National Formulary
Choline salicylate + Glycerol
BNF
Drug monograph — bnf.nice.org.ukSource: British National Formulary, NICE. Joint Formulary Committee. Contains public sector information licensed under the Open Government Licence v3.0.
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Codes for healthcare professionals and prescribing systems
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NHS UK identifiers
SNOMED CT and dm+d codes from NHS TRUD (Technology Reference data Update Distribution), licensed under the Open Government Licence v3.0. BNF codes from NHS Business Services Authority (NHSBSA).
Active and completed clinical studies from ClinicalTrials.gov
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Source: ClinicalTrials.gov, a database of the U.S. National Library of Medicine (NLM), National Institutes of Health (NIH). Data accessed via ClinicalTrials.gov API v2. Trial information is provided for research purposes and does not constitute medical advice.
Pharmacology and chemical data from DrugBank
Key facts
Drug status
Approved
Major interactions
13 found
Half-life
2-4 hours
Mechanism
Choline salicylate relieves pain by inhibition of prostaglandin synthesis and re…
Food interactions
None known
Human targets
7 targets
Data: DrugBank · CC BY-NC 4.0
Pharmacokinetics at a glance
Absorption
1-2 hr
Onset: 1-2 hr after ingestion [L2133]
In the oral form, choline salicylate is absorbed across the buccal mucosa.…
In the oral form, choline salicylate is absorbed across the buccal mucosa.…
Half-life
2-4 hours
The plasma half-life of salicylic acid is 2-4 hours.
[L2139]
[L2139]
Protein binding
80-90%
Salicylic acid is highly (80-90%) protein-bound.
[L2139]
[L2139]
Volume of distribution
0.15 L/kg
0.15 L/kg (salicylate), and widely distributed throughout extracellular water and most tissues [L2139]
Metabolism
The metabolism of salicylic acid is by glycine and phenolic or acyl glucuronate conjugation with small amounts of the drug undergoing hydroxylation.
[L2139]…
[L2139]…
Elimination
Both metabolites of choline salicylate, and a small amount of intact salicylic acid are excreted, primarily in the urine.
[L2139]
[L2139]
Pharmacokinetic data: DrugBank · CC BY-NC 4.0
Status:
Approved
Investigational
Nutraceutical
Small molecule
About this compound
Choline salicylate is an anti-inflammatory pain reliever agent that is related to aspirin. It is used to decrease swelling and to treat mild-moderate pain. It is used to treat arthritis in both children and adults. This medicine can also be used for fever [L2129].
Choline Salicylate is the choline salt of salicylic acid, used as an analgesic, antipyretic and antirheumatic. It relieves mild to moderate pain and reduce fever and inflammation or swelling. Choline salicylate is effective in the treatment of gout, rheumatic fever, rheumatoid arthritis and muscle injuries [A245119].
This drug is also a main ingredient in teething gels to relieve pains associated with tooth growth in the infant population [L2134]. The UK government has regulated its use, due to toxicity in those under 16 years of age. Topical oral salicylate gels are no longer indicated for people younger than 16 years for pain associated with infant teething, orthodontic devices, cold sores, or mouth ulcers [L2134].
Choline Salicylate is the choline salt of salicylic acid, used as an analgesic, antipyretic and antirheumatic. It relieves mild to moderate pain and reduce fever and inflammation or swelling. Choline salicylate is effective in the treatment of gout, rheumatic fever, rheumatoid arthritis and muscle injuries [A245119].
This drug is also a main ingredient in teething gels to relieve pains associated with tooth growth in the infant population [L2134]. The UK government has regulated its use, due to toxicity in those under 16 years of age. Topical oral salicylate gels are no longer indicated for people younger than 16 years for pain associated with infant teething, orthodontic devices, cold sores, or mouth ulcers [L2134].
Properties:
solid
Avg. mass: 241.29 Da
DrugBank indication
The oral gel is indicated for the relief of pain and discomfort of common mouth ulcers, cold sores, denture sore spots, infant teething and mouth ulcers, and sore spots due to orthodontic devices in children .
[L2135]
[L2135]
Also known as(107)
Choline salicylate
2.7.7.15
CCT B
CCT-beta
CCTB
CT B
CTP:phosphocholine cytidylyltransferase B
Phosphorylcholine transferase B
Dosage forms(15)
Gel (Cutaneous)
Liquid (Topical)
Gel (Oral) — 8.71 %
Gel (Oral) — 87.1 mg/g
Gel (Submucosal) — 0.01 % w/w
Gel (Oral) — 20 g
Solution (Oral)
Liquid (Oral)
Molecular properties(19)
Drug interactions(1066)
Known interactions with other medications. Always consult a healthcare professional.
Ammonium chloride
Unknown severity
The serum concentration of Choline salicylate can be increased when it is combined with Ammonium chloride.
Ginkgo biloba
Unknown severity
The risk or severity of bleeding can be increased when Ginkgo biloba is combined with Choline salicylate.
Methotrexate
Unknown severity
The serum concentration of Methotrexate can be increased when it is combined with Choline salicylate.
Pralatrexate
Unknown severity
The serum concentration of Pralatrexate can be increased when it is combined with Choline salicylate.
Probenecid
Moderate
The therapeutic efficacy of Probenecid can be decreased when used in combination with Choline salicylate.
Treprostinil
Unknown severity
The risk or severity of bleeding can be increased when Treprostinil is combined with Choline salicylate.
The excretion of Choline salicylate can be decreased when combined with Bupropion.
Ketoprofen
Unknown severity
The risk or severity of bleeding and gastrointestinal bleeding can be increased when Choline salicylate is combined with Ketoprofen.
Dexketoprofen
Unknown severity
The risk or severity of bleeding and gastrointestinal bleeding can be increased when Choline salicylate is combined with Dexketoprofen.
Dicoumarol
Moderate
Choline salicylate may increase the anticoagulant activities of Dicoumarol.
Phenindione
Moderate
Choline salicylate may increase the anticoagulant activities of Phenindione.
Phenprocoumon
Moderate
Choline salicylate may increase the anticoagulant activities of Phenprocoumon.
Acenocoumarol
Moderate
Choline salicylate may increase the anticoagulant activities of Acenocoumarol.
4-hydroxycoumarin
Moderate
Choline salicylate may increase the anticoagulant activities of 4-hydroxycoumarin.
Choline salicylate may increase the anticoagulant activities of Coumarin.
(R)-warfarin
Moderate
Choline salicylate may increase the anticoagulant activities of (R)-warfarin.
Ethyl biscoumacetate
Moderate
Choline salicylate may increase the anticoagulant activities of Ethyl biscoumacetate.
Fluindione
Moderate
Choline salicylate may increase the anticoagulant activities of Fluindione.
Clorindione
Moderate
Choline salicylate may increase the anticoagulant activities of Clorindione.
Diphenadione
Moderate
Choline salicylate may increase the anticoagulant activities of Diphenadione.
Tioclomarol
Moderate
Choline salicylate may increase the anticoagulant activities of Tioclomarol.
(S)-Warfarin
Moderate
Choline salicylate may increase the anticoagulant activities of (S)-Warfarin.
Acetyldigitoxin
Unknown severity
The serum concentration of Acetyldigitoxin can be decreased when it is combined with Choline salicylate.
Deslanoside
Unknown severity
The serum concentration of Deslanoside can be decreased when it is combined with Choline salicylate.
The serum concentration of Ouabain can be decreased when it is combined with Choline salicylate.
The serum concentration of Digitoxin can be decreased when it is combined with Choline salicylate.
The serum concentration of Oleandrin can be decreased when it is combined with Choline salicylate.
The serum concentration of Cymarin can be decreased when it is combined with Choline salicylate.
Proscillaridin
Unknown severity
The serum concentration of Proscillaridin can be decreased when it is combined with Choline salicylate.
Metildigoxin
Unknown severity
The serum concentration of Metildigoxin can be decreased when it is combined with Choline salicylate.
Lanatoside C
Unknown severity
The serum concentration of Lanatoside C can be decreased when it is combined with Choline salicylate.
Gitoformate
Unknown severity
The serum concentration of Gitoformate can be decreased when it is combined with Choline salicylate.
Acetyldigoxin
Unknown severity
The serum concentration of Acetyldigoxin can be decreased when it is combined with Choline salicylate.
Peruvoside
Unknown severity
The serum concentration of Peruvoside can be decreased when it is combined with Choline salicylate.
Tioguanine
Moderate
The metabolism of Tioguanine can be decreased when combined with Choline salicylate.
Mercaptopurine
Moderate
The metabolism of Mercaptopurine can be decreased when combined with Choline salicylate.
Azathioprine
Moderate
The metabolism of Azathioprine can be decreased when combined with Choline salicylate.
The risk or severity of bleeding can be increased when Choline salicylate is combined with Lepirudin.
Bivalirudin
Unknown severity
The risk or severity of bleeding can be increased when Choline salicylate is combined with Bivalirudin.
The risk or severity of bleeding can be increased when Choline salicylate is combined with Alteplase.
The risk or severity of bleeding can be increased when Choline salicylate is combined with Urokinase.
The risk or severity of bleeding can be increased when Choline salicylate is combined with Reteplase.
Anistreplase
Unknown severity
The risk or severity of bleeding can be increased when Choline salicylate is combined with Anistreplase.
Tenecteplase
Unknown severity
The risk or severity of bleeding can be increased when Choline salicylate is combined with Tenecteplase.
The risk or severity of bleeding can be increased when Choline salicylate is combined with Abciximab.
Drotrecogin alfa
Unknown severity
The risk or severity of bleeding can be increased when Choline salicylate is combined with Drotrecogin alfa.
Streptokinase
Unknown severity
The risk or severity of bleeding can be increased when Choline salicylate is combined with Streptokinase.
Argatroban
Unknown severity
The risk or severity of bleeding can be increased when Choline salicylate is combined with Argatroban.
The risk or severity of bleeding can be increased when Choline salicylate is combined with Ardeparin.
Fondaparinux
Unknown severity
The risk or severity of bleeding can be increased when Choline salicylate is combined with Fondaparinux.
Showing 50 of 1066 interactions
Toxicity & overdose
LD50, oral in mouse: 2690mg/kg .
[L2125]
Ld50, subcutaneous in mouse: 1gm/kg .
[L2125]
Interferes with thyroid function test .
[L2132]
Gastrointestinal (GI) disorders, fatigue, hypersensitivity reactions, skin eruptions, hemolytic anemia, weakness, dyspnoea; local irritation (rectally); Reye's syndrome.
Potentially Fatal: Paroxysmal bronchospasm; hepatotoxicity; renal impairment/failure; thrombocytopenia, iron-deficiency anemia, occult bleeding, leukopenia; mild chronic salicylate intoxication .
[L2132]
Salicylate poisoning is normally associated with plasma concentrations >350 mg/L (2.5 mmol/L). Most adult deaths due to salicylate poisoning occur in patients whose serum concentrations of salicylate are over 700 mg/L (5.1 mmol/L). Single doses of less than 100 mg/kg are very unlikely to lead to serious poisoning.
Patients should be provided with supportive therapy or treatment for salicylate poisoning as necessary. This may include treatment like activated charcoal, urinary alkalinization and, in severe cases, hemodialysis .
[L2139]
[L2125]
Ld50, subcutaneous in mouse: 1gm/kg .
[L2125]
Interferes with thyroid function test .
[L2132]
Gastrointestinal (GI) disorders, fatigue, hypersensitivity reactions, skin eruptions, hemolytic anemia, weakness, dyspnoea; local irritation (rectally); Reye's syndrome.
Potentially Fatal: Paroxysmal bronchospasm; hepatotoxicity; renal impairment/failure; thrombocytopenia, iron-deficiency anemia, occult bleeding, leukopenia; mild chronic salicylate intoxication .
[L2132]
Salicylate poisoning is normally associated with plasma concentrations >350 mg/L (2.5 mmol/L). Most adult deaths due to salicylate poisoning occur in patients whose serum concentrations of salicylate are over 700 mg/L (5.1 mmol/L). Single doses of less than 100 mg/kg are very unlikely to lead to serious poisoning.
Patients should be provided with supportive therapy or treatment for salicylate poisoning as necessary. This may include treatment like activated charcoal, urinary alkalinization and, in severe cases, hemodialysis .
[L2139]
How it works
Mechanism of action
Choline salicylate relieves pain by inhibition of prostaglandin synthesis and reduces fever by acting on the hypothalamus heat-regulating center. It also inhibits the generation of impulses through the inhibition of cyclooxygenase enzyme (COX) [L2132], [A245119].
Cyclooxygenase is involved in the production of prostaglandins, in response to injury and after various other stimuli. The prostaglandins promote pain, swelling, and inflammation. The choline salicylate decreases inflammation and pain by reducing the production of these prostaglandins in the area of the mouth it is applied to [L2137].
Cyclooxygenase is involved in the production of prostaglandins, in response to injury and after various other stimuli. The prostaglandins promote pain, swelling, and inflammation. The choline salicylate decreases inflammation and pain by reducing the production of these prostaglandins in the area of the mouth it is applied to [L2137].
Pharmacodynamics
This is an anti-inflammatory and antipyretic medication [L2132], [L2133].
If is often used in oral gel form for the relief of pain, discomfort, and inflammation caused by common mouth ulcers, cold sores, denture and sore spots, as well as mouth ulcers, and sore spots because of orthodontic devices [L2139].
If is often used in oral gel form for the relief of pain, discomfort, and inflammation caused by common mouth ulcers, cold sores, denture and sore spots, as well as mouth ulcers, and sore spots because of orthodontic devices [L2139].
Pharmacokinetics
How the body processes this drug — absorption, distribution, metabolism, and elimination
Absorption
Onset: 1-2 hr after ingestion [L2133]
In the oral form, choline salicylate is absorbed across the buccal mucosa. There is a need for caution not to exceed the stated dose and monitor for any signs of suggested salicylism, especially when this drug is used for infants .
[L2135]
In one study, it was found that this drug was more rapidly absorbed than ASA (absorption t1/2 = 0.1 vs 0.36 h) .
[L2138]
In the oral form, choline salicylate is absorbed across the buccal mucosa. There is a need for caution not to exceed the stated dose and monitor for any signs of suggested salicylism, especially when this drug is used for infants .
[L2135]
In one study, it was found that this drug was more rapidly absorbed than ASA (absorption t1/2 = 0.1 vs 0.36 h) .
[L2138]
Half-life
The plasma half-life of salicylic acid is 2-4 hours.
[L2139]
[L2139]
Protein binding
Salicylic acid is highly (80-90%) protein-bound.
[L2139]
[L2139]
Volume of distribution
0.15 L/kg (salicylate), and widely distributed throughout extracellular water and most tissues [L2139]
Metabolism
The metabolism of salicylic acid is by glycine and phenolic or acyl glucuronate conjugation with small amounts of the drug undergoing hydroxylation.
[L2139]
[L2139]
Route of elimination
Both metabolites of choline salicylate, and a small amount of intact salicylic acid are excreted, primarily in the urine.
[L2139]
[L2139]
Drug targets(7)
Proteins and enzymes this drug interacts with in the body
Choline-phosphate cytidylyltransferase B
PCYT1B
product of
Specific functioncholine-phosphate cytidylyltransferase activity
Cellular location
Cytoplasm
General function & pharmacology
Catalyzes the key rate-limiting step in the CDP-choline pathway for phosphatidylcholine biosynthesis
Acetylcholinesterase
ACHE
product of
Specific functionacetylcholine binding
Cellular location
Synapse
General function & pharmacology
Hydrolyzes rapidly the acetylcholine neurotransmitter released into the synaptic cleft allowing to terminate the signal transduction at the neuromuscular junction. Role in neuronal apoptosis
Choline-phosphate cytidylyltransferase A
PCYT1A
product of
Specific functioncalmodulin binding
Cellular location
Cytoplasm, cytosol
General function & pharmacology
Catalyzes the key rate-limiting step in the CDP-choline pathway for phosphatidylcholine biosynthesis
Phospholipase D2
PLD2
product of
Specific functionphosphatidylinositol binding
Cellular location
Cell membrane
General function & pharmacology
Function as phospholipase selective for phosphatidylcholine .
PMID:9582313
May have a role in signal-induced cytoskeletal regulation and/or endocytosis (By similarity)
PMID:9582313
May have a role in signal-induced cytoskeletal regulation and/or endocytosis (By similarity)
Cholinesterase
BCHE
product of
Specific functionacetylcholinesterase activity
Cellular location
Secreted
General function & pharmacology
Esterase with broad substrate specificity. Contributes to the inactivation of the neurotransmitter acetylcholine. Can degrade neurotoxic organophosphate esters
Metabolizing enzymes(5)
Enzymes involved in drug metabolism — important for understanding drug interactions
Enzyme activity key
substrate
inhibitor
inducer
CEPT1Choline/ethanolaminephosphotransferase 1
substrate
CHKBCholine/ethanolamine kinase
substrate
CHATCholine O-acetyltransferase
substrate
CHKACholine kinase alpha
substrate
CHDHCholine dehydrogenase, mitochondrial
substrate
Transporters(9)
Proteins that transport this drug across cell membranes
Solute carrier family 22 member 2
SLC22A2
substrate
inhibitor
Specific functionacetylcholine transmembrane transporter activity
Cellular location
Basolateral cell membrane
General function & pharmacology
Electrogenic voltage-dependent transporter that mediates the transport of a variety of organic cations such as endogenous bioactive amines, cationic drugs and xenobiotics .
PMID:9260930 PMID:9687576
Functions as a Na(+)-independent, bidirectional uniporter .
PMID:21128598 PMID:9687576
Cation cellular uptake or release is driven by the electrochemical potential, i.e. membrane potential and concentration gradient .
PMID:15212162 PMID:9260930 PMID: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 .
PMID: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 .
PMID:16581093 PMID:17460754 PMID: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 .
PMID: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 .
PMID:15817714
Also transports guanidine and endogenous monoamines such as vitamin B1/thiamine, creatinine and N-1-methylnicotinamide (NMN) .
PMID:12089365 PMID:15212162 PMID:17072098 PMID:24961373 PMID:9260930
Mediates the uptake and efflux of quaternary ammonium compound choline .
PMID:9260930
Mediates the bidirectional transport of polyamine agmatine and the uptake of polyamines putrescine and spermidine .
PMID:12538837 PMID:21128598
Able to transport non-amine endogenous compounds such as prostaglandin E2 (PGE2) and prostaglandin F2-alpha (PGF2-alpha) .
PMID:11907186
Also involved in the uptake of xenobiotic 4-(4-(dimethylamino)styryl)-N-methylpyridinium (ASP) .
PMID:12395288 PMID:16394027
May contribute to regulate the transport of organic compounds in testis across the blood-testis-barrier (Probable)
PMID:9260930 PMID:9687576
Functions as a Na(+)-independent, bidirectional uniporter .
PMID:21128598 PMID:9687576
Cation cellular uptake or release is driven by the electrochemical potential, i.e. membrane potential and concentration gradient .
PMID:15212162 PMID:9260930 PMID: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 .
PMID: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 .
PMID:16581093 PMID:17460754 PMID: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 .
PMID: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 .
PMID:15817714
Also transports guanidine and endogenous monoamines such as vitamin B1/thiamine, creatinine and N-1-methylnicotinamide (NMN) .
PMID:12089365 PMID:15212162 PMID:17072098 PMID:24961373 PMID:9260930
Mediates the uptake and efflux of quaternary ammonium compound choline .
PMID:9260930
Mediates the bidirectional transport of polyamine agmatine and the uptake of polyamines putrescine and spermidine .
PMID:12538837 PMID:21128598
Able to transport non-amine endogenous compounds such as prostaglandin E2 (PGE2) and prostaglandin F2-alpha (PGF2-alpha) .
PMID:11907186
Also involved in the uptake of xenobiotic 4-(4-(dimethylamino)styryl)-N-methylpyridinium (ASP) .
PMID:12395288 PMID:16394027
May contribute to regulate the transport of organic compounds in testis across the blood-testis-barrier (Probable)
Solute carrier family 22 member 1
SLC22A1
substrate
inhibitor
Specific function(R)-carnitine transmembrane transporter activity
Cellular location
Basolateral cell membrane
General function & pharmacology
Electrogenic voltage-dependent transporter that mediates the transport of a variety of organic cations such as endogenous bioactive amines, cationic drugs and xenobiotics .
PMID:11388889 PMID:11408531 PMID:12439218 PMID:12719534 PMID:15389554 PMID:16263091 PMID:16272756 PMID:16581093 PMID:19536068 PMID:21128598 PMID:23680637 PMID:24961373 PMID:34040533 PMID:9187257 PMID:9260930 PMID: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 .
PMID:16263091
Transports endogenous monoamines such as N-1-methylnicotinamide (NMN), guanidine, histamine, neurotransmitters dopamine, serotonin and adrenaline .
PMID:12439218 PMID:24961373 PMID:35469921 PMID:9260930
Also transports natural polyamines such as spermidine, agmatine and putrescine at low affinity, but relatively high turnover .
PMID:21128598
Involved in the hepatic uptake of vitamin B1/thiamine, hence regulating hepatic lipid and energy metabolism .
PMID: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 .
PMID:15817714
Transports dopaminergic neuromodulators cyclo(his-pro) and salsolinol with lower efficency .
PMID:17460754
Also capable of transporting non-amine endogenous compounds such as prostaglandin E2 (PGE2) and prostaglandin F2-alpha (PGF2-alpha) .
PMID: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) PMID:11408531 PMID:15389554 PMID:35469921 PMID:9260930
PMID:11388889 PMID:11408531 PMID:12439218 PMID:12719534 PMID:15389554 PMID:16263091 PMID:16272756 PMID:16581093 PMID:19536068 PMID:21128598 PMID:23680637 PMID:24961373 PMID:34040533 PMID:9187257 PMID:9260930 PMID: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 .
PMID:16263091
Transports endogenous monoamines such as N-1-methylnicotinamide (NMN), guanidine, histamine, neurotransmitters dopamine, serotonin and adrenaline .
PMID:12439218 PMID:24961373 PMID:35469921 PMID:9260930
Also transports natural polyamines such as spermidine, agmatine and putrescine at low affinity, but relatively high turnover .
PMID:21128598
Involved in the hepatic uptake of vitamin B1/thiamine, hence regulating hepatic lipid and energy metabolism .
PMID: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 .
PMID:15817714
Transports dopaminergic neuromodulators cyclo(his-pro) and salsolinol with lower efficency .
PMID:17460754
Also capable of transporting non-amine endogenous compounds such as prostaglandin E2 (PGE2) and prostaglandin F2-alpha (PGF2-alpha) .
PMID: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) PMID:11408531 PMID:15389554 PMID:35469921 PMID:9260930
Solute carrier family 22 member 3
SLC22A3
inhibitor
Specific functionmonoamine transmembrane transporter activity
Cellular location
Cell membrane
General function & pharmacology
Electrogenic voltage-dependent transporter that mediates the transport of a variety of organic cations such as endogenous bioactive amines, cationic drugs and xenobiotics .
PMID:10196521 PMID:10966924 PMID:12538837 PMID:17460754 PMID:20858707
Cation cellular uptake or release is driven by the electrochemical potential, i.e. membrane potential and concentration gradient .
PMID:10966924
Functions as a Na(+)- and Cl(-)-independent, bidirectional uniporter .
PMID: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 .
PMID:10196521 PMID:16581093 PMID:20858707
Transports dopaminergic neuromodulators cyclo(his-pro) and salsolinol with low efficiency .
PMID:17460754
May be involved in the uptake and disposition of cationic compounds by renal clearance from the blood flow .
PMID: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 .
PMID:12538837
Also transports guanidine .
PMID:10966924
May also mediate intracellular transport of organic cations, thereby playing a role in amine metabolism and intracellular signaling (By similarity)
PMID:10196521 PMID:10966924 PMID:12538837 PMID:17460754 PMID:20858707
Cation cellular uptake or release is driven by the electrochemical potential, i.e. membrane potential and concentration gradient .
PMID:10966924
Functions as a Na(+)- and Cl(-)-independent, bidirectional uniporter .
PMID: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 .
PMID:10196521 PMID:16581093 PMID:20858707
Transports dopaminergic neuromodulators cyclo(his-pro) and salsolinol with low efficiency .
PMID:17460754
May be involved in the uptake and disposition of cationic compounds by renal clearance from the blood flow .
PMID: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 .
PMID:12538837
Also transports guanidine .
PMID:10966924
May also mediate intracellular transport of organic cations, thereby playing a role in amine metabolism and intracellular signaling (By similarity)
Organic cation/carnitine transporter 2
SLC22A5
inhibitor
Specific function(R)-carnitine transmembrane transporter activity
Cellular location
Cell membrane
General function & pharmacology
Sodium-ion dependent, high affinity carnitine transporter. Involved in the active cellular uptake of carnitine. Transports one sodium ion with one molecule of carnitine .
PMID:10454528 PMID:10525100 PMID:10966938 PMID:17509700 PMID:20722056 PMID: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 .
PMID:10454528 PMID:10525100 PMID:10966938
In intestinal epithelia, transports the quorum-sensing pentapeptide CSF (competence and sporulation factor) from B.subtilis which induces cytoprotective heat shock proteins contributing to intestinal homeostasis .
PMID:18005709
May also contribute to regulate the transport of organic compounds in testis across the blood-testis-barrier (Probable)
PMID:10454528 PMID:10525100 PMID:10966938 PMID:17509700 PMID:20722056 PMID: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 .
PMID:10454528 PMID:10525100 PMID:10966938
In intestinal epithelia, transports the quorum-sensing pentapeptide CSF (competence and sporulation factor) from B.subtilis which induces cytoprotective heat shock proteins contributing to intestinal homeostasis .
PMID:18005709
May also contribute to regulate the transport of organic compounds in testis across the blood-testis-barrier (Probable)
Solute carrier family 22 member 4
SLC22A4
inhibitor
Specific functionacetylcholine transmembrane transporter activity
Cellular location
Apical cell membrane
General function & pharmacology
Transporter that mediates the transport of endogenous and microbial zwitterions and organic cations .
PMID:10215651 PMID:15107849 PMID:15795384 PMID:16729965 PMID:20601551 PMID:22206629 PMID:22569296 PMID:29530864
Functions as a Na(+)-dependent and pH-dependent high affinity microbial symporter of potent food-derived antioxidant ergothioeine .
PMID:15795384 PMID:29530864 PMID: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 .
PMID:20601551
Also mediates the bidirectional transport of acetycholine, although the exact transport mechanism has not been fully identified yet .
PMID:22206629
Most likely exports anti-inflammatory acetylcholine in non-neuronal tissues, thereby contributing to the non-neuronal cholinergic system .
PMID:22206629 PMID: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 .
PMID:15795384 PMID:22206629
May also function as a low-affinity Na(+)-dependent transporter of L-carnitine through the mitochondrial membrane, thereby maintaining intracellular carnitine homeostasis .
PMID:10215651 PMID:15107849 PMID:16729965
May contribute to regulate the transport of cationic compounds in testis across the blood-testis-barrier PMID:35307651
PMID:10215651 PMID:15107849 PMID:15795384 PMID:16729965 PMID:20601551 PMID:22206629 PMID:22569296 PMID:29530864
Functions as a Na(+)-dependent and pH-dependent high affinity microbial symporter of potent food-derived antioxidant ergothioeine .
PMID:15795384 PMID:29530864 PMID: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 .
PMID:20601551
Also mediates the bidirectional transport of acetycholine, although the exact transport mechanism has not been fully identified yet .
PMID:22206629
Most likely exports anti-inflammatory acetylcholine in non-neuronal tissues, thereby contributing to the non-neuronal cholinergic system .
PMID:22206629 PMID: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 .
PMID:15795384 PMID:22206629
May also function as a low-affinity Na(+)-dependent transporter of L-carnitine through the mitochondrial membrane, thereby maintaining intracellular carnitine homeostasis .
PMID:10215651 PMID:15107849 PMID:16729965
May contribute to regulate the transport of cationic compounds in testis across the blood-testis-barrier PMID:35307651
Choline transporter-like protein 1
SLC44A1
substrate
Specific functionantiporter activity
Cellular location
Cell membrane
General function & pharmacology
Choline/H+ antiporter .
PMID:19357133 PMID:23651124 PMID:31855247 PMID: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 .
PMID:33789160
Involved in membrane synthesis and myelin production PMID:31855247
PMID:19357133 PMID:23651124 PMID:31855247 PMID: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 .
PMID:33789160
Involved in membrane synthesis and myelin production PMID:31855247
Choline transporter-like protein 4
SLC44A4
substrate
Specific functionantiporter activity
Cellular location
Membrane
General function & pharmacology
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) .
PMID:23651124 PMID: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 PMID:24379411 PMID:26741288
PMID:23651124 PMID: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 PMID:24379411 PMID:26741288
Choline transporter-like protein 3
SLC44A3
substrate
Specific functioncholine transmembrane transporter activity
Cellular location
Membrane
High affinity choline transporter 1
SLC5A7
substrate
Specific functioncholine binding
Cellular location
Presynaptic cell membrane
General function & pharmacology
High-affinity Na(+)-coupled choline transmembrane symporter .
PMID:11027560 PMID:11068039 PMID:12237312 PMID:12969261 PMID:17005849 PMID:23132865 PMID:23141292 PMID:27569547
Functions as an electrogenic, voltage-dependent transporter with variable charge/choline stoichiometry .
PMID:17005849
Choline uptake and choline-induced current is also Cl(-)-dependent where Cl(-) is likely a regulatory ion rather than cotransported ion .
PMID:11068039 PMID:12237312 PMID: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 .
PMID: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 .
PMID:11027560
Localized predominantly in presynaptic terminal intracellular organelles, and translocated to the plasma membrane in active form in response to neuronal activity PMID:12969261 PMID:15953352
PMID:11027560 PMID:11068039 PMID:12237312 PMID:12969261 PMID:17005849 PMID:23132865 PMID:23141292 PMID:27569547
Functions as an electrogenic, voltage-dependent transporter with variable charge/choline stoichiometry .
PMID:17005849
Choline uptake and choline-induced current is also Cl(-)-dependent where Cl(-) is likely a regulatory ion rather than cotransported ion .
PMID:11068039 PMID:12237312 PMID: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 .
PMID: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 .
PMID:11027560
Localized predominantly in presynaptic terminal intracellular organelles, and translocated to the plasma membrane in active form in response to neuronal activity PMID:12969261 PMID:15953352
Scientific references(4)
Bochner F., Graham G.G., Cham B.E., Imhoff D.M., Haavisto T.M.
Salicylate metabolite kinetics after several salicylates.
Clinical Pharmacology and Therapeutics
198130(2):266-275. doi: 10.1038/clpt.1981.158
Needs C.J., Brooks P.M.
Clinical pharmacokinetics of the salicylates.
Clinical Pharmacokinetics
1985 Mar-Apr10(2):164-77. doi: 10.2165/00003088-198510020-00004
Kuehl G.E., Bigler J., Potter J.D., Lampe J.W.
Glucuronidation of the aspirin metabolite salicylic acid by expressed UDP-glucuronosyltransferases and human liver microsomes.
Drug Metabolism and Disposition
2006 Feb34(2):199-202. doi: 10.1124/dmd.105.005652. Epub 2005 Oct 28
Wroblewska K.B., Plewa S., Derezinski P., Muszalska-Kolos I.
Choline Salicylate Analysis: Chemical Stability and Degradation Product Identification.
Molecules
2019 Dec 2225(1). pii: molecules25010051. doi: 10.3390/molecules25010051
ATC classification(1 code)
ATC N02BA03
Affected organisms(1)
Humans and other mammals
Experimental properties(1)
Commercial products(21)
Chemical identifiers
CAS, UNII, InChI Key and database cross-references
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Chemical identifiers
CAS, UNII, InChI Key and database cross-references
DrugBank citations
If you use DrugBank data in your research, please cite the following publications:
Knox C., Wilson M., Klinger C.M., et al
DrugBank 6.
0: the DrugBank Knowledgebase for 2024
Nucleic Acids Res. 2024 Jan 552(D1):D1265-D1275
Wishart D.S., Feunang Y.D., Guo A.C., et al
DrugBank 5.
0: a major update to the DrugBank database for 2018
Nucleic Acids Res. 2017 Nov 846(D1):D1074-D1082
Show earlier publications
Law V., Knox C., Djoumbou Y., et al
DrugBank 4.
0: shedding new light on drug metabolism
Nucleic Acids Res. 2014 Jan 142(1):D1091-7
Knox C., Law V., Jewison T., et al
DrugBank 3.
0: a comprehensive resource for 'omics' research on drugs
Nucleic Acids Res. 2011 Jan39(Database issue):D1035-41
Wishart D.S., Knox C., Guo A.C., et al
DrugBank: a knowledgebase for drugs, drug actions and drug targets.
Nucleic Acids Research
2008 Jan36(Database issue):D901-6
Wishart D.S., Knox C., Guo A.C., et al
DrugBank: a comprehensive resource for in silico drug discovery and exploration.
Nucleic Acids Research
2006 Jan 134(Database issue):D668-72
Source: go.drugbank.comCC BY-NC 4.0
Updated 26 days ago(8 Mar 2026)