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Identification
NameClonidine
Accession NumberDB00575  (APRD00174, DB07566)
Typesmall molecule
Groupsapproved
Description

Clonidine, an imidazoline-derivative hypotensive agent is a centrally-acting α2-adrenergic agonist. It crosses the blood-brain barrier and acts in the hypothalamus to induce a decrease in blood pressure. It may also be administered as an epidural infusion as an adjunct treatment in the management of severe cancer pain that is not relieved by opiate analgesics alone. Clonidine may be used for differential diagnosis of pheochromocytoma in hypertensive patients. Other uses for clonidine include prophylaxis of vascular migraine headaches, treatment of severe dysmenorrhea, management of vasomotor symptoms associated with menopause, rapid detoxification in the management of opiate withdrawal, treatment of alcohol withdrawal used in conjunction with benzodiazepines, management of nicotine dependence, topical use to reduce intraocular pressure in the treatment of open-angle and secondary glaucoma and hemorrhagic glaucoma associated with hypertension, and in the treatment of attention-deficit hyperactivity disorder (ADHD). Clonidine also exhibits some peripheral activity.

Structure
Thumb
Synonyms
SynonymLanguageCode
ChlofazolineNot AvailableIS
ClonidinGermanINN
ClonidinaSpanishINN
ClonidinumLatinINN
Salts
Name/CAS Structure Properties
Clonidine Hydrochloride
4205-91-8
Thumb
  • InChI Key: ZNIFSRGNXRYGHF-UHFFFAOYSA-N
  • Monoisotopic Mass: 264.994030456
  • Average Mass: 266.555
DBSALT000538
Brand names
NameCompany
CatapresBoehringer Ingelheim
Catapres-TTSBoehringer Ingelheim
CatapresanBoehringer Ingelheim
CatapressanBoehringer Ingelheim
DixaritBoehringer Ingelheim
DuraclonBioniche
IsoglauconAgepha
KapvayShionogi
Run RuiBausch & Lomb
VelarilRoemmers
WinpressWinston
Brand mixtures
Brand NameIngredients
Arkamin-HClonidine and Hydrochlorothiazide
ClorpresClonidine and Chlortalidone
Combipres 0.1/15 TabChlorthalidone + Clonidine Hydrochloride
Categories
CAS number4205-90-7
WeightAverage: 230.094
Monoisotopic: 229.017352717
Chemical FormulaC9H9Cl2N3
InChI KeyInChIKey=GJSURZIOUXUGAL-UHFFFAOYSA-N
InChI
InChI=1S/C9H9Cl2N3/c10-6-2-1-3-7(11)8(6)14-9-12-4-5-13-9/h1-3H,4-5H2,(H2,12,13,14)
IUPAC Name
N-(2,6-dichlorophenyl)-4,5-dihydro-1H-imidazol-2-amine
SMILES
ClC1=CC=CC(Cl)=C1NC1=NCCN1
Mass SpecNot Available
Taxonomy
KingdomOrganic Compounds
SuperclassBenzenoids
ClassBenzene and Substituted Derivatives
SubclassHalobenzenes
Direct parentDichlorobenzenes
Alternative parentsAryl Chlorides; Guanidines; Polyamines; Organochlorides
Substituentsaryl chloride; aryl halide; guanidine; polyamine; organochloride; organohalogen; amine; organonitrogen compound
Classification descriptionThis compound belongs to the dichlorobenzenes. These are compounds containing a benzene with exactly two chlorine atoms attached to it.
Pharmacology
IndicationMay be used as an adjunct in the treatment of hypertension, as an epidural infusion as an adjunct treatment in the management of severe cancer pain that is not relieved by opiate analgesics alone, for differential diagnosis of pheochromocytoma in hypertensive patients, prophylaxis of vascular migraine headaches, treatment of severe dysmenorrhea, management of vasomotor symptoms associated with menopause, rapid detoxification in the management of opiate withdrawal, treatment of alcohol withdrawal used in conjunction with benzodiazepines, management of nicotine dependence, topical use to reduce intraocular pressure in the treatment of open-angle and secondary glaucoma and hemorrhagic glaucoma associated with hypertension, and in the treatment of attention-deficit hyperactivity disorder (ADHD).
PharmacodynamicsClonidine is an α-adrenergic agent that acts specifically on α2-receptors. α2-receptors regulate a number of signaling pathways mediated by multiple Gi proteins, Gαi1, Gαi2, and G&alphai3. Stimulation of α2-receptors mediates effects such as inhibition of adenylyl cyclase, stimulation fo phospholipase D, stimulation of mitogen-activated protein kinases, stimulation of K+ currents and inhibition of Ca2+ currents. Three G-protein coupled α2-receptor subtypes have been identified: α2A, α2B, and α2C. Each subtype has a unique pattern of tissue distribution in the central nervous system and peripheral tissues. The α2A-receptor is widely distributed throughout the central nervous system; it is found in the locus coeruleus, brain stem nuclei, cerebral cortex, septum, hypothalamus, and hippocampus. α2A-receptors are also expressed in the kidneys, spleen, thymus, lung and salivary glands. The α2C-receptor is primarily expressed in the central nervous system, including the striatum, olfactory tubercle, hippocampus and cerebral cortex. Low levels of the α2C-subtype are also found in the kidneys. The α2B-receptor is located primarily in the periphery (kidney, liver, lung and heart) with low levels of expression in the thalamic nuclei of the central nervous system. The α2A- and α2C-receptors are located presynaptically and inhibit the released of noradrenaline from sympathetic nerves. Stimulation of these receptors decreases sympathetic tone, resulting in decreases in blood pressure and heart rate. Sedation and analgesia is mediated by centrally located α2A-receptors, while peripheral α2B-receptors mediate constriction of vascular smooth muscle. α2A-Receptors also mediate essential components of the analgesic effect of nitrous oxide in the spinal cord. Clonidine stimulates all three α2-receptor subtypes with similar potency. Its actions in the nervous system decreases blood pressure in patients with hypertension and decreases sympathetic overactivity in patients undergoing opioid withdrawal. Clonidine is also a potent sedative and analgesic and can prevent post-operative shivering in intensive and post-operative care. Its use in differential diagnosis of pheochromocytoma owes to the fact that hypertension in patients with pheochromocytoma is refractory to antihypertensive treatment with clonidine.
Mechanism of actionSee Pharmacology section above.
AbsorptionWell absorbed following oral administration. Bioavailability following chronic administration is approximately 65%.
Volume of distributionNot Available
Protein binding20-40%, primarily to albumin
Metabolism

Hepatic. Metabolized via minor pathways. The major metabolite, <i>p</i>-hydroxyclonidine, is present in concentrations less than 10% of those of unchanged clonidine in urine. Four metabolites have been detected, but only <i>p</i>-hydroxyclonidine has been identified.

SubstrateEnzymesProduct
Clonidine
4-HydroxyclonidineDetails
Route of eliminationNot Available
Half life6-20 hours; 40-60% is excreted in urine unchanged, 20% is excreted in feces. Less than 10% is excreted by p-hydroxyclonidine.
ClearanceNot Available
ToxicityOral LD50 is 150 mg/kg in rat and 30 mg/kg in dog. Symptoms of overdose include constriction of pupils of the eye, drowsiness, high blood pressure followed by a drop in pressure, irritability, low body temperature, slowed breathing, slowed heartbeat, slowed reflexes, and weakness.
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 + 0.9632
Blood Brain Barrier + 0.9402
Caco-2 permeable + 0.8866
P-glycoprotein substrate Substrate 0.6305
P-glycoprotein inhibitor I Non-inhibitor 0.9061
P-glycoprotein inhibitor II Non-inhibitor 0.8383
Renal organic cation transporter Inhibitor 0.745
CYP450 2C9 substrate Non-substrate 0.8219
CYP450 2D6 substrate Non-substrate 0.6984
CYP450 3A4 substrate Non-substrate 0.6353
CYP450 1A2 substrate Non-inhibitor 0.8998
CYP450 2C9 substrate Non-inhibitor 0.7681
CYP450 2D6 substrate Inhibitor 0.8931
CYP450 2C19 substrate Non-inhibitor 0.8732
CYP450 3A4 substrate Non-inhibitor 0.8332
CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.803
Ames test Non AMES toxic 0.9133
Carcinogenicity Non-carcinogens 0.9303
Biodegradation Not ready biodegradable 0.9949
Rat acute toxicity 3.5030 LD50, mol/kg Not applicable
hERG inhibition (predictor I) Weak inhibitor 0.7232
hERG inhibition (predictor II) Non-inhibitor 0.8905
Pharmacoeconomics
Manufacturers
  • Boehringer ingelheim
  • Aveva drug delivery systems inc
  • Mylan technologies inc
  • Tris pharma inc
  • Pharmaforce inc
  • Bioniche pharma usa llc
  • Actavis elizabeth llc
  • American therapeutics inc
  • Dava pharmaceuticals inc
  • Duramed pharmaceuticals inc sub barr laboratories inc
  • Impax laboratories inc
  • Interpharm inc
  • Mutual pharmaceutical co inc
  • Mylan pharmaceuticals inc
  • Par pharmaceutical inc
  • Sandoz inc
  • Teva pharmaceuticals usa inc
  • Unichem laboratories ltd
  • Vintage pharmaceuticals llc
  • Warner chilcott div warner lambert co
  • Watson laboratories inc
  • Shionogi pharma inc
Packagers
Dosage forms
FormRouteStrength
Injection, solutionEpidural100 mcg/ml
Injection, solution, concentrateEpidural500 mcg/ml
PatchTransdermal0.1 mg/24 hours
PatchTransdermal0.2 mg/24 hours
PatchTransdermal0.3 mg/24 hours
TabletOral0.025 mg
TabletOral0.1 mg
TabletOral0.2 mg
TabletOral0.3 mg
Prices
Unit descriptionCostUnit
Catapres-TTS-3 4 0.3 mg/24hr Patches Box328.42USDbox
CloNIDine HCl 4 0.3 mg/24hr Patches Box279.9USDbox
Catapres-TTS-2 4 0.2 mg/24hr Patches Box236.75USDbox
CloNIDine HCl 4 0.2 mg/24hr Patches Box201.75USDbox
Catapres-TTS-1 4 0.1 mg/24hr Patches Box141.08USDbox
CloNIDine HCl 4 0.1 mg/24hr Patches Box119.84USDbox
Catapres-tts 3 patch78.95USDpatch
Clonidine 0.3 mg/day patch67.28USDpatch
Clonidine hcl powder53.09USDg
Clonidine 0.2 mg/day patch48.5USDpatch
Duraclon 500 mcg/ml vial47.4USDml
Catapres-tts 2 patch39.23USDpatch
Clonidine 0.1 mg/day patch28.81USDpatch
Catapres-tts 1 patch21.18USDpatch
Clonidine 5000 mcg/10 ml vial21.0USDml
Duraclon 0.1 mg/ml vial14.4USDml
Clonidine 1000 mcg/10 ml vial5.04USDml
Catapres 0.3 mg tablet2.98USDtablet
Catapres 0.2 mg tablet2.35USDtablet
Catapres 0.1 mg tablet1.57USDtablet
Clonidine hcl 0.3 mg tablet0.5USDtablet
Clonidine hcl 0.2 mg tablet0.35USDtablet
Catapres 0.2 mg Tablet0.35USDtablet
Apo-Clonidine 0.2 mg Tablet0.33USDtablet
Novo-Clonidine 0.2 mg Tablet0.33USDtablet
Nu-Clonidine 0.2 mg Tablet0.33USDtablet
Dixarit 0.025 mg Tablet0.28USDtablet
Clonidine hcl 0.1 mg tablet0.24USDtablet
Catapres 0.1 mg Tablet0.19USDtablet
Apo-Clonidine 0.1 mg Tablet0.18USDtablet
Novo-Clonidine 0.1 mg Tablet0.18USDtablet
Nu-Clonidine 0.1 mg Tablet0.18USDtablet
Apo-Clonidine 0.025 mg Tablet0.16USDtablet
Novo-Clonidine 0.025 mg Tablet0.16USDtablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
CountryPatent NumberApprovedExpires (estimated)
United States58691001993-10-132013-10-13
Properties
Statesolid
Experimental Properties
PropertyValueSource
melting point3053,202,660
water solubilityAppreciableNot Available
logP1.59HANSCH,C & LEO,AJ (1985)
Caco2 permeability-4.59ADME Research, USCD
pKa8.05 (at 25 °C)KONTTURI,K & MURTOMAKI,L (1992)
Predicted Properties
PropertyValueSource
water solubility4.80e-01 g/lALOGPS
logP2.55ALOGPS
logP2.49ChemAxon
logS-2.7ALOGPS
pKa (strongest basic)8.16ChemAxon
physiological charge1ChemAxon
hydrogen acceptor count3ChemAxon
hydrogen donor count2ChemAxon
polar surface area36.42ChemAxon
rotatable bond count1ChemAxon
refractivity59.09ChemAxon
polarizability21.7ChemAxon
number of rings2ChemAxon
bioavailability1ChemAxon
rule of fiveYesChemAxon
Ghose filterYesChemAxon
Veber's ruleYesChemAxon
MDDR-like ruleNoChemAxon
Spectra
SpectraNot Available
References
Synthesis Reference

David R. Pierce, William D. Dean, Michael E. Deason, “Process for preparation of clonidine derivatives.” U.S. Patent US5684156, issued October, 1968.

US5684156
General Reference
  1. Schapiro NA: “Dude, you don’t have Tourette’s:” Tourette’s syndrome, beyond the tics. Pediatr Nurs. 2002 May-Jun;28(3):243-6, 249-53. Pubmed
  2. Hossmann V, Maling TJ, Hamilton CA, Reid JL, Dollery CT: Sedative and cardiovascular effects of clonidine and nitrazepam. Clin Pharmacol Ther. 1980 Aug;28(2):167-76. Pubmed
External Links
ResourceLink
KEGG DrugD00281
PubChem Compound2803
PubChem Substance46508119
ChemSpider2701
ChEBI46631
ChEMBLCHEMBL134
Therapeutic Targets DatabaseDAP000231
PharmGKBPA449051
IUPHAR516
Guide to Pharmacology516
HETCLU
Drug Product Database2247608
RxListhttp://www.rxlist.com/cgi/generic/clonidin.htm
Drugs.comhttp://www.drugs.com/clonidine.html
PDRhealthhttp://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/cat1072.shtml
WikipediaClonidine
ATC CodesC02AC01N02CX02S01EA04S01EA03
AHFS Codes
  • 24:08.16
PDB EntriesNot Available
FDA labelNot Available
MSDSshow(73.8 KB)
Interactions
Drug Interactions
Drug
AcebutololIncreased hypertension when clonidine stopped
AmitriptylineThe tricyclic antidepressant, amitriptyline, decreases the effect of clonidine.
AmoxapineThe tricyclic antidepressant, amoxapine, decreases the effect of clonidine.
AtenololIncreased hypertension when clonidine stopped
BetaxololIncreased hypertension when clonidine stopped
BevantololIncreased hypertension when clonidine stopped
BisoprololIncreased hypertension when clonidine stopped
CarteololIncreased hypertension when clonidine stopped
CarvedilolIncreased hypertension when clonidine stopped
ClomipramineThe tricyclic antidepressant, clomipramine, may decrease the effect of clonidine.
DesipramineThe tricyclic antidepressant, desipramine, decreases the effect of clonidine.
DoxepinThe tricyclic antidepressant, doxepin, decreases the effect of clonidine.
EsmololIncreased hypertension when clonidine stopped
ImipramineThe tricyclic antidepressant, imipramine, decreases the effect of clonidine.
LabetalolIncreased hypertension when clonidine stopped
MetoprololIncreased hypertension when clonidine stopped
MilnacipranBecause Savella inhibits norepinephrine reuptake, co-administration with clonidine may inhibit clonidine's anti-hypertensive effect.
MirtazapinePossible hypertensive crisis
NadololIncreased hypertension when clonidine stopped
NortriptylineThe tricyclic antidepressant, nortriptyline, decreases the effect of clonidine.
OxprenololIncreased hypertension when clonidine stopped
PenbutololIncreased hypertension when clonidine stopped
PindololIncreased hypertension when clonidine stopped
PractololIncreased hypertension when clonidine stopped
PropranololIncreased hypertension when clonidine stopped
ProtriptylineThe tricyclic antidepressant, protriptyline, decreases the effect of clonidine.
SotalolIncreased hypertension when clonidine stopped
TimololIncreased hypertension when clonidine stopped
TreprostinilAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
TrimipramineTrimipramine may reduce the antihypertensive effect of the alpha2-agonist, Clonidine. Trimipramine may also increase the rebound hypertensive effect of Clonidine. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of Clonidine if Trimipramine is initiated, discontinued or dose changed. Clonidine should be withdrawn very gradually to reduce the risk of hypertensive crisis.
Food Interactions
  • Avoid alcohol.
  • Take without regard to meals.

1. Alpha-2A adrenergic receptor

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: agonist

Components

Name UniProt ID Details
Alpha-2A adrenergic receptor P08913 Details

References:

  1. Fairbanks CA, Stone LS, Kitto KF, Nguyen HO, Posthumus IJ, Wilcox GL: alpha(2C)-Adrenergic receptors mediate spinal analgesia and adrenergic-opioid synergy. J Pharmacol Exp Ther. 2002 Jan;300(1):282-90. Pubmed
  2. Hein, L. (2004). α-Adrenergic system. In S. Offermanns, & W. Rosenthal (Eds.). Encyclopedic reference of molecular pharmacology (pp. 27-30). Berlin, Germany: Springer.
  3. Lavand’homme PM, Ma W, De Kock M, Eisenach JC: Perineural alpha(2A)-adrenoceptor activation inhibits spinal cord neuroplasticity and tactile allodynia after nerve injury. Anesthesiology. 2002 Oct;97(4):972-80. Pubmed
  4. Ozdogan UK, Lahdesmaki J, Hakala K, Scheinin M: The involvement of alpha 2A-adrenoceptors in morphine analgesia, tolerance and withdrawal in mice. Eur J Pharmacol. 2004 Aug 23;497(2):161-71. Pubmed
  5. Ozdogan UK, Lahdesmaki J, Mansikka H, Scheinin M: Loss of amitriptyline analgesia in alpha 2A-adrenoceptor deficient mice. Eur J Pharmacol. 2004 Feb 6;485(1-3):193-6. Pubmed
  6. Wang XM, Zhang ZJ, Bains R, Mokha SS: Effect of antisense knock-down of alpha(2a)- and alpha(2c)-adrenoceptors on the antinociceptive action of clonidine on trigeminal nociception in the rat. Pain. 2002 Jul;98(1-2):27-35. Pubmed

2. Alpha-2B adrenergic receptor

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: agonist

Components

Name UniProt ID Details
Alpha-2B adrenergic receptor P18089 Details

References:

  1. Hein, L. (2004). α-Adrenergic system. In S. Offermanns, & W. Rosenthal (Eds.). Encyclopedic reference of molecular pharmacology (pp. 27-30). Berlin, Germany: Springer.

3. Alpha-2C adrenergic receptor

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: agonist

Components

Name UniProt ID Details
Alpha-2C adrenergic receptor P18825 Details

References:

  1. Hein, L. (2004). α-Adrenergic system. In S. Offermanns, & W. Rosenthal (Eds.). Encyclopedic reference of molecular pharmacology (pp. 27-30). Berlin, Germany: Springer.

1. Cytochrome P450 2D6

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 2D6 P10635 Details

References:

  1. Claessens AJ, Risler LJ, Eyal S, Shen DD, Easterling TR, Hebert MF: CYP2D6 mediates 4-hydroxylation of clonidine in vitro: implication for pregnancy-induced changes in clonidine clearance. Drug Metab Dispos. 2010 Sep;38(9):1393-6. Epub 2010 Jun 22. Pubmed

2. Cytochrome P450 1A2

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 1A2 P05177 Details

References:

  1. Claessens AJ, Risler LJ, Eyal S, Shen DD, Easterling TR, Hebert MF: CYP2D6 mediates 4-hydroxylation of clonidine in vitro: implication for pregnancy-induced changes in clonidine clearance. Drug Metab Dispos. 2010 Sep;38(9):1393-6. Epub 2010 Jun 22. Pubmed

3. Cytochrome P450 3A4

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 3A4 P08684 Details

References:

  1. Claessens AJ, Risler LJ, Eyal S, Shen DD, Easterling TR, Hebert MF: CYP2D6 mediates 4-hydroxylation of clonidine in vitro: implication for pregnancy-induced changes in clonidine clearance. Drug Metab Dispos. 2010 Sep;38(9):1393-6. Epub 2010 Jun 22. Pubmed

4. Cytochrome P450 1A1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 1A1 P04798 Details

References:

  1. Claessens AJ, Risler LJ, Eyal S, Shen DD, Easterling TR, Hebert MF: CYP2D6 mediates 4-hydroxylation of clonidine in vitro: implication for pregnancy-induced changes in clonidine clearance. Drug Metab Dispos. 2010 Sep;38(9):1393-6. Epub 2010 Jun 22. Pubmed

5. Cytochrome P450 3A5

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 3A5 P20815 Details

References:

  1. Claessens AJ, Risler LJ, Eyal S, Shen DD, Easterling TR, Hebert MF: CYP2D6 mediates 4-hydroxylation of clonidine in vitro: implication for pregnancy-induced changes in clonidine clearance. Drug Metab Dispos. 2010 Sep;38(9):1393-6. Epub 2010 Jun 22. Pubmed

1. Solute carrier family 22 member 1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: 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. Martel F, Vetter T, Russ H, Grundemann D, Azevedo I, Koepsell H, Schomig E: Transport of small organic cations in the rat liver. The role of the organic cation transporter OCT1. Naunyn Schmiedebergs Arch Pharmacol. 1996 Aug-Sep;354(3):320-6. Pubmed

2. 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. Wu X, Huang W, Ganapathy ME, Wang H, Kekuda R, Conway SJ, Leibach FH, Ganapathy V: Structure, function, and regional distribution of the organic cation transporter OCT3 in the kidney. Am J Physiol Renal Physiol. 2000 Sep;279(3):F449-58. Pubmed
  2. Martel F, Grundemann D, Calhau C, Schomig E: Apical uptake of organic cations by human intestinal Caco-2 cells: putative involvement of ASF transporters. Naunyn Schmiedebergs Arch Pharmacol. 2001 Jan;363(1):40-9. Pubmed

3. 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. Ohashi R, Tamai I, Yabuuchi H, Nezu JI, Oku A, Sai Y, Shimane M, Tsuji A: Na(+)-dependent carnitine transport by organic cation transporter (OCTN2): its pharmacological and toxicological relevance. J Pharmacol Exp Ther. 1999 Nov;291(2):778-84. 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

4. 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

5. Multidrug resistance protein 1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Multidrug resistance protein 1 P08183 Details

References:

  1. Faassen F, Vogel G, Spanings H, Vromans H: Caco-2 permeability, P-glycoprotein transport ratios and brain penetration of heterocyclic drugs. Int J Pharm. 2003 Sep 16;263(1-2):113-22. Pubmed

Comments
Drug created on June 13, 2005 07:24 / Updated on September 16, 2013 17:11