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Identification
NameSumatriptan
Accession NumberDB00669  (APRD00379)
Typesmall molecule
Groupsapproved, investigational
Description

A serotonin agonist that acts selectively at 5HT1 receptors. It is used in the treatment of migraine disorders. A transdermal patch version of sumatriptan is currently in phase I trials in the U.S. under the code name NP101 (NuPathe).

Structure
Thumb
Synonyms
SynonymLanguageCode
(3-[2-(dimethylamino)Ethyl]-1H-indol-5-yl)-N-methylmethanesulfonamideNot AvailableNot Available
1-[3-(2-Dimethylaminoethyl)-1H-indol-5-yl]-N-methyl-methanesulfonamideNot AvailableNot Available
3-(2-(dimethylamino)Ethyl)-N-methyl-1H-indole-5-methanesulfonamideNot AvailableNot Available
3-[2-(dimethylamino)Ethyl]-N-methylindole-5-methanesulfonamideNot AvailableNot Available
ImigranNot AvailableNot Available
ImitrexNot AvailableNot Available
NP101Not AvailableNot Available
SumatranNot AvailableNot Available
SumatriptanGerman/FrenchINN
SumatriptánSpanishINN
Sumatriptan SuccinateNot AvailableNot Available
SumatriptanumLatinINN
SumaxNot AvailableNot Available
triptanNot AvailableNot Available
Salts
Name/CAS Structure Properties
Sumatriptan Succinate
Thumb Not applicable DBSALT001003
Brand names
NameCompany
AdraconInti
ALSUMANot Available
AltaxaAlapis Pharma
ApigraneAdvanced Pharmaceutical
Boots Pharmacy Migraine ReliefBoots
CinieZentiva
FrimigOrion
IllumentPliva
ImigenMylan
ImigranGlaxoSmithKline
Imigran miteGlaxoSmithKline
Imigran RadisGlaxoSmithKline
ImigraneGlaxoSmithKline
ImitrexGlaxoSmithKline
Imitrex OralGlaxoSmithKline
MigralginGMP
MigraneitorDriburg
NazdavDr. Reddy's
SapphirexHemofarm
SumatranRowex
SumaxLibbs
SuminatSun
YoushuSimcere
ZECUITYNot Available
Brand mixtures
Brand NameIngredients
TreximetSumatriptan and Naproxen
Categories
CAS number103628-46-2
WeightAverage: 295.4
Monoisotopic: 295.135447621
Chemical FormulaC14H21N3O2S
InChI KeyKQKPFRSPSRPDEB-UHFFFAOYSA-N
InChI
InChI=1S/C14H21N3O2S/c1-15-20(18,19)10-11-4-5-14-13(8-11)12(9-16-14)6-7-17(2)3/h4-5,8-9,15-16H,6-7,10H2,1-3H3
IUPAC Name
1-{3-[2-(dimethylamino)ethyl]-1H-indol-5-yl}-N-methylmethanesulfonamide
SMILES
CNS(=O)(=O)CC1=CC2=C(NC=C2CCN(C)C)C=C1
Mass SpecNot Available
Taxonomy
KingdomOrganic Compounds
SuperclassHeterocyclic Compounds
ClassIndoles and Derivatives
SubclassTryptamines and Derivatives
Direct parentTryptamines and Derivatives
Alternative parentsIndoles; Benzene and Substituted Derivatives; Substituted Pyrroles; Sulfonamides; Sulfonyls; Tertiary Amines; Polyamines
Substituentsindole; substituted pyrrole; benzene; sulfonyl; sulfonamide; pyrrole; sulfonic acid derivative; tertiary amine; polyamine; amine; organonitrogen compound
Classification descriptionThis compound belongs to the tryptamines and derivatives. These are compounds containing the tryptamine backbone, which is structurally characterized by an indole ring subsituted at the thrid position by an ethanamine.
Pharmacology
IndicationFor the treatment of migraine attacks with or without aura.
PharmacodynamicsSumatriptan, an antimigraine drug, is a selective agonist of vascular serotonin ((5-hydroxytryptamine; 5-HT) type 1-like receptors, likely the 5-HT1D and 5-HT1B subtypes. It has no significant affinity (as measured using standard radioligand binding assays) or pharmacological activity at 5-HT2, 5-HT3 receptor subtypes or at alpha1-, alpha2-, or beta-adrenergic; dopamine1; dopamine2; muscarinic; or benzodiazepine receptors.
Mechanism of actionThe 5-HT1B and 5-HT1D receptors function as autoreceptors, which inhibit the firing of serotonin neurons and a reduction in the synthesis and release of serotonin upon activation. After sumatriptan binds to these receptors, adenylate cyclase activity is inhibited via regulatory G proteins, incrases intracellular calcium, and affects other intracellular events. This results in vasoconstriction and inhibtion of sensory nociceptive (trigeminal) nerve firing and vasoactive neuropeptide release.
AbsorptionApproximately 15%
Volume of distribution
  • 2.7 L/kg [subcutaneous dosing]
Protein binding14%-21%
Metabolism

Hepatic. In vitro studies with human microsomes suggest that sumatriptan is metabolized by monoamine oxidase (MAO), predominantly the A isoenzyme.

Route of eliminationOnly 3% of the dose is excreted in the urine as unchanged sumatriptan; 42% of the dose is excreted as the major metabolite, the indole acetic acid analogue of sumatriptan.
Half life2.5 hours
Clearance
  • 1200 mL/min [Following a 6-mg SC injection]
ToxicitySymptoms of overdose include convulsions, tremor, paralysis, inactivity, ptosis, erythema of the extremities, abnormal respiration, cyanosis, ataxia, mydriasis, salivation, and lacrimation.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated Effects
Interacting Gene/EnzymeSNP RS IDAllele nameDefining changeEffectReference(s)
Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-3
Gene symbol: GNB3
UniProt: P16520
rs5443 Not AvailableT AlleleBetter response to drug treatment17361120
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
Property Value Probability
Human Intestinal Absorption + 1.0
Blood Brain Barrier + 0.9626
Caco-2 permeable - 0.8957
P-glycoprotein substrate Substrate 0.5914
P-glycoprotein inhibitor I Non-inhibitor 0.8782
P-glycoprotein inhibitor II Non-inhibitor 0.9081
Renal organic cation transporter Non-inhibitor 0.7344
CYP450 2C9 substrate Non-substrate 0.8014
CYP450 2D6 substrate Non-substrate 0.5913
CYP450 3A4 substrate Substrate 0.6029
CYP450 1A2 substrate Non-inhibitor 0.5603
CYP450 2C9 substrate Non-inhibitor 0.7898
CYP450 2D6 substrate Non-inhibitor 0.7422
CYP450 2C19 substrate Non-inhibitor 0.7428
CYP450 3A4 substrate Non-inhibitor 0.8309
CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.6974
Ames test Non AMES toxic 0.649
Carcinogenicity Non-carcinogens 0.8134
Biodegradation Not ready biodegradable 1.0
Rat acute toxicity 2.5404 LD50, mol/kg Not applicable
hERG inhibition (predictor I) Weak inhibitor 0.5668
hERG inhibition (predictor II) Non-inhibitor 0.7046
Pharmacoeconomics
Manufacturers
  • Glaxosmithkline
  • King pharmaceuticals inc
  • App pharmaceuticals llc
  • Bedford laboratories div ben venue laboratories inc
  • Bedford laboratories
  • Jhp pharmaceuticals llc
  • Par pharmaceutical inc
  • Sagent strides llc
  • Sandoz canada inc
  • Teva parenteral medicines inc
  • Wockhardt ltd
  • Zogenix inc
  • Aurobindo pharma ltd
  • Dr reddys laboratories inc
  • Mylan pharmaceuticals inc
  • Orchid healthcare
  • Ranbaxy laboratories ltd
  • Roxane laboratories inc
  • Sandoz inc
  • Sun pharmaceutical industries ltd
  • Teva pharmaceuticals usa inc
  • Watson laboratories inc
Packagers
Dosage forms
FormRouteStrength
LiquidSubcutaneous
Patch, extended releaseTransdermal
SprayNasal
TabletOral
Prices
Unit descriptionCostUnit
Imitrex 4 mg/0.5 ml syringe kit229.02USDkit
Imitrex 6 mg/0.5 ml syringe kit229.02USDkit
Imitrex STATdose Refill 1 Ea = 2 unit Refill Box217.16USDbox
Imitrex 4 mg/0.5 ml kit refill216.92USDkit
Imitrex 6 mg/0.5 ml kit refill216.92USDkit
SUMAtriptan Succinate Refill 6 mg/0.5ml Kit Box191.84USDbox
Sumatriptan 6 mg/0.5 ml refill184.46USDeach
Sumatriptan 4 mg/0.5 ml refill184.44USDeach
Imitrex 6 mg/0.5 ml vial106.84USDvial
Imitrex 6 mg/0.5ml Solution 0.5ml Vial98.93USDvial
Imitrex 5 mg/act Solution Nasal Inhaler55.49USDinhaler
Imitrex 20 mg nasal spray45.73USDeach
Imitrex 5 mg nasal spray45.73USDeach
Imitrex 20 mg/act Solution Nasal Inhaler43.44USDinhaler
Sumatriptan 20 mg nasal spray38.89USDeach
Sumatriptan 5 mg nasal spray38.89USDeach
Imitrex 25 mg tablet32.45USDtablet
Imitrex 100 mg tablet30.16USDtablet
Imitrex 50 mg tablet30.16USDtablet
Sumatriptan Succinate 25 mg tablet28.14USDtablet
Sumatriptan succ 25 mg tablet27.06USDtablet
Sumatriptan Succinate 100 mg tablet26.15USDtablet
Sumatriptan Succinate 50 mg tablet26.15USDtablet
Sumatriptan succ 100 mg tablet25.14USDtablet
Sumatriptan succ 50 mg tablet25.14USDtablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
CountryPatent NumberApprovedExpires (estimated)
United States61359791997-03-212017-03-21
United States57055201994-12-102011-12-10
Canada24690192005-09-132022-12-04
Canada20983022001-10-162011-12-10
Properties
Statesolid
Experimental Properties
PropertyValueSource
melting point169-171 ┬░CNot Available
water solubility21.4 mg/mlNot Available
logP0.93ADLARD,M ET AL. (1995)
Predicted Properties
PropertyValueSource
water solubility1.27e-01 g/lALOGPS
logP1.17ALOGPS
logP0.74ChemAxon
logS-3.4ALOGPS
pKa (strongest acidic)11.24ChemAxon
pKa (strongest basic)9.54ChemAxon
physiological charge1ChemAxon
hydrogen acceptor count3ChemAxon
hydrogen donor count2ChemAxon
polar surface area65.2ChemAxon
rotatable bond count5ChemAxon
refractivity82.08ChemAxon
polarizability32.31ChemAxon
number of rings2ChemAxon
bioavailability1ChemAxon
rule of fiveYesChemAxon
Ghose filterYesChemAxon
Veber's ruleNoChemAxon
MDDR-like ruleNoChemAxon
Spectra
SpectraNot Available
References
Synthesis Reference

Rajeev Mathur, T. Kumar, Sunilendu Roy, Rajiv Malik, “Taste masked sumatriptan tablets and processes for their preparation.” U.S. Patent US20060233875, issued October 19, 2006.

US20060233875
General Reference
  1. Nikai T, Basbaum AI, Ahn AH: Profound reduction of somatic and visceral pain in mice by intrathecal administration of the anti-migraine drug, sumatriptan. Pain. 2008 Oct 31;139(3):533-40. Epub 2008 Aug 23. Pubmed
External Links
ResourceLink
KEGG DrugD00451
KEGG CompoundC07319
PubChem Compound5358
PubChem Substance46506520
ChemSpider5165
ChEBI10650
ChEMBLCHEMBL128
Therapeutic Targets DatabaseDNC001649
PharmGKBPA451566
IUPHAR119
Guide to Pharmacology119
Drug Product Database2239738
RxListhttp://www.rxlist.com/cgi/generic/sumitr.htm
Drugs.comhttp://www.drugs.com/cdi/sumatriptan.html
WikipediaSumatriptan
ATC CodesN02CC01
AHFS Codes
  • 28:32.28
PDB EntriesNot Available
FDA labelshow(142 KB)
MSDSshow(49.9 KB)
Interactions
Drug Interactions
Drug
CitalopramIncreased risk of CNS adverse effects
DesvenlafaxineIncreased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
DihydroergotaminePossible severe and prolonged vasoconstriction
ErgotaminePossible severe and prolonged vasoconstriction
EscitalopramIncreased risk of CNS adverse effects
FluoxetineIncreased risk of CNS adverse effects
FluvoxamineIncreased risk of CNS adverse effects
IsocarboxazidThe MAO inhibitor, isocarboxazid, may decrease the metabolism and clearance of the serotonin 5-HT receptor agonist, sumatriptan. Concomitant therapy is contraindicated.
LithiumPossible serotoninergic syndrome with this combination
MethysergidePossible severe and prolonged vasoconstriction
NefazodoneIncreased risk of CNS adverse effects
ParoxetineIncreased risk of CNS adverse effects
PhenelzineThe MAO inhibitor, phenelzine, may decrease the metabolism and clearance of the serotonin 5-HT receptor agonist, sumatriptan. Concomitant therapy is contraindicated.
TramadolIncreased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
TranylcypromineThe MAO inhibitor, Tranylcypromine, may reduce the metabolism and clearance of the serotonin 5-HT1D receptor agonist, Sumatriptan. Risk of serotonin syndrome and Sumatriptan toxicity. Concomitant therapy should be avoided.
TrazodoneIncreased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
TrimipramineIncreased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
VenlafaxineIncreased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
VilazodoneIncreased risk of serotonin syndrome
ZolmitriptanConcomitant use of two serotonin 5-HT1D receptor agonists, such as zolmitriptan and sumatriptan, may result in additive vasoconstrictive effects. Concomitant use within 24 hours is contraindicated.
Food InteractionsNot Available

Targets

1. 5-hydroxytryptamine receptor 1D

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: agonist

Components

Name UniProt ID Details
5-hydroxytryptamine receptor 1D P28221 Details

References:

  1. Koran LM, Pallanti S, Quercioli L: Sumatriptan, 5-HT receptors and obsessive-compulsive disorder. Eur Neuropsychopharmacol. 2001 Apr;11(2):169-72. Pubmed
  2. Baxter LR Jr: Brain mediation of Anolis social dominance displays. III. Differential forebrain 3H-sumatriptan binding in dominant vs. submissive males. Brain Behav Evol. 2001 Apr;57(4):202-13. Pubmed
  3. Razzaque Z, Pickard JD, Ma QP, Shaw D, Morrison K, Wang T, Longmore J: 5-HT1B-receptors and vascular reactivity in human isolated blood vessels: assessment of the potential craniovascular selectivity of sumatriptan. Br J Clin Pharmacol. 2002 Mar;53(3):266-74. Pubmed
  4. Akin D, Gurdal H: Involvement of 5-HT1B and 5-HT1D receptors in sumatriptan mediated vasocontractile response in rabbit common carotid artery. Br J Pharmacol. 2002 May;136(2):177-82. Pubmed
  5. Zohar J, Kennedy JL, Hollander E, Koran LM: Serotonin-1D hypothesis of obsessive-compulsive disorder: an update. J Clin Psychiatry. 2004;65 Suppl 14:18-21. Pubmed
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed
  7. Mitsikostas DD, Sanchez del Rio M, Moskowitz MA, Waeber C: Both 5-HT1B and 5-HT1F receptors modulate c-fos expression within rat trigeminal nucleus caudalis. Eur J Pharmacol. 1999 Mar 26;369(3):271-7. Pubmed
  8. Cohen ML, Schenck KW, Hemrick-Luecke SH: 5-Hydroxytryptamine(1A) receptor activation enhances norepinephrine release from nerves in the rabbit saphenous vein. J Pharmacol Exp Ther. 1999 Sep;290(3):1195-201. Pubmed
  9. Roy A, Brand NJ, Yacoub MH: Expression of 5-hydroxytryptamine receptor subtype messenger RNA in interstitial cells from human heart valves. J Heart Valve Dis. 2000 Mar;9(2):256-60; discussion 260-1. Pubmed
  10. Nikai T, Basbaum AI, Ahn AH: Profound reduction of somatic and visceral pain in mice by intrathecal administration of the anti-migraine drug, sumatriptan. Pain. 2008 Oct 31;139(3):533-40. Epub 2008 Aug 23. Pubmed
  11. Mitsikostas DD, Sanchez del Rio M, Waeber C: 5-Hydroxytryptamine(1B/1D) and 5-hydroxytryptamine1F receptors inhibit capsaicin-induced c-fos immunoreactivity within mouse trigeminal nucleus caudalis. Cephalalgia. 2002 Jun;22(5):384-94. Pubmed

2. 5-hydroxytryptamine receptor 1B

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: agonist

Components

Name UniProt ID Details
5-hydroxytryptamine receptor 1B P28222 Details

References:

  1. Dupuis DS, Perez M, Halazy S, Colpaert FC, Pauwels PJ: Magnitude of 5-HT1B and 5-HT1A receptor activation in guinea-pig and rat brain: evidence from sumatriptan dimer-mediated [35S]GTPgammaS binding responses. Brain Res Mol Brain Res. 1999 Apr 6;67(1):107-23. Pubmed
  2. Mitsikostas DD, Sanchez del Rio M, Moskowitz MA, Waeber C: Both 5-HT1B and 5-HT1F receptors modulate c-fos expression within rat trigeminal nucleus caudalis. Eur J Pharmacol. 1999 Mar 26;369(3):271-7. Pubmed
  3. Cohen ML, Schenck KW, Hemrick-Luecke SH: 5-Hydroxytryptamine(1A) receptor activation enhances norepinephrine release from nerves in the rabbit saphenous vein. J Pharmacol Exp Ther. 1999 Sep;290(3):1195-201. Pubmed
  4. Cohen Z, Bouchelet I, Olivier A, Villemure JG, Ball R, Stanimirovic DB, Hamel E: Multiple microvascular and astroglial 5-hydroxytryptamine receptor subtypes in human brain: molecular and pharmacologic characterization. J Cereb Blood Flow Metab. 1999 Aug;19(8):908-17. Pubmed
  5. Granas C, Larhammar D: Identification of an amino acid residue important for binding of methiothepin and sumatriptan to the human 5-HT receptor. Eur J Pharmacol. 1999 Sep 10;380(2-3):171-81. Pubmed
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed
  7. Razzaque Z, Pickard JD, Ma QP, Shaw D, Morrison K, Wang T, Longmore J: 5-HT1B-receptors and vascular reactivity in human isolated blood vessels: assessment of the potential craniovascular selectivity of sumatriptan. Br J Clin Pharmacol. 2002 Mar;53(3):266-74. Pubmed
  8. Akin D, Gurdal H: Involvement of 5-HT1B and 5-HT1D receptors in sumatriptan mediated vasocontractile response in rabbit common carotid artery. Br J Pharmacol. 2002 May;136(2):177-82. Pubmed
  9. Roy A, Brand NJ, Yacoub MH: Expression of 5-hydroxytryptamine receptor subtype messenger RNA in interstitial cells from human heart valves. J Heart Valve Dis. 2000 Mar;9(2):256-60; discussion 260-1. Pubmed
  10. Nikai T, Basbaum AI, Ahn AH: Profound reduction of somatic and visceral pain in mice by intrathecal administration of the anti-migraine drug, sumatriptan. Pain. 2008 Oct 31;139(3):533-40. Epub 2008 Aug 23. Pubmed
  11. Mitsikostas DD, Sanchez del Rio M, Waeber C: 5-Hydroxytryptamine(1B/1D) and 5-hydroxytryptamine1F receptors inhibit capsaicin-induced c-fos immunoreactivity within mouse trigeminal nucleus caudalis. Cephalalgia. 2002 Jun;22(5):384-94. Pubmed

3. 5-hydroxytryptamine receptor 1F

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: agonist

Components

Name UniProt ID Details
5-hydroxytryptamine receptor 1F P30939 Details

References:

  1. Razzaque Z, Heald MA, Pickard JD, Maskell L, Beer MS, Hill RG, Longmore J: Vasoconstriction in human isolated middle meningeal arteries: determining the contribution of 5-HT1B- and 5-HT1F-receptor activation. Br J Clin Pharmacol. 1999 Jan;47(1):75-82. Pubmed
  2. Pauwels PJ, John GW: Present and future of 5-HT receptor agonists as antimigraine drugs. Clin Neuropharmacol. 1999 May-Jun;22(3):123-36. Pubmed
  3. Cohen ML, Schenck K: Contractile responses to sumatriptan and ergotamine in the rabbit saphenous vein: effect of selective 5-HT receptor agonists and PGF. Br J Pharmacol. 2000 Oct;131(3):562-8. Pubmed
  4. Janssen P, Tack J, Sifrim D, Meulemans AL, Lefebvre RA: Influence of 5-HT1 receptor agonists on feline stomach relaxation. Eur J Pharmacol. 2004 May 25;492(2-3):259-67. Pubmed
  5. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed
  6. Mitsikostas DD, Sanchez del Rio M, Moskowitz MA, Waeber C: Both 5-HT1B and 5-HT1F receptors modulate c-fos expression within rat trigeminal nucleus caudalis. Eur J Pharmacol. 1999 Mar 26;369(3):271-7. Pubmed
  7. Nikai T, Basbaum AI, Ahn AH: Profound reduction of somatic and visceral pain in mice by intrathecal administration of the anti-migraine drug, sumatriptan. Pain. 2008 Oct 31;139(3):533-40. Epub 2008 Aug 23. Pubmed
  8. Mitsikostas DD, Sanchez del Rio M, Waeber C: 5-Hydroxytryptamine(1B/1D) and 5-hydroxytryptamine1F receptors inhibit capsaicin-induced c-fos immunoreactivity within mouse trigeminal nucleus caudalis. Cephalalgia. 2002 Jun;22(5):384-94. Pubmed

4. 5-hydroxytryptamine receptor 1A

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: agonist

Components

Name UniProt ID Details
5-hydroxytryptamine receptor 1A P08908 Details

References:

  1. Johnson DE, Rollema H, Schmidt AW, McHarg AD: Serotonergic effects and extracellular brain levels of eletriptan, zolmitriptan and sumatriptan in rat brain. Eur J Pharmacol. 2001 Aug 17;425(3):203-10. Pubmed

Enzymes

1. Amine oxidase [flavin-containing] A

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Amine oxidase [flavin-containing] A P21397 Details

References:

  1. Fox AW: Subcutaneous sumatriptan pharmacokinetics: delimiting the monoamine oxidase inhibitor effect. Headache. 2010 Feb;50(2):249-55. Epub 2009 Nov 17. Pubmed
  2. Fuseau E, Petricoul O, Moore KH, Barrow A, Ibbotson T: Clinical pharmacokinetics of intranasal sumatriptan. Clin Pharmacokinet. 2002;41(11):801-11. Pubmed

Transporters

1. Solute carrier organic anion transporter family member 1A2

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inducer

Components

Name UniProt ID Details
Solute carrier organic anion transporter family member 1A2 P46721 Details

References:

  1. Lu R, Kanai N, Bao Y, Wolkoff AW, Schuster VL: Regulation of renal oatp mRNA expression by testosterone. Am J Physiol. 1996 Feb;270(2 Pt 2):F332-7. Pubmed

2. Multidrug resistance protein 1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Multidrug resistance protein 1 P08183 Details

References:

  1. Mahar Doan KM, Humphreys JE, Webster LO, Wring SA, Shampine LJ, Serabjit-Singh CJ, Adkison KK, Polli JW: Passive permeability and P-glycoprotein-mediated efflux differentiate central nervous system (CNS) and non-CNS marketed drugs. J Pharmacol Exp Ther. 2002 Dec;303(3):1029-37. Pubmed

3. ATP-binding cassette sub-family G member 2

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
ATP-binding cassette sub-family G member 2 Q9UNQ0 Details

References:

  1. Janvilisri T, Venter H, Shahi S, Reuter G, Balakrishnan L, van Veen HW: Sterol transport by the human breast cancer resistance protein (ABCG2) expressed in Lactococcus lactis. J Biol Chem. 2003 Jun 6;278(23):20645-51. Epub 2003 Mar 28. Pubmed

4. Solute carrier organic anion transporter family member 1B1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Solute carrier organic anion transporter family member 1B1 Q9Y6L6 Details

References:

  1. Suzuki H, Sugiyama Y: Transport of drugs across the hepatic sinusoidal membrane: sinusoidal drug influx and efflux in the liver. Semin Liver Dis. 2000;20(3):251-63. Pubmed

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