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Identification
Name Promethazine
Accession Number DB01069 (APRD00601)
Type small molecule
Groups approved
Description

A phenothiazine derivative with histamine H1-blocking, antimuscarinic, and sedative properties. It is used as an antiallergic, in pruritus, for motion sickness and sedation, and also in animals. [PubChem]

Structure Thumb
Download: MOL | SDF | SMILES | InChI
Display: 2D Structure | 3D Structure
Synonyms
  • Isopromethazine
  • Lilly 1516
  • Proazaimine
  • Proazamine
  • Promazinamide
  • Prometazine
  • Promethazin
  • Promethazine Hcl
  • Promethiazine
  • Promezathine
  • Prothazin
  • Prothazine
Brand names
  • Allergan
  • Aprobit
  • Avomine
  • Dimapp
  • Diphergan
  • Diprazine
  • Diprozin
  • Dorme
  • Duplamin
  • Fargan
  • Fellozine
  • Fenazil
  • Fenergan
  • Fenetazina
  • Genphen
  • Hiberna
  • Histargan
  • Iergigan
  • Isophenergan
  • Lercigan
  • Lergigan
  • Mymethazine Fortis
  • Phargan
  • Phenargan
  • Phencen
  • Phenergan
  • Phenergan Fortis
  • Phensedyl
  • Pilpophen
  • Pipolphen
  • Procit
  • Prometasin
  • Prometazin
  • Prometh Fortis
  • Prometh Plain
  • Promethacon
  • Promethaine
  • Promethegan
  • Prorex
  • Protazine
  • Provigan
  • Pyrethia
  • Pyrethiazine
  • Remsed
  • Romergan
  • Synalgos
  • Tanidil
  • Thiergan
  • Valergine
  • Vallergine
  • Zipan-25
Brand name mixtures
  • Phenergan VC Expectorant Syrup (Phenylephrine hydrochloride + Potassium guaiacol sulphonate + Promethazine hydrochloride)
Categories
  • Antipruritics
  • Anti-Allergic Agents
  • Histamine H1 Antagonists
  • Phenothiazine Derivatives
CAS number 60-87-7
Weight Average: 284.419
Monoisotopic: 284.134719340
Chemical Formula C17H20N2S
InChI Key InChIKey=PWWVAXIEGOYWEE-UHFFFAOYSA-N
InChI
InChI=1S/C17H20N2S/c1-13(18(2)3)12-19-14-8-4-6-10-16(14)20-17-11-7-5-9-15(17)19/h4-11,13H,12H2,1-3H3
Plain Text
IUPAC Name
dimethyl[1-(10H-phenothiazin-10-yl)propan-2-yl]amine
SMILES
CC(CN1C2=C(SC3=C1C=CC=C3)C=CC=C2)N(C)C
Plain Text
Mass Spec show (7.9 KB)
Taxonomy
Kingdom Organic
Classes
  • Phenothiazines
Substructures
  • Ethers
  • Phenothiazines
  • Aliphatic and Aryl Amines
  • Thiazines
  • Benzene and Derivatives
  • Heterocyclic compounds
  • Aromatic compounds
  • Anilines
Pharmacology
Indication For the treatment of allergic disorders, and nausea/vomiting.
Pharmacodynamics Promethazine, a phenothiazine, is an H1-antagonist with anticholinergic, sedative, and antiemetic effects and some local anesthetic properties. Promethazine is used as an antiemetic or to prevent motion sickness.
Mechanism of action Like other H1-antagonists, promethazine competes with free histamine for binding at H1-receptor sites in the GI tract, uterus, large blood vessels, and bronchial muscle. The relief of nausea appears to be related to central anticholinergic actions and may implicate activity on the medullary chemoreceptor trigger zone.
Absorption On average, 88% of a promethazine dose is absorbed after oral administration; however, the absolute bioavailability is only 25% because of first-pass clearance.
Volume of distribution Not Available
Protein binding 93%
Metabolism

Hepatic

Route of elimination Promethazine hydrochloride is metabolized in the liver, with the sulfoxides of promethazine and N-desmethylpromethazine being the predominant metabolites appearing in the urine.
Half life 16-19 hours
Clearance Not Available
Toxicity Symptoms of overdose include mild depression of the central nervous system and cardiovascular system to profound hypotension, respiratory depression, unconsciousness, and sudden death. Other reported reactions include hyperreflexia, hypertonia, ataxia, athetosis, and extensor-plantar reflexes (Babinski reflex). LD50=55mg/kg (I.V. in mice)
Affected organisms
  • Humans and other mammals
Pathways Not Available
Pharmacoeconomics
Manufacturers
  • Wyeth ayerst laboratories
  • Abbott laboratories pharmaceutical products div
  • Akorn inc
  • Baxter healthcare corp anesthesia and critical care
  • Bedford laboratories
  • Bioniche pharma usa llc
  • Hikma farmaceutica (portugal) sa
  • Hospira inc
  • Marsam pharmaceuticals llc
  • Pharmaforce inc
  • Sandoz inc
  • Teva parenteral medicines inc
  • Watson laboratories inc
  • Wockhardt ltd
  • Altana inc
  • Victory pharma inc
  • Polymedica industries inc
  • Able laboratories inc
  • G and w laboratories inc
  • Paddock laboratories inc
  • Perrigo new york inc
  • Taro pharmaceuticals usa inc
  • Usl pharma inc
  • Alpharma us pharmaceuticals division
  • Actavis mid atlantic llc
  • Amneal pharmaceuticals
  • Hi tech pharmacal co inc
  • Kv pharmaceutical co
  • Pharmaceutical assoc inc div beach products
  • Sun pharmaceutical industries inc
  • Vintage pharmaceuticals llc
  • Whiteworth towne paulsen inc
  • Ani pharmaceuticals inc
  • Wockhardt eu operations (swiss) ag
  • Wyeth pharmaceuticals inc
  • Actavis totowa llc
  • Impax laboratories inc
  • Ivax pharmaceuticals inc sub teva pharmaceuticals usa
  • Kvk tech inc
  • Lannett co inc
  • Mutual pharmaceutical co inc
  • Private formulations inc
  • Tablicaps inc
  • Teva pharmaceuticals usa inc
  • Vintage pharmaceuticals inc
  • Zydus pharmaceuticals usa inc
  • Bristol myers squibb pharma co
Packagers
Dosage forms
Form Route Strength
Cream Topical
Liquid Intramuscular
Solution Intravenous
Syrup Oral
Tablet Oral
Prices
Unit description Cost Unit
Promethegan 12 50 mg Suppository Box 101.64 USD box
Phenergan 12 50 mg Suppository Box 80.16 USD box
Phenergan 12 25 mg Suppository Box 62.59 USD box
Promethegan 12 25 mg Suppository Box 62.27 USD box
Promethazine HCl 12 50 mg Suppository Box 60.94 USD box
Phenergan 12 12.5 mg Suppository Box 54.58 USD box
Phenergan 25 mg suppository 8.32 USD suppository
Promethegan 50 mg suppository 8.14 USD suppository
Phenergan 12.5 mg suppository 7.94 USD suppository
Phenergan 50 mg suppository 7.39 USD suppository
Promethazine 50 mg suppository 4.88 USD suppository
Promethegan 25 mg suppository 4.62 USD suppository
Phenadoz 25 mg suppository 4.45 USD suppository
Promethazine 25 mg suppository 4.32 USD suppository
Promethegan 12.5 mg suppository 4.02 USD suppository
Promethazine HCl 12.5 mg Suppository 4.0 USD suppository
Phenadoz 12.5 mg suppository 3.89 USD suppository
Phenergan 25 mg/ml ampul 3.84 USD ml
Promethazine 12.5 mg suppository 3.82 USD suppository
Phenergan 50 mg/ml ampul 3.68 USD ml
Promethazine HCl 50 mg/ml Solution 1ml Ampule 2.8 USD ampule
Promethazine 50 mg/ml ampul 2.25 USD ml
Promethazine hcl powder 2.14 USD g
Promethazine 25 mg/ml ampul 1.1 USD ml
Promethazine 25 mg/ml 1.06 USD ml
Promethazine HCl 50 mg tablet 0.81 USD tablet
Promethazine 50 mg tablet 0.78 USD tablet
Promethazine HCl 25 mg tablet 0.73 USD tablet
Phenergan 25 mg tablet 0.62 USD tablet
Promethazine 25 mg tablet 0.51 USD tablet
Promethazine 12.5 mg tablet 0.49 USD tablet
Promethazine-DM 6.25-15 mg/5ml Syrup 0.18 USD ml
Promethazine HCl 6.25 mg/5ml Syrup 0.11 USD ml
Promethazine VC Plain 6.25-5 mg/5ml Syrup 0.09 USD ml
Promethazine-Codeine 6.25-10 mg/5ml Syrup 0.06 USD ml
Patents Not Available
Properties
State solid
Melting point 60oC
Experimental Properties
Property Value Source
water solubility Freely soluble PhysProp
logP 4.4 PhysProp
logS -4.26 [ADME Research, USCD] PhysProp
Predicted Properties
Property Value Source
water solubility 2.45e-02 g/l ALOGPS
logP 4.52 ALOGPS
logP 4.29 ChemAxon Molconvert
logS -4.07 ALOGPS
pKa ChemAxon Molconvert
hydrogen acceptor count 2 ChemAxon Molconvert
hydrogen donor count 0 ChemAxon Molconvert
polar surface area 6.48 ChemAxon Molconvert
rotatable bond count 3 ChemAxon Molconvert
refractivity 88.50 ChemAxon Molconvert
polarizability 32.38 ChemAxon Molconvert
References
Synthesis Reference Not Available
General Reference
  1. Peters RJ Jr, Kelder SH, Markham CM, Yacoubian GS Jr, Peters LA, Ellis A: Beliefs and social norms about codeine and promethazine hydrochloride cough syrup (CPHCS) onset and perceived addiction among urban Houstonian adolescents: an addiction trend in the city of lean. J Drug Educ. 2003;33(4):415-25. Pubmed
External Links
Resource Link
KEGG Drug D00494 Link_out
KEGG Compound C07404 Link_out
PubChem Compound 4927 Link_out
PubChem Substance 46507798 Link_out
ChemSpider 4758 Link_out
ChEBI 8461 Link_out
ChEMBL 8461 Link_out
Therapeutic Targets Database DAP000334 Link_out
Drug Product Database 583979 Link_out
RxList http://www.rxlist.com/cgi/generic3/phenergan.htm Link_out
Drugs.com http://www.drugs.com/promethazine.html Link_out
Wikipedia http://en.wikipedia.org/wiki/Promethazine Link_out
ATC Codes
  • D04AA10
  • R06AD02
  • R06AD05
AHFS Codes
  • 04:04.12
PDB Entries Not Available
FDA label show (93.4 KB)
MSDS show (74.8 KB)
Interactions
Drug Interactions Not Available
Food Interactions
  • Take with food to reduce irritation. Avoid alcohol.
Targets

1. Histamine H1 receptor

Pharmacological action: yes
Actions: antagonist

In peripheral tissues, the H1 subclass of histamine receptors mediates the contraction of smooth muscles, increase in capillary permeability due to contraction of terminal venules, and catecholamine release from adrenal medulla, as well as mediating neurotransmission in the central nervous system

Organism class: human
UniProt ID: P35367 Link_out
Gene: HRH1 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed
  2. Suzuki A, Yasui-Furukori N, Mihara K, Kondo T, Furukori H, Inoue Y, Kaneko S, Otani K: Histamine H1-receptor antagonists, promethazine and homochlorcyclizine, increase the steady-state plasma concentrations of haloperidol and reduced haloperidol. Ther Drug Monit. 2003 Apr;25(2):192-6. Pubmed
  3. Smith BN, Armstrong WE: Histamine enhances the depolarizing afterpotential of immunohistochemically identified vasopressin neurons in the rat supraoptic nucleus via H1-receptor activation. Neuroscience. 1993 Apr;53(3):855-64. Pubmed
  4. Miller RA, Tu AT: Factors in snake venoms that increase capillary permeability. J Pharm Pharmacol. 1989 Nov;41(11):792-4. Pubmed
  5. Claro E, Arbones L, Garcia A, Picatoste F: Phosphoinositide hydrolysis mediated by histamine H1-receptors in rat brain cortex. Eur J Pharmacol. 1986 Apr 16;123(2):187-96. Pubmed
  6. Ikeda H, Kubo N, Nakamura A, Harada N, Minamino M, Yamashita T: Histamine-induced calcium released from cultured human mucosal microvascular endothelial cells from nasal inferior turbinate. Acta Otolaryngol. 1997 Nov;117(6):864-70. Pubmed
  7. Paton DM, Webster DR: Clinical pharmacokinetics of H1-receptor antagonists (the antihistamines). Clin Pharmacokinet. 1985 Nov-Dec;10(6):477-97. Pubmed

2. D(2) dopamine receptor

Pharmacological action: unknown
Actions: antagonist

This is one of the five types (D1 to D5) of receptors for dopamine. The activity of this receptor is mediated by G proteins which inhibit adenylyl cyclase

Organism class: human
UniProt ID: P14416 Link_out
Gene: DRD2 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Golembiewski JA, O’Brien D: A systematic approach to the management of postoperative nausea and vomiting. J Perianesth Nurs. 2002 Dec;17(6):364-76. Pubmed

3. Muscarinic acetylcholine receptor M1

Pharmacological action: unknown
Actions: antagonist

The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is Pi turnover

Organism class: human
UniProt ID: P11229 Link_out
Gene: CHRM1 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Golembiewski JA, O’Brien D: A systematic approach to the management of postoperative nausea and vomiting. J Perianesth Nurs. 2002 Dec;17(6):364-76. Pubmed

4. Muscarinic acetylcholine receptor M2

Pharmacological action: unknown
Actions: antagonist

The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is adenylate cyclase inhibition

Organism class: human
UniProt ID: P08172 Link_out
Gene: CHRM2 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Golembiewski JA, O’Brien D: A systematic approach to the management of postoperative nausea and vomiting. J Perianesth Nurs. 2002 Dec;17(6):364-76. Pubmed

5. Muscarinic acetylcholine receptor M3

Pharmacological action: unknown
Actions: antagonist

The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is Pi turnover

Organism class: human
UniProt ID: P20309 Link_out
Gene: CHRM3 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Golembiewski JA, O’Brien D: A systematic approach to the management of postoperative nausea and vomiting. J Perianesth Nurs. 2002 Dec;17(6):364-76. Pubmed

6. Muscarinic acetylcholine receptor M4

Pharmacological action: unknown
Actions: antagonist

The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is inhibition of adenylate cyclase

Organism class: human
UniProt ID: P08173 Link_out
Gene: CHRM4 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Golembiewski JA, O’Brien D: A systematic approach to the management of postoperative nausea and vomiting. J Perianesth Nurs. 2002 Dec;17(6):364-76. Pubmed

7. Muscarinic acetylcholine receptor M5

Pharmacological action: unknown
Actions: antagonist

The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is Pi turnover

Organism class: human
UniProt ID: P08912 Link_out
Gene: CHRM5 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Golembiewski JA, O’Brien D: A systematic approach to the management of postoperative nausea and vomiting. J Perianesth Nurs. 2002 Dec;17(6):364-76. Pubmed

8. Alpha-1A adrenergic receptor

Pharmacological action: unknown
Actions: unknown

This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol- calcium second messenger system. Its effect is mediated by G(q) and G(11) proteins

Organism class: human
UniProt ID: P35348 Link_out
Gene: ADRA1A Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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. 5-hydroxytryptamine 2A receptor

Pharmacological action: unknown
Actions: antagonist

This is one of the several different receptors for 5- hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. This receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. This receptor is involved in tracheal smooth muscle contraction, bronchoconstriction, and control of aldosterone production

Organism class: human
UniProt ID: P28223 Link_out
Gene: HTR2A Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Bileviciute I, Stenfors C, Theodorsson E, Lundeberg T: Unilateral injection of calcitonin gene-related peptide (CGRP) induces bilateral oedema formation and release of CGRP-like immunoreactivity in the rat hindpaw. Br J Pharmacol. 1998 Nov;125(6):1304-12. Pubmed
  2. Kelley BM, Porter JH: The role of muscarinic cholinergic receptors in the discriminative stimulus properties of clozapine in rats. Pharmacol Biochem Behav. 1997 Aug;57(4):707-19. Pubmed
  3. Hoenicke EM, Vanecek SA, Woods JH: The discriminative stimulus effects of clozapine in pigeons: involvement of 5-hydroxytryptamine1C and 5-hydroxytryptamine2 receptors. J Pharmacol Exp Ther. 1992 Oct;263(1):276-84. Pubmed
  4. Martinez F, Coleman JW: A comparison of the effects of chlorpromazine and more selective histamine and 5-hydroxytryptamine antagonists on human IgG synthesis in vitro. Int J Immunopharmacol. 1990;12(2):185-91. Pubmed
  5. Fiorella D, Rabin RA, Winter JC: The role of the 5-HT2A and 5-HT2C receptors in the stimulus effects of hallucinogenic drugs. I: Antagonist correlation analysis. Psychopharmacology (Berl). 1995 Oct;121(3):347-56. Pubmed

10. Calmodulin

Pharmacological action: unknown
Actions: inhibitor

Calmodulin mediates the control of a large number of enzymes and other proteins by Ca(2+). Among the enzymes to be stimulated by the calmodulin-Ca(2+) complex are a number of protein kinases and phosphatases

Organism class: human
UniProt ID: P62158 Link_out
Gene: CALM1 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Cohen ME, Sharp GW, Donowitz M: Suggestion of a role for calmodulin and phosphorylation in regulation of rabbit ileal electrolyte transport: effects of promethazine. Am J Physiol. 1986 Nov;251(5 Pt 1):G710-7. Pubmed
  2. Scott JA, Khaw BA, Fallon JT, Locke E, Rabito CA, Peto CA, Homcy CJ: The effect of phenothiazines upon maintenance of membrane integrity in the cultured myocardial cell. J Mol Cell Cardiol. 1986 Dec;18(12):1243-54. Pubmed
  3. Lohr KM, Feix JB, Kurth C: Chlorpromazine inhibits neutrophil chemotaxis beyond the chemotactic receptor-ligand interaction. J Infect Dis. 1984 Nov;150(5):643-52. Pubmed
  4. DiPaola M, Keith CH, Feldman D, Tycko B, Maxfield FR: Loss of alpha 2-macroglobulin and epidermal growth factor surface binding induced by phenothiazines and naphthalene sulfonamides. J Cell Physiol. 1984 Feb;118(2):193-202. Pubmed
  5. Luchowski EM, Yousif F, Triggle DJ, Maurer SC, Sarmiento JG, Janis RA: Effects of metal cations and calmodulin antagonists on [3H] nitrendipine binding in smooth and cardiac muscle. J Pharmacol Exp Ther. 1984 Sep;230(3):607-13. Pubmed

Enzymes

1. Cytochrome P450 2D6

Actions: substrate, inhibitor

Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants

UniProt ID: P10635 Link_out
Gene: CYP2D6 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed
  3. Platts SH, Shi SJ, Meck JV: Akathisia with combined use of midodrine and promethazine. JAMA. 2006 May 3;295(17):2000-1. Pubmed

2. Cytochrome P450 2B6

Actions: substrate

Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics

UniProt ID: P20813 Link_out
Gene: CYP2B6 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

3. Cytochrome P450 2C9

Actions: inhibitor

Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S- warfarin, diclofenac, phenytoin, tolbutamide and losartan

UniProt ID: P11712 Link_out
Gene: CYP2C9
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

Transporters

1. Multidrug resistance protein 1

Actions: inhibitor

Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells

UniProt ID: P08183 Link_out
Gene: ABCB1 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Ibrahim S, Peggins J, Knapton A, Licht T, Aszalos A: Influence of antipsychotic, antiemetic, and Ca(2+) channel blocker drugs on the cellular accumulation of the anticancer drug daunorubicin: P-glycoprotein modulation. J Pharmacol Exp Ther. 2000 Dec;295(3):1276-83. Pubmed

Comments
Drug created on June 13, 2005 07:24 / Updated on December 02, 2010 16:28

This project is supported by Genome Alberta & Genome Canada, a not-for-profit organization that is leading Canada's national genomics strategy with $600 million in funding from the federal government. This project is also supported in part by GenomeQuest, Inc., an enterprise genomic information company serving the life science community.