Methyltestosterone
Identification
- Summary
Methyltestosterone is a synthetic anabolic steroid used for the replacement therapy in conditions associated with testosterone deficiencies in males, such as hypogonadism, and treatment of advancing inoperable metastatic breast cancer in females.
- Brand Names
- Covaryx, Methitest
- Generic Name
- Methyltestosterone
- DrugBank Accession Number
- DB06710
- Background
A synthetic anabolic steroid used for treating men with testosterone deficiency or similar androgen replacement therapies. Also, has antineoplastic properties and so has been used secondarily in women with advanced breast cancer. Methyltestosterone is a schedule III drug in the US.
- Type
- Small Molecule
- Groups
- Approved
- Structure
- Weight
- Average: 302.451
Monoisotopic: 302.224580204 - Chemical Formula
- C20H30O2
- Synonyms
- 17-beta-Hydroxy-17-methylandrost-4-en-3-one
- 17-methyltestosterone
- 17alpha-Methyl-3-oxo-4-androsten-17beta-ol
- 17alpha-Methyltestosterone
- 17beta-Hydroxy-17-methylandrost-4-en-3-one
- 17α-methyl-Δ4-androsten-17β-ol-3-one
- 17α-methyltestosterone
- 4-Androstene-17alpha-methyl-17beta-ol-3-one
- Methyltestosterone
- Methyltestosteronum
- Metiltestosterona
- External IDs
- L 589.372
- NSC-139965
- RU 24400
Pharmacology
- Indication
Methyltestosterone is an anabolic steroid hormone used to treat men with a testosterone deficiency. It is also used in women to treat breast cancer, breast pain, swelling due to pregnancy, and with the addition of estrogen it can treat symptoms of menopause.
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Management of Delayed puberty •••••••••••• Management of Hypogonadotropic hypogonadism •••••••••••• Treatment of Metastatic breast cancer •••••••••••• •••••••••••••• Treatment of Primary hypogonadism •••••••••••• Used in combination to treat Testosterone deficiency Combination Product in combination with: alpha-Tocopherol acetate (DB14003) •••••••••••• ••••••• ••••••• •••••• - Contraindications & Blackbox Warnings
- Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API
- Pharmacodynamics
Testosterone is a steroid hormone from the androgen group. Testosterone is primarily secreted from the testes of males. In females, it is produced in the ovaries, adrenal glands and by conversion of adrostenedione in the periphery. It is the principal male sex hormone and an anabolic steroid. In both males and females, it plays key roles in health and well-being. Examples include enhanced libido, energy, immune function, and protection against osteoporosis. On average, the adult male body produces about twenty times the amount of testosterone than an adult female's body does.
- Mechanism of action
The effects of testosterone in humans and other vertebrates occur by way of two main mechanisms: by activation of the androgen receptor (directly or as DHT), and by conversion to estradiol and activation of certain estrogen receptors. Free testosterone (T) is transported into the cytoplasm of target tissue cells, where it can bind to the androgen receptor, or can be reduced to 5α-dihydrotestosterone (DHT) by the cytoplasmic enzyme 5α-reductase. DHT binds to the same androgen receptor even more strongly than T, so that its androgenic potency is about 2.5 times that of T. The T-receptor or DHT-receptor complex undergoes a structural change that allows it to move into the cell nucleus and bind directly to specific nucleotide sequences of the chromosomal DNA. The areas of binding are called hormone response elements (HREs), and influence transcriptional activity of certain genes, producing the androgen effects.
Target Actions Organism AAndrogen receptor agonistHumans UEstrogen receptor alpha Not Available Humans - Absorption
The methyl group aids to increase oral bioavailability.
- Volume of distribution
Not Available
- Protein binding
40% of testosterone in plasma is bound to sex hormone-binding globulin and 2% remains unbound and the rest is bound to albumin and other proteins.
- Metabolism
Hepatic. Testosterone is metabolized to 17-keto steroids through two different pathways. The major active metabolites are estradiol and dihydrotestosterone (DHT).
- Route of elimination
90% urine / 10% feces
- Half-life
6-8 hours
- Clearance
Not Available
- Adverse Effects
- Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.
- Toxicity
Side effects include amnesia, anxiety, discolored hair, dizziness, dry skin, hirsutism, hostility, impaired urination, paresthesia, penis disorder, peripheral edema, sweating, and vasodilation.
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAbacavir Abacavir may decrease the excretion rate of Methyltestosterone which could result in a higher serum level. Abametapir The serum concentration of Methyltestosterone can be increased when it is combined with Abametapir. Abatacept The metabolism of Methyltestosterone can be increased when combined with Abatacept. Acamprosate The excretion of Acamprosate can be increased when combined with Methyltestosterone. Acarbose Methyltestosterone may increase the hypoglycemic activities of Acarbose. - Food Interactions
- No interactions found.
Products
- Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.
- Product Images
- International/Other Brands
- Testred / Virilon
- Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Android Capsule 10 mg/1 Oral Valeant Pharmaceuticals North America 1973-12-03 2018-04-30 US Methitest Tablet 10 mg/1 Oral Amneal Pharmaceuticals of New York Llc 1974-10-17 Not applicable US MethylTESTOSTERone Capsule 10 mg/1 Oral Amneal Pharmaceuticals of New York Llc 2015-09-21 Not applicable US Methyltestosterone Capsule 10 mg/1 Oral Novitium Pharma Llc 2022-02-18 Not applicable US Testred C-III Capsule 10 mg/1 Oral Valeant Pharmaceuticals North America 1973-12-03 2018-04-30 US - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image ยาผสมฮอร์โมนชาย ที.พี Methyltestosterone (10 MG) + Vitamin E (10 MG) Tablet, sugar coated Oral บริษัท ที.พี.ดรัก แลบบอราทอรี่ส์ (1969) จำกัด 2008-10-27 Not applicable Thailand เทสโทฮอฟ Methyltestosterone (5 MG) + Vitamin E (3 MG) Tablet, coated Oral บริษัท โรงงานเภสัชอุตสาหกรรม เจเอสพี (ประเทศไทย) จำกัด (มหาชน) 2017-08-09 2020-09-29 Thailand - Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Covaryx Methyltestosterone (2.5 mg/1) + Esterified estrogens (1.25 mg/1) Tablet, coated Oral CENTRIX PHARMACEUTICAL, INC, 2007-04-01 Not applicable US Covaryx Hs Methyltestosterone (1.25 mg/1) + Esterified estrogens (0.625 mg/1) Tablet, coated Oral CENTRIX PHARMACEUTICAL, INC, 2007-04-01 Not applicable US Eemt Methyltestosterone (2.5 mg/1) + Esterified estrogens (1.25 mg/1) Tablet, coated Oral CREEKWOOD PHARMACEUTICAL, INC, 2011-09-01 Not applicable US Eemt D.S. Methyltestosterone (1.25 mg/1) + Estrone sodium sulfate (0.625 mg/1) Tablet, coated Oral Breckenridge Pharmaceutical, Inc. 2003-11-01 2012-01-31 US Eemt H.S. Methyltestosterone (1.25 mg/1) + Esterified estrogens (0.625 mg/1) Tablet, coated Oral Physicians Total Care, Inc. 2006-06-27 2013-01-15 US
Categories
- ATC Codes
- G03BA02 — Methyltestosterone
- G03BA — 3-oxoandrosten (4) derivatives
- G03B — ANDROGENS
- G03 — SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM
- G — GENITO URINARY SYSTEM AND SEX HORMONES
- G03EA — Androgens and estrogens
- G03E — ANDROGENS AND FEMALE SEX HORMONES IN COMBINATION
- G03 — SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM
- G — GENITO URINARY SYSTEM AND SEX HORMONES
- Drug Categories
- 3-Oxoandrosten (4) Derivatives
- Anabolic Agents
- Androgens
- Androgens and Estrogens
- Androstanes
- Androstenes
- Androstenols
- Antineoplastic Agents
- Antineoplastic Agents, Hormonal
- Cytochrome P-450 CYP2B6 Substrates
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 Substrates
- Drugs that are Mainly Renally Excreted
- Fused-Ring Compounds
- Genito Urinary System and Sex Hormones
- Hormones
- Hormones, Hormone Substitutes, and Hormone Antagonists
- OAT3/SLC22A8 Inducers
- Sex Hormones and Modulators of the Genital System
- Steroids
- Testosterone Congeners
- Thyroxine-binding globulin inhibitors
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as androgens and derivatives. These are 3-hydroxylated C19 steroid hormones. They are known to favor the development of masculine characteristics. They also show profound effects on scalp and body hair in humans.
- Kingdom
- Organic compounds
- Super Class
- Lipids and lipid-like molecules
- Class
- Steroids and steroid derivatives
- Sub Class
- Androstane steroids
- Direct Parent
- Androgens and derivatives
- Alternative Parents
- 3-oxo delta-4-steroids / 17-hydroxysteroids / Delta-4-steroids / Cyclohexenones / Tertiary alcohols / Cyclic alcohols and derivatives / Organic oxides / Hydrocarbon derivatives
- Substituents
- 17-hydroxysteroid / 3-oxo-delta-4-steroid / 3-oxosteroid / Alcohol / Aliphatic homopolycyclic compound / Androgen-skeleton / Carbonyl group / Cyclic alcohol / Cyclic ketone / Cyclohexenone
- Molecular Framework
- Aliphatic homopolycyclic compounds
- External Descriptors
- enone, 3-oxo Delta(4)-steroid, 17beta-hydroxy steroid (CHEBI:27436) / C19 steroids (androgens) and derivatives (C07198) / C19 steroids (androgens) and derivatives (LMST02020029)
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- V9EFU16ZIF
- CAS number
- 58-18-4
- InChI Key
- GCKMFJBGXUYNAG-HLXURNFRSA-N
- InChI
- InChI=1S/C20H30O2/c1-18-9-6-14(21)12-13(18)4-5-15-16(18)7-10-19(2)17(15)8-11-20(19,3)22/h12,15-17,22H,4-11H2,1-3H3/t15-,16+,17+,18+,19+,20+/m1/s1
- IUPAC Name
- (1S,3aS,3bR,9aR,9bS,11aS)-1-hydroxy-1,9a,11a-trimethyl-1H,2H,3H,3aH,3bH,4H,5H,7H,8H,9H,9aH,9bH,10H,11H,11aH-cyclopenta[a]phenanthren-7-one
- SMILES
- [H][C@@]12CC[C@](C)(O)[C@@]1(C)CC[C@@]1([H])[C@@]2([H])CCC2=CC(=O)CC[C@]12C
References
- General References
- Not Available
- External Links
- Human Metabolome Database
- HMDB0015655
- KEGG Drug
- D00408
- KEGG Compound
- C07198
- PubChem Compound
- 6010
- PubChem Substance
- 99443262
- ChemSpider
- 5788
- BindingDB
- 50410531
- 6904
- ChEBI
- 27436
- ChEMBL
- CHEMBL1395
- ZINC
- ZINC000003814422
- PharmGKB
- PA165958383
- Wikipedia
- Methyltestosterone
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 2 Completed Treatment Hot Flushes, Menopause, Postmenopause 1 2 Completed Treatment Menopause 1 2 Recruiting Treatment Castration-Resistant Prostate Carcinoma / Metastatic Prostate Adenocarcinoma / Stage IV Prostate Cancer AJCC v8 1 2 Terminated Treatment Menopause 2 1 Recruiting Supportive Care Hypogonadism / Malignant Urinary System Neoplasm / Urinary System Disorder / Urinary System Neoplasm 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Tablet Oral 25 mg Tablet, coated Oral Tablet Oral Tablet, film coated Oral Tablet Oral 0.005 g Tablet Oral 10 mg / tab Tablet Oral 25 mg / tab Tablet Oral 10 mg/1 Capsule Oral 10 mg/1 Tablet, sugar coated Oral Capsule Oral 10 mg Tablet, coated Oral 10 mg - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 163 °C PhysProp water solubility 33.9 mg/L (at 25 °C) YALKOWSKY,SH & HE,Y (2003) logP 3.36 HANSCH,C ET AL. (1995) - Predicted Properties
Property Value Source Water Solubility 0.0139 mg/mL ALOGPS logP 3.61 ALOGPS logP 3.65 Chemaxon logS -4.3 ALOGPS pKa (Strongest Acidic) 18.52 Chemaxon pKa (Strongest Basic) -0.53 Chemaxon Physiological Charge 0 Chemaxon Hydrogen Acceptor Count 2 Chemaxon Hydrogen Donor Count 1 Chemaxon Polar Surface Area 37.3 Å2 Chemaxon Rotatable Bond Count 0 Chemaxon Refractivity 89.07 m3·mol-1 Chemaxon Polarizability 35.85 Å3 Chemaxon Number of Rings 4 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule Yes Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 1.0 Blood Brain Barrier + 0.9774 Caco-2 permeable + 0.8737 P-glycoprotein substrate Substrate 0.6431 P-glycoprotein inhibitor I Inhibitor 0.5981 P-glycoprotein inhibitor II Non-inhibitor 0.732 Renal organic cation transporter Non-inhibitor 0.757 CYP450 2C9 substrate Non-substrate 0.8075 CYP450 2D6 substrate Non-substrate 0.8604 CYP450 3A4 substrate Substrate 0.7916 CYP450 1A2 substrate Non-inhibitor 0.8619 CYP450 2C9 inhibitor Non-inhibitor 0.8844 CYP450 2D6 inhibitor Non-inhibitor 0.951 CYP450 2C19 inhibitor Non-inhibitor 0.6629 CYP450 3A4 inhibitor Non-inhibitor 0.8713 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.8711 Ames test Non AMES toxic 0.9429 Carcinogenicity Non-carcinogens 0.9361 Biodegradation Not ready biodegradable 0.9494 Rat acute toxicity 2.0516 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.886 hERG inhibition (predictor II) Non-inhibitor 0.7219
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 181.2661164 predictedDarkChem Lite v0.1.0 [M-H]- 181.4418164 predictedDarkChem Lite v0.1.0 [M-H]- 180.8835164 predictedDarkChem Lite v0.1.0 [M-H]- 181.5307164 predictedDarkChem Lite v0.1.0 [M-H]- 171.98305 predictedDeepCCS 1.0 (2019) [M+H]+ 182.1172164 predictedDarkChem Lite v0.1.0 [M+H]+ 181.3277164 predictedDarkChem Lite v0.1.0 [M+H]+ 182.3375164 predictedDarkChem Lite v0.1.0 [M+H]+ 181.9768164 predictedDarkChem Lite v0.1.0 [M+H]+ 174.11662 predictedDeepCCS 1.0 (2019) [M+Na]+ 181.4550164 predictedDarkChem Lite v0.1.0 [M+Na]+ 182.0242164 predictedDarkChem Lite v0.1.0 [M+Na]+ 181.6795164 predictedDarkChem Lite v0.1.0 [M+Na]+ 181.4019164 predictedDarkChem Lite v0.1.0 [M+Na]+ 180.09163 predictedDeepCCS 1.0 (2019)
Targets
![](https://go.drugbank.com/assets/locked/DrugTargets2-682eb846d210ae4bf33ca03febccfb57bb1c61318e699b729e5df4dfab2c5b67.png)
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- Zinc ion binding
- Specific Function
- Steroid hormone receptors are ligand-activated transcription factors that regulate eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. Transcription ...
- Gene Name
- AR
- Uniprot ID
- P10275
- Uniprot Name
- Androgen receptor
- Molecular Weight
- 98987.9 Da
References
- Small EJ, Ryan CJ: The case for secondary hormonal therapies in the chemotherapy age. J Urol. 2006 Dec;176(6 Pt 2):S66-71. [Article]
- Omwancha J, Brown TR: Selective androgen receptor modulators: in pursuit of tissue-selective androgens. Curr Opin Investig Drugs. 2006 Oct;7(10):873-81. [Article]
- Petraki CD, Sfikas CP: Histopathological changes induced by therapies in the benign prostate and prostate adenocarcinoma. Histol Histopathol. 2007 Jan;22(1):107-18. [Article]
- Maudsley S, Davidson L, Pawson AJ, Freestone SH, Lopez de Maturana R, Thomson AA, Millar RP: Gonadotropin-releasing hormone functionally antagonizes testosterone activation of the human androgen receptor in prostate cells through focal adhesion complexes involving Hic-5. Neuroendocrinology. 2006;84(5):285-300. Epub 2007 Jan 4. [Article]
- Lapauw B, Goemaere S, Crabbe P, Kaufman JM, Ruige JB: Is the effect of testosterone on body composition modulated by the androgen receptor gene CAG repeat polymorphism in elderly men? Eur J Endocrinol. 2007 Mar;156(3):395-401. [Article]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Curator comments
- Interacting drug is a metabolite: Methyltestosterone is aromatized to methylestradiol which binds to estrogen receptors
- General Function
- Zinc ion binding
- Specific Function
- Nuclear hormone receptor. The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissu...
- Gene Name
- ESR1
- Uniprot ID
- P03372
- Uniprot Name
- Estrogen receptor
- Molecular Weight
- 66215.45 Da
References
- Huang R, Sakamuru S, Martin MT, Reif DM, Judson RS, Houck KA, Casey W, Hsieh JH, Shockley KR, Ceger P, Fostel J, Witt KL, Tong W, Rotroff DM, Zhao T, Shinn P, Simeonov A, Dix DJ, Austin CP, Kavlock RJ, Tice RR, Xia M: Profiling of the Tox21 10K compound library for agonists and antagonists of the estrogen receptor alpha signaling pathway. Sci Rep. 2014 Jul 11;4:5664. doi: 10.1038/srep05664. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Steroid hydroxylase activity
- Specific Function
- 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 un...
- Gene Name
- CYP2B6
- Uniprot ID
- P20813
- Uniprot Name
- Cytochrome P450 2B6
- Molecular Weight
- 56277.81 Da
References
- Rendic S: Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Vitamin d3 25-hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
- Gene Name
- CYP3A4
- Uniprot ID
- P08684
- Uniprot Name
- Cytochrome P450 3A4
- Molecular Weight
- 57342.67 Da
References
- Rendic S, Nolteernsting E, Schanzer W: Metabolism of anabolic steroids by recombinant human cytochrome P450 enzymes. Gas chromatographic-mass spectrometric determination of metabolites. J Chromatogr B Biomed Sci Appl. 1999 Nov 26;735(1):73-83. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInducer
- General Function
- Oxygen binding
- Specific Function
- Catalyzes the formation of aromatic C18 estrogens from C19 androgens.
- Gene Name
- CYP19A1
- Uniprot ID
- P11511
- Uniprot Name
- Aromatase
- Molecular Weight
- 57882.48 Da
References
- Tsai CL, Wang LH, Fang LS: Estradiol and para-chlorophenylalanine downregulate the expression of brain aromatase and estrogen receptor-alpha mRNA during the critical period of feminization in tilapia (Oreochromis mossambicus). Neuroendocrinology. 2001 Nov;74(5):325-34. doi: 10.1159/000054699. [Article]
Carriers
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Toxic substance binding
- Specific Function
- Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
- Gene Name
- ALB
- Uniprot ID
- P02768
- Uniprot Name
- Serum albumin
- Molecular Weight
- 69365.94 Da
References
- Pardridge WM: Serum bioavailability of sex steroid hormones. Clin Endocrinol Metab. 1986 May;15(2):259-78. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Androgen binding
- Specific Function
- Functions as an androgen transport protein, but may also be involved in receptor mediated processes. Each dimer binds one molecule of steroid. Specific for 5-alpha-dihydrotestosterone, testosterone...
- Gene Name
- SHBG
- Uniprot ID
- P04278
- Uniprot Name
- Sex hormone-binding globulin
- Molecular Weight
- 43778.755 Da
References
- Pardridge WM: Serum bioavailability of sex steroid hormones. Clin Endocrinol Metab. 1986 May;15(2):259-78. [Article]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- InhibitorInducer
- General Function
- Sodium-independent organic anion transmembrane transporter activity
- Specific Function
- Mediates the Na(+)-independent transport of organic anions such as sulfobromophthalein (BSP) and conjugated (taurocholate) and unconjugated (cholate) bile acids (By similarity). Selectively inhibit...
- Gene Name
- SLCO1A2
- Uniprot ID
- P46721
- Uniprot Name
- Solute carrier organic anion transporter family member 1A2
- Molecular Weight
- 74144.105 Da
References
- 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. [Article]
- Kanai N, Lu R, Bao Y, Wolkoff AW, Vore M, Schuster VL: Estradiol 17 beta-D-glucuronide is a high-affinity substrate for oatp organic anion transporter. Am J Physiol. 1996 Feb;270(2 Pt 2):F326-31. [Article]
- Bossuyt X, Muller M, Hagenbuch B, Meier PJ: Polyspecific drug and steroid clearance by an organic anion transporter of mammalian liver. J Pharmacol Exp Ther. 1996 Mar;276(3):891-6. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inducer
- General Function
- Sodium-independent organic anion transmembrane transporter activity
- Specific Function
- Plays an important role in the excretion/detoxification of endogenous and exogenous organic anions, especially from the brain and kidney. Involved in the transport basolateral of steviol, fexofenad...
- Gene Name
- SLC22A8
- Uniprot ID
- Q8TCC7
- Uniprot Name
- Solute carrier family 22 member 8
- Molecular Weight
- 59855.585 Da
References
- Kobayashi Y, Hirokawa N, Ohshiro N, Sekine T, Sasaki T, Tokuyama S, Endou H, Yamamoto T: Differential gene expression of organic anion transporters in male and female rats. Biochem Biophys Res Commun. 2002 Jan 11;290(1):482-7. [Article]
Drug created at May 16, 2010 15:41 / Updated at February 21, 2021 18:52