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IdentificationPharmacologyInteractionsReferencesTrialsEconomicsPropertiesSpectraTaxonomyAllylestrenol
Identification
- Name
- Allylestrenol
- Accession Number
- DB01431
- Type
- Small Molecule
- Groups
- Approved
- Description
A synthetic steroid with progestational activity. It is widely marketed throughout Europe, including Russia and many other European countries, and is also available in Japan, Hong Kong, India, Bangladesh, Indonesia, and much of Southeast Asia, though notably not in the United States or Canada.
- Structure
Structure for DB01431 (Allylestrenol)
- Synonyms
- 17α-allylestr-4-en-17β-ol
- 3-deketo-17α-allyl-19-nortestosterone
- Allyl estrenol
- Allyloestrenol
- External IDs
- NSC-37723
- International/Other Brands
- Gestanin / Gestanol / Gestanon / Gestin / Gestrenol / Maintaine / Orageston / Perselin / Profar / Turinal
- Categories
- Adrenal Cortex Hormones
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 CYP3A4 Substrates (strength unknown)
- Estranes
- Estren Derivatives
- Estrenes
- Genito Urinary System and Sex Hormones
- Hormones
- Hormones, Hormone Substitutes, and Hormone Antagonists
- Progestins
- Sex Hormones and Modulators of the Genital System
- Steroids
- UNII
- I47VB5DZ8O
- CAS number
- 432-60-0
- Weight
- Average: 300.4782
Monoisotopic: 300.245315646 - Chemical Formula
- C21H32O
- InChI Key
- ATXHVCQZZJYMCF-XUDSTZEESA-N
- InChI
- InChI=1S/C21H32O/c1-3-12-21(22)14-11-19-18-9-8-15-6-4-5-7-16(15)17(18)10-13-20(19,21)2/h3,6,16-19,22H,1,4-5,7-14H2,2H3/t16-,17+,18+,19-,20-,21-/m0/s1
- IUPAC Name
- (1S,2R,10R,11S,14R,15S)-15-methyl-14-(prop-2-en-1-yl)tetracyclo[8.7.0.0²,⁷.0¹¹,¹⁵]heptadec-6-en-14-ol
- SMILES
- [H][C@@]12CC[C@@](O)(CC=C)[C@@]1(C)CC[C@]1([H])[C@@]3([H])CCCC=C3CC[C@@]21[H]
Pharmacology
- Indication
Allylestrenol was designed to be used for miscarriage prevention, prevention of premature labour and has been investigated for possible use in men for treatment for benign prostatic hyperplasia.
- Pharmacodynamics
Allylestrenol is a progestogen structurally related to progesterone that has been given in threatened and recurrent miscarriage, and to prevent premature labour. However, with the exception of proven progesterone deficiency, such use is no longer recommended. In threatened miscarriage in progesterone-deficient women a suggested dose is 5 mg three times daily by mouth for 5 to 7 days.
- Mechanism of action
Allylestrenol is similar in structure and function to progesterone. Progesterone shares the pharmacological actions of the progestins. Progesterone binds to the progesterone and estrogen receptors. Target cells include the female reproductive tract, the mammary gland, the hypothalamus, and the pituitary. Once bound to the receptor, progestins like Progesterone will slow the frequency of release of gonadotropin releasing hormone (GnRH) from the hypothalamus and blunt the pre-ovulatory LH (luteinizing hormone) surge. In women who have adequate endogenous estrogen, progesterone transforms a proliferative endometrium into a secretory one. Progesterone is essential for the development of decidual tissue and is necessary to increase endometrial receptivity for implantation of an embryo. Once an embryo has been implanted, progesterone acts to maintain the pregnancy. Progesterone also stimulates the growth of mammary alveolar tissue and relaxes uterine smooth muscle. It has little estrogenic and androgenic activity.
Target Actions Organism AProgesterone receptor agonistHuman UEstrogen receptor alpha agonistHuman - Absorption
- Not Available
- Volume of distribution
- Not Available
- Protein binding
- Not Available
- Metabolism
- Not Available
- Route of elimination
The glucuronide and sulfate conjugates of pregnanediol and pregnanolone are excreted in the urine and bile. Progesterone metabolites which are excreted in the bile may undergo enterohepatic recycling or may be excreted in the feces. Progesterone metabolites are excreted mainly by the kidneys.
- Half life
- Not Available
- Clearance
- Not Available
- Toxicity
- Not Available
- Affected organisms
- Not Available
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
Drug Interaction Drug group Abciximab The therapeutic efficacy of Abciximab can be decreased when used in combination with Allylestrenol. Approved Acenocoumarol The therapeutic efficacy of Acenocoumarol can be decreased when used in combination with Allylestrenol. Approved, Investigational Acetyl sulfisoxazole The metabolism of Allylestrenol can be decreased when combined with Acetyl sulfisoxazole. Approved, Vet Approved Amiodarone The metabolism of Allylestrenol can be decreased when combined with Amiodarone. Approved, Investigational Ancrod The therapeutic efficacy of Ancrod can be decreased when used in combination with Allylestrenol. Approved, Investigational Antithrombin III human The therapeutic efficacy of Antithrombin III human can be decreased when used in combination with Allylestrenol. Approved Apalutamide The serum concentration of Allylestrenol can be decreased when it is combined with Apalutamide. Approved, Investigational Apixaban The therapeutic efficacy of Apixaban can be decreased when used in combination with Allylestrenol. Approved Aprepitant The serum concentration of Allylestrenol can be increased when it is combined with Aprepitant. Approved, Investigational Ardeparin The therapeutic efficacy of Ardeparin can be decreased when used in combination with Allylestrenol. Approved, Investigational, Withdrawn Argatroban The therapeutic efficacy of Argatroban can be decreased when used in combination with Allylestrenol. Approved, Investigational Atazanavir The metabolism of Allylestrenol can be decreased when combined with Atazanavir. Approved, Investigational Atomoxetine The metabolism of Allylestrenol can be decreased when combined with Atomoxetine. Approved Becaplermin The therapeutic efficacy of Becaplermin can be decreased when used in combination with Allylestrenol. Approved, Investigational Bivalirudin The therapeutic efficacy of Bivalirudin can be decreased when used in combination with Allylestrenol. Approved, Investigational Boceprevir The metabolism of Allylestrenol can be decreased when combined with Boceprevir. Approved, Withdrawn Bortezomib The metabolism of Allylestrenol can be decreased when combined with Bortezomib. Approved, Investigational Bosentan The serum concentration of Allylestrenol can be decreased when it is combined with Bosentan. Approved, Investigational Carbamazepine The metabolism of Allylestrenol can be increased when combined with Carbamazepine. Approved, Investigational Ceritinib The serum concentration of Allylestrenol can be increased when it is combined with Ceritinib. Approved Certoparin The therapeutic efficacy of Certoparin can be decreased when used in combination with Allylestrenol. Approved, Investigational Clarithromycin The metabolism of Allylestrenol can be decreased when combined with Clarithromycin. Approved Clotrimazole The metabolism of Allylestrenol can be decreased when combined with Clotrimazole. Approved, Vet Approved Cobicistat The metabolism of Allylestrenol can be decreased when combined with Cobicistat. Approved Conestat alfa Allylestrenol may increase the thrombogenic activities of Conestat alfa. Approved, Investigational Conivaptan The serum concentration of Conivaptan can be increased when it is combined with Allylestrenol. Approved, Investigational Crizotinib The metabolism of Allylestrenol can be decreased when combined with Crizotinib. Approved Curcumin The metabolism of Allylestrenol can be decreased when combined with Curcumin. Approved, Investigational Cyclosporine The metabolism of Allylestrenol can be decreased when combined with Cyclosporine. Approved, Investigational, Vet Approved Dabigatran etexilate The therapeutic efficacy of Dabigatran etexilate can be decreased when used in combination with Allylestrenol. Approved Dabrafenib The serum concentration of Allylestrenol can be decreased when it is combined with Dabrafenib. Approved, Investigational Dalteparin The therapeutic efficacy of Dalteparin can be decreased when used in combination with Allylestrenol. Approved Danaparoid The therapeutic efficacy of Danaparoid can be decreased when used in combination with Allylestrenol. Approved, Withdrawn Darexaban The therapeutic efficacy of Darexaban can be decreased when used in combination with Allylestrenol. Investigational Darunavir The metabolism of Allylestrenol can be decreased when combined with Darunavir. Approved Dasatinib The serum concentration of Allylestrenol can be increased when it is combined with Dasatinib. Approved, Investigational Deferasirox The serum concentration of Allylestrenol can be decreased when it is combined with Deferasirox. Approved, Investigational Delavirdine The metabolism of Allylestrenol can be decreased when combined with Delavirdine. Approved Desirudin The therapeutic efficacy of Desirudin can be decreased when used in combination with Allylestrenol. Approved Dexamethasone The serum concentration of Allylestrenol can be decreased when it is combined with Dexamethasone. Approved, Investigational, Vet Approved Dextran The therapeutic efficacy of Dextran can be decreased when used in combination with Allylestrenol. Approved, Investigational, Vet Approved Dicoumarol The therapeutic efficacy of Dicoumarol can be decreased when used in combination with Allylestrenol. Approved Dihydroergotamine The metabolism of Allylestrenol can be decreased when combined with Dihydroergotamine. Approved, Investigational Diltiazem The metabolism of Allylestrenol can be decreased when combined with Diltiazem. Approved, Investigational Doxycycline The metabolism of Allylestrenol can be decreased when combined with Doxycycline. Approved, Investigational, Vet Approved Dronedarone The metabolism of Allylestrenol can be decreased when combined with Dronedarone. Approved Edetic Acid The therapeutic efficacy of Edetic Acid can be decreased when used in combination with Allylestrenol. Approved, Vet Approved Edoxaban The therapeutic efficacy of Edoxaban can be decreased when used in combination with Allylestrenol. Approved Enoxaparin The therapeutic efficacy of Enoxaparin can be decreased when used in combination with Allylestrenol. Approved Enzalutamide The serum concentration of Allylestrenol can be decreased when it is combined with Enzalutamide. Approved Erythromycin The metabolism of Allylestrenol can be decreased when combined with Erythromycin. Approved, Investigational, Vet Approved Ethyl biscoumacetate The therapeutic efficacy of Ethyl biscoumacetate can be decreased when used in combination with Allylestrenol. Withdrawn Ferulic acid The therapeutic efficacy of Ferulic acid can be decreased when used in combination with Allylestrenol. Experimental Fluconazole The metabolism of Allylestrenol can be decreased when combined with Fluconazole. Approved, Investigational Fluindione The therapeutic efficacy of Fluindione can be decreased when used in combination with Allylestrenol. Approved, Investigational Fluvoxamine The metabolism of Allylestrenol can be decreased when combined with Fluvoxamine. Approved, Investigational Fondaparinux The therapeutic efficacy of Fondaparinux sodium can be decreased when used in combination with Allylestrenol. Approved, Investigational Fosamprenavir The metabolism of Allylestrenol can be decreased when combined with Fosamprenavir. Approved Fosaprepitant The serum concentration of Allylestrenol can be increased when it is combined with Fosaprepitant. Approved Fosphenytoin The metabolism of Allylestrenol can be increased when combined with Fosphenytoin. Approved, Investigational Fusidic Acid The serum concentration of Allylestrenol can be increased when it is combined with Fusidic Acid. Approved, Investigational Gabexate The therapeutic efficacy of Gabexate can be decreased when used in combination with Allylestrenol. Investigational Heparin The therapeutic efficacy of Heparin can be decreased when used in combination with Allylestrenol. Approved, Investigational Human C1-esterase inhibitor Allylestrenol may increase the thrombogenic activities of Human C1-esterase inhibitor. Approved Idelalisib The metabolism of Allylestrenol can be decreased when combined with Idelalisib. Approved Idraparinux The therapeutic efficacy of Idraparinux can be decreased when used in combination with Allylestrenol. Investigational Imatinib The metabolism of Allylestrenol can be decreased when combined with Imatinib. Approved Indinavir The metabolism of Allylestrenol can be decreased when combined with Indinavir. Approved Isavuconazole The serum concentration of Allylestrenol can be increased when it is combined with Isavuconazole. Approved, Investigational Isavuconazonium The metabolism of Allylestrenol can be decreased when combined with Isavuconazonium. Approved, Investigational Itraconazole The metabolism of Allylestrenol can be decreased when combined with Itraconazole. Approved, Investigational Ivacaftor The serum concentration of Allylestrenol can be increased when it is combined with Ivacaftor. Approved Ketoconazole The metabolism of Allylestrenol can be decreased when combined with Ketoconazole. Approved, Investigational Lepirudin The therapeutic efficacy of Lepirudin can be decreased when used in combination with Allylestrenol. Approved Letaxaban The therapeutic efficacy of Letaxaban can be decreased when used in combination with Allylestrenol. Investigational Lopinavir The metabolism of Allylestrenol can be decreased when combined with Lopinavir. Approved Lorpiprazole The serum concentration of Allylestrenol can be increased when it is combined with Lorpiprazole. Approved Lovastatin The metabolism of Allylestrenol can be decreased when combined with Lovastatin. Approved, Investigational Luliconazole The serum concentration of Allylestrenol can be increased when it is combined with Luliconazole. Approved Lumacaftor The metabolism of Allylestrenol can be increased when combined with Lumacaftor. Approved Melagatran The therapeutic efficacy of Melagatran can be decreased when used in combination with Allylestrenol. Experimental Mibefradil The metabolism of Allylestrenol can be decreased when combined with Mibefradil. Investigational, Withdrawn Miconazole The metabolism of Allylestrenol can be decreased when combined with Miconazole. Approved, Investigational, Vet Approved Mifepristone The serum concentration of Allylestrenol can be increased when it is combined with Mifepristone. Approved, Investigational Mitotane The serum concentration of Allylestrenol can be decreased when it is combined with Mitotane. Approved Nadroparin The therapeutic efficacy of Nadroparin can be decreased when used in combination with Allylestrenol. Approved, Investigational Nafamostat The therapeutic efficacy of Nafamostat can be decreased when used in combination with Allylestrenol. Approved, Investigational Nefazodone The metabolism of Allylestrenol can be decreased when combined with Nefazodone. Approved, Withdrawn Nelfinavir The metabolism of Allylestrenol can be decreased when combined with Nelfinavir. Approved Netupitant The serum concentration of Allylestrenol can be increased when it is combined with Netupitant. Approved, Investigational Nevirapine The metabolism of Allylestrenol can be increased when combined with Nevirapine. Approved Nicardipine The metabolism of Allylestrenol can be decreased when combined with Nicardipine. Approved, Investigational Nilotinib The metabolism of Allylestrenol can be decreased when combined with Nilotinib. Approved, Investigational Olaparib The metabolism of Allylestrenol can be decreased when combined with Olaparib. Approved Osimertinib The serum concentration of Allylestrenol can be increased when it is combined with Osimertinib. Approved Otamixaban The therapeutic efficacy of Otamixaban can be decreased when used in combination with Allylestrenol. Investigational Palbociclib The serum concentration of Allylestrenol can be increased when it is combined with Palbociclib. Approved, Investigational Pentaerythritol Tetranitrate The therapeutic efficacy of Pentaerythritol Tetranitrate can be decreased when used in combination with Allylestrenol. Approved Pentobarbital The metabolism of Allylestrenol can be increased when combined with Pentobarbital. Approved, Investigational, Vet Approved Pentosan Polysulfate The therapeutic efficacy of Pentosan Polysulfate can be decreased when used in combination with Allylestrenol. Approved Phenindione The therapeutic efficacy of Phenindione can be decreased when used in combination with Allylestrenol. Approved, Investigational Phenobarbital The metabolism of Allylestrenol can be increased when combined with Phenobarbital. Approved, Investigational Phenprocoumon The therapeutic efficacy of Phenprocoumon can be decreased when used in combination with Allylestrenol. Approved, Investigational Phenytoin The metabolism of Allylestrenol can be increased when combined with Phenytoin. Approved, Vet Approved Pitolisant The serum concentration of Allylestrenol can be decreased when it is combined with Pitolisant. Approved, Investigational Posaconazole The metabolism of Allylestrenol can be decreased when combined with Posaconazole. Approved, Investigational, Vet Approved Potassium Citrate The therapeutic efficacy of Potassium Citrate can be decreased when used in combination with Allylestrenol. Approved, Investigational, Vet Approved Primidone The metabolism of Allylestrenol can be increased when combined with Primidone. Approved, Vet Approved Protein C The therapeutic efficacy of Protein C can be decreased when used in combination with Allylestrenol. Approved Protein S human The therapeutic efficacy of Protein S human can be decreased when used in combination with Allylestrenol. Approved Protocatechualdehyde The therapeutic efficacy of Protocatechualdehyde can be decreased when used in combination with Allylestrenol. Approved Ranolazine The metabolism of Allylestrenol can be decreased when combined with Ranolazine. Approved, Investigational Reviparin The therapeutic efficacy of Reviparin can be decreased when used in combination with Allylestrenol. Approved, Investigational Rifabutin The metabolism of Allylestrenol can be increased when combined with Rifabutin. Approved, Investigational Rifampicin The metabolism of Allylestrenol can be increased when combined with Rifampicin. Approved Rifapentine The metabolism of Allylestrenol can be increased when combined with Rifapentine. Approved, Investigational Rivaroxaban The therapeutic efficacy of Rivaroxaban can be decreased when used in combination with Allylestrenol. Approved Rucaparib The metabolism of Allylestrenol can be decreased when combined with Rucaparib. Approved, Investigational Saquinavir The metabolism of Allylestrenol can be decreased when combined with Saquinavir. Approved, Investigational Sarilumab The therapeutic efficacy of Allylestrenol can be decreased when used in combination with Sarilumab. Approved, Investigational Sildenafil The metabolism of Allylestrenol can be decreased when combined with Sildenafil. Approved, Investigational Siltuximab The serum concentration of Allylestrenol can be decreased when it is combined with Siltuximab. Approved, Investigational Simeprevir The serum concentration of Allylestrenol can be increased when it is combined with Simeprevir. Approved Sodium Citrate Allylestrenol may decrease the anticoagulant activities of Sodium Citrate. Approved, Investigational St. John's Wort The serum concentration of Allylestrenol can be decreased when it is combined with St. John's Wort. Approved, Investigational, Nutraceutical Stiripentol The serum concentration of Allylestrenol can be increased when it is combined with Stiripentol. Approved Sulfisoxazole The metabolism of Allylestrenol can be decreased when combined with Sulfisoxazole. Approved, Vet Approved Sulodexide The therapeutic efficacy of Sulodexide can be decreased when used in combination with Allylestrenol. Approved, Investigational Telaprevir The metabolism of Allylestrenol can be decreased when combined with Telaprevir. Approved, Withdrawn Telithromycin The metabolism of Allylestrenol can be decreased when combined with Telithromycin. Approved Ticlopidine The metabolism of Allylestrenol can be decreased when combined with Ticlopidine. Approved Tocilizumab The serum concentration of Allylestrenol can be decreased when it is combined with Tocilizumab. Approved Troxerutin The therapeutic efficacy of Troxerutin can be decreased when used in combination with Allylestrenol. Investigational Ulipristal The therapeutic efficacy of Allylestrenol can be decreased when used in combination with Ulipristal. Approved Vemurafenib The serum concentration of Allylestrenol can be decreased when it is combined with Vemurafenib. Approved Verapamil The metabolism of Allylestrenol can be decreased when combined with Verapamil. Approved Voriconazole The metabolism of Allylestrenol can be decreased when combined with Voriconazole. Approved, Investigational Warfarin The therapeutic efficacy of Warfarin can be decreased when used in combination with Allylestrenol. Approved Ximelagatran The therapeutic efficacy of Ximelagatran can be decreased when used in combination with Allylestrenol. Approved, Investigational, Withdrawn Ziprasidone The metabolism of Allylestrenol can be decreased when combined with Ziprasidone. Approved - Food Interactions
- Not Available
References
- General References
- Not Available
- External Links
- Human Metabolome Database
- HMDB0015500
- KEGG Drug
- D01374
- KEGG Compound
- C12811
- PubChem Compound
- 235905
- PubChem Substance
- 46506946
- ChemSpider
- 205855
- ChEBI
- 31189
- ChEMBL
- CHEMBL3185133
- Therapeutic Targets Database
- DPR000085
- PharmGKB
- PA164745307
- Wikipedia
- Allylestrenol
- ATC Codes
- G03DC01 — Allylestrenol
Clinical Trials
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage forms
- Not Available
- Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 80 °C PhysProp - Predicted Properties
Property Value Source Water Solubility 0.000558 mg/mL ALOGPS logP 5.14 ALOGPS logP 4.83 ChemAxon logS -5.7 ALOGPS pKa (Strongest Basic) -0.17 ChemAxon Physiological Charge 0 ChemAxon Hydrogen Acceptor Count 1 ChemAxon Hydrogen Donor Count 1 ChemAxon Polar Surface Area 20.23 Å2 ChemAxon Rotatable Bond Count 2 ChemAxon Refractivity 93.14 m3·mol-1 ChemAxon Polarizability 37.17 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 + 0.9966 Blood Brain Barrier + 0.9817 Caco-2 permeable + 0.8469 P-glycoprotein substrate Substrate 0.6615 P-glycoprotein inhibitor I Inhibitor 0.5781 P-glycoprotein inhibitor II Non-inhibitor 0.795 Renal organic cation transporter Non-inhibitor 0.6625 CYP450 2C9 substrate Non-substrate 0.807 CYP450 2D6 substrate Non-substrate 0.9046 CYP450 3A4 substrate Substrate 0.6941 CYP450 1A2 substrate Non-inhibitor 0.8345 CYP450 2C9 inhibitor Non-inhibitor 0.8006 CYP450 2D6 inhibitor Non-inhibitor 0.9427 CYP450 2C19 inhibitor Inhibitor 0.5498 CYP450 3A4 inhibitor Non-inhibitor 0.8408 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.6449 Ames test Non AMES toxic 0.936 Carcinogenicity Non-carcinogens 0.9458 Biodegradation Not ready biodegradable 0.9828 Rat acute toxicity 2.4200 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.6669 hERG inhibition (predictor II) Non-inhibitor 0.7541
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted GC-MS Spectrum - GC-MS Predicted GC-MS Not Available Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS Not Available
Taxonomy
- Description
- This compound belongs to the class of organic compounds known as estrane steroids. These are steroids with a structure based on the estrane skeleton.
- Kingdom
- Organic compounds
- Super Class
- Lipids and lipid-like molecules
- Class
- Steroids and steroid derivatives
- Sub Class
- Estrane steroids
- Direct Parent
- Estrane steroids
- Alternative Parents
- 17-hydroxysteroids / Delta-4-steroids / Tertiary alcohols / Cyclic alcohols and derivatives / Hydrocarbon derivatives
- Substituents
- 17-hydroxysteroid / Hydroxysteroid / Estrane-skeleton / Delta-4-steroid / Tertiary alcohol / Cyclic alcohol / Organic oxygen compound / Hydrocarbon derivative / Organooxygen compound / Alcohol
- Molecular Framework
- Aliphatic homopolycyclic compounds
- External Descriptors
- steroid (CHEBI:31189) / Estrane and derivatives, C21 steroids (gluco/mineralocorticoids, progestogens) and derivatives (C12811) / C21 steroids (gluco/mineralocorticoids, progestogins) and derivatives (LMST02030125)
Targets
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- Zinc ion binding
- Specific Function
- The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. Progesterone receptor ...
- Gene Name
- PGR
- Uniprot ID
- P06401
- Uniprot Name
- Progesterone receptor
- Molecular Weight
- 98979.96 Da
References
- Madauss KP, Stewart EL, Williams SP: The evolution of progesterone receptor ligands. Med Res Rev. 2007 May;27(3):374-400. [PubMed:17013809]
- Gizard F, Robillard R, Gross B, Barbier O, Revillion F, Peyrat JP, Torpier G, Hum DW, Staels B: TReP-132 is a novel progesterone receptor coactivator required for the inhibition of breast cancer cell growth and enhancement of differentiation by progesterone. Mol Cell Biol. 2006 Oct;26(20):7632-44. [PubMed:17015480]
- Wu HB, Fabian S, Jenab S, Quinones-Jenab V: Progesterone receptors activation after acute cocaine administration. Brain Res. 2006 Dec 18;1126(1):188-92. Epub 2006 Nov 15. [PubMed:17109827]
- Boonyaratanakornkit V, McGowan E, Sherman L, Mancini MA, Cheskis BJ, Edwards DP: The role of extranuclear signaling actions of progesterone receptor in mediating progesterone regulation of gene expression and the cell cycle. Mol Endocrinol. 2007 Feb;21(2):359-75. Epub 2006 Nov 30. [PubMed:17138644]
- Tranguch S, Smith DF, Dey SK: Progesterone receptor requires a co-chaperone for signalling in uterine biology and implantation. Reprod Biomed Online. 2006 Nov;13(5):651-60. [PubMed:17169175]
- Bergink EW, Loonen PB, Kloosterboer HJ: Receptor binding of allylestrenol, a progestagen of the 19-nortestosterone series without androgenic properties. J Steroid Biochem. 1985 Aug;23(2):165-8. [PubMed:3928974]
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- Actions
- Agonist
- 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
- Kumar AS, Cureton E, Shim V, Sakata T, Moore DH, Benz CC, Esserman LJ, Hwang ES: Type and duration of exogenous hormone use affects breast cancer histology. Ann Surg Oncol. 2007 Feb;14(2):695-703. Epub 2006 Nov 14. [PubMed:17103262]
- Lessey BA, Palomino WA, Apparao KB, Young SL, Lininger RA: Estrogen receptor-alpha (ER-alpha) and defects in uterine receptivity in women. Reprod Biol Endocrinol. 2006;4 Suppl 1:S9. [PubMed:17118173]
- Yuri T, Tsukamoto R, Uehara N, Matsuoka Y, Tsubura A: Effects of different durations of estrogen and progesterone treatment on development of N-methyl-N-nitrosourea-induced mammary carcinomas in female Lewis rats. In Vivo. 2006 Nov-Dec;20(6B):829-36. [PubMed:17203775]
- Montero Girard G, Vanzulli SI, Cerliani JP, Bottino MC, Bolado J, Vela J, Becu-Villalobos D, Benavides F, Gutkind S, Patel V, Molinolo A, Lanari C: Association of estrogen receptor-alpha and progesterone receptor A expression with hormonal mammary carcinogenesis: role of the host microenvironment. Breast Cancer Res. 2007;9(2):R22. [PubMed:17341305]
- Ghebeh H, Tulbah A, Mohammed S, Elkum N, Bin Amer SM, Al-Tweigeri T, Dermime S: Expression of B7-H1 in breast cancer patients is strongly associated with high proliferative Ki-67-expressing tumor cells. Int J Cancer. 2007 Aug 15;121(4):751-8. [PubMed:17415709]
- Csaba G, Gonda AI, Karabelyos C: Contraceptive treatment increases the affinity of uterine estrogen receptor in adult rat: perinatal gestagen treatment changes the reaction. Horm Metab Res. 1996 Jan;28(1):16-9. [PubMed:8820988]
Enzymes
- Kind
- Protein
- Organism
- Human
- 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
- 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. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
Drug created on July 24, 2007 10:58 / Updated on August 02, 2018 04:36