Tìm theo
Estradiol
Các tên gọi khác (18 ) :
  • (17beta)-Estra-1,3,5(10)-triene-3,17-diol
  • 17beta Oestradiol
  • 17beta-Estra-1,3,5(10)-triene-3,17-diol
  • 17beta-Oestradiol
  • Benzhormovarine
  • beta-Estradiol
  • cis-Estradiol
  • Dihydrofollicular hormone
  • Dihydrofolliculin
  • Dihydrotheelin
  • Dihydroxyestrin
  • Estradiol
  • Estradiol
  • Estradiol
  • Estradiol-17beta
  • Estradiolum
  • Femestral
  • Lio-Oid
Hormon, Nội tiết tố
Thuốc Gốc
Small Molecule
CAS: 50-28-2
ATC: G03CA01, G03CA03, L02AA02, L02AA03
ĐG : Apotheca Inc.
CTHH: C18H24O2
PTK: 272.382
Generally refers to the 17-beta-isomer of estradiol, an aromatized C18 steroid with hydroxyl group at 3-beta- and 17-beta-position. Estradiol-17-beta is the most potent form of mammalian estrogenic steroids. In humans, it is produced primarily by the cyclic ovaries and the placenta. It is also produced by the adipose tissue of men and postmenopausal women. The 17-alpha-isomer of estradiol binds weakly to estrogen receptors (receptors, estrogen) and exhibits little estrogenic activity in estrogen-responsive tissues. Various isomers can be synthesized. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C18H24O2
Phân tử khối
272.382
Monoisotopic mass
272.177630012
InChI
InChI=1S/C18H24O2/c1-18-9-8-14-13-5-3-12(19)10-11(13)2-4-15(14)16(18)6-7-17(18)20/h3,5,10,14-17,19-20H,2,4,6-9H2,1H3/t14-,15-,16+,17+,18+/m1/s1
InChI Key
InChIKey=VOXZDWNPVJITMN-ZBRFXRBCSA-N
IUPAC Name
(1S,10R,11S,14S,15S)-15-methyltetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadeca-2(7),3,5-triene-5,14-diol
Traditional IUPAC Name
estradiol
SMILES
[H][C@@]12CC[C@H](O)[C@@]1(C)CC[C@]1([H])C3=C(CC[C@@]21[H])C=C(O)C=C3
Độ tan chảy
151-152
Độ hòa tan
3.6 mg/L (at 27 °C)
logP
4.01
logS
-4.1
pKa (strongest acidic)
10.33
pKa (Strongest Basic)
-0.88
PSA
40.46 Å2
Refractivity
79.9 m3·mol-1
Polarizability
32.13 Å3
Rotatable Bond Count
0
H Bond Acceptor Count
2
H Bond Donor Count
2
Physiological Charge
0
Number of Rings
4
Bioavailability
1
Rule of Five
true
Ghose Filter
true
caco2 Permeability
-4.77
Dược Lực Học : Estradiol, the principal intracellular human estrogen, is substantially more active than its metabolites, estrone and estriol, at the cellular level.
Cơ Chế Tác Dụng : Generally refers to the 17-beta-isomer of estradiol, an aromatized C18 steroid with hydroxyl group at 3-beta- and 17-beta-position. Estradiol-17-beta is the most potent form of mammalian estrogenic steroids. In humans, it is produced primarily by the cyclic ovaries and the placenta. It is also produced by the adipose tissue of men and postmenopausal women. The 17-alpha-isomer of estradiol binds weakly to estrogen receptors (receptors, estrogen) and exhibits little estrogenic activity in estrogen-responsive tissues. Various isomers can be synthesized. [PubChem] Estradiol enters target cells freely (e.g., female organs, breasts, hypothalamus, pituitary) and interacts with a target cell receptor. When the estrogen receptor has bound its ligand it can enter the nucleus of the target cell, and regulate gene transcription which leads to formation of messenger RNA. The mRNA interacts with ribosomes to produce specific proteins that express the effect of estradiol upon the target cell. Estrogens increase the hepatic synthesis of sex hormone binding globulin (SHBG), thyroid-binding globulin (TBG), and other serum proteins and suppress follicle-stimulating hormone (FSH) from the anterior pituitary.
Dược Động Học :
▧ Absorption :
43%
▧ Protein binding :
>95%
▧ Metabolism :
Exogenous estrogens are metabolized using the same mechanism as endogenous estrogens. Estrogens are partially metabolized by cytochrome P450.
▧ Route of Elimination :
Estradiol, estrone and estriol are excreted in the urine along with glucuronide and sulfate conjugates.
▧ Half Life :
36 hours
Độc Tính : Can cause nausea and vomiting, and withdrawal bleeding may occur in females.
Chỉ Định : For the treatment of urogenital symptoms associated with post-menopausal atrophy of the vagina (such as dryness, burning, pruritus and dyspareunia) and/or the lower urinary tract (urinary urgency and dysuria).
Tương Tác Thuốc :
  • Amobarbital The enzyme inducer, amobarbital, decreases the effect of the hormone agent, estradiol.
  • Aprobarbital The enzyme inducer, aprobarbital, decreases the effect of the hormone agent, estradiol.
  • Butabarbital The enzyme inducer, butabarbital, decreases the effect of the hormone agent, estradiol.
  • Butalbital The enzyme inducer, butalbital, decreases the effect of the hormone agent, estradiol.
  • Butethal The enzyme inducer, butethal, decreases the effect of the hormone agent, estradiol.
  • Ethotoin The enzyme inducer, ethotoin, decreases the effect of the hormone agent, estradiol.
  • Fosphenytoin The enzyme inducer, fosphenytoin, decreases the effect of the hormone agent, estradiol.
  • Griseofulvin The enzyme inducer, griseofulvin, decreases the effect of the hormone agent, estradiol.
  • Heptabarbital The enzyme inducer, heptabarbital, decreases the effect of the hormone agent, estradiol.
  • Hexobarbital The enzyme inducer, hexobarbital, decreases the effect of the hormone agent, estradiol.
  • Mephenytoin The enzyme inducer, mephenytoin, decreases the effect of the hormone agent, estradiol.
  • Methohexital The enzyme inducer, methohexital, decreases the effect of the hormone agent, estradiol.
  • Methylphenobarbital The enzyme inducer, methylphenobarbital, decreases the effect of the hormone agent, estradiol.
  • Pentobarbital The enzyme inducer, pentobarbital, decreases the effect of the hormone agent, estradiol.
  • Phenobarbital The enzyme inducer, phenobarbital, decreases the effect of the hormone agent, estradiol.
  • Phenytoin The enzyme inducer, phenytoin, decreases the effect of the hormone agent, estradiol.
  • Prednisolone The estrogenic agent, estradiol, may increase the effect of the corticosteroid, prednisolone.
  • Prednisone The estrogenic agent, estradiol, may increase the effect of corticosteroid, prednisone.
  • Primidone The enzyme inducer, primidone, decreases the effect of the hormone agent, estradiol.
  • Raloxifene Association not recommended
  • Secobarbital The enzyme inducer, secobarbital, decreases the effect of the hormone agent, estradiol.
  • Talbutal The enzyme inducer, talbutal, decreases the effect of the hormone agent, estradiol.
  • Tipranavir Estradiol may increase the adverse dermatological effects (i.e. skin rash) of Tipranavir. Tipranavir may decrease the serum concentration Estradiol. Use an alternate form of contraception or monitor for estrogen deficiency if Estradiol is used for hormone replacement therapy.
  • Ursodeoxycholic acid Estrogens decreases the effect of ursodiol
Liều Lượng & Cách Dùng : Disc - Transdermal
Gel - Transdermal
Liquid - Intramuscular
Patch - Transdermal
Ring - Intravaginal
Tablet - Intravaginal
Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Watson
    Sản phẩm biệt dược : Alora
  • Công ty : Bayer
    Sản phẩm biệt dược : Climara
  • Công ty :
    Sản phẩm biệt dược : Depo-Estradiol
  • Công ty : Orion
    Sản phẩm biệt dược : Divigel
  • Sản phẩm biệt dược : Elestrin
  • Sản phẩm biệt dược : Estrace
  • Công ty : Novartis
    Sản phẩm biệt dược : Estraderm MX
  • Công ty : Novartis
    Sản phẩm biệt dược : Estraderm TTS
  • Công ty : Medicis
    Sản phẩm biệt dược : Estrasorb
  • Công ty : Pfizer
    Sản phẩm biệt dược : Estring
  • Công ty : Novo Nordisk
    Sản phẩm biệt dược : Estrofem
  • Công ty : Schering-Plough
    Sản phẩm biệt dược : Estrogel
  • Sản phẩm biệt dược : EvaMist
  • Công ty : Warner Chilcott
    Sản phẩm biệt dược : Femring
  • Công ty : Warner Chilcott
    Sản phẩm biệt dược : Femtrace
  • Công ty : Novo Nordisk
    Sản phẩm biệt dược : Innofem
  • Công ty : Bayer
    Sản phẩm biệt dược : Menostar
  • Công ty :
    Sản phẩm biệt dược : Minivelle
  • Công ty :
    Sản phẩm biệt dược : Vagifem
  • Công ty : Novartis
    Sản phẩm biệt dược : Vivelle
  • Công ty : Novartis
    Sản phẩm biệt dược : Vivelle-Dot
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00783
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=5757
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508115
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C00951
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00105
ChemSpider
http://www.chemspider.com/Chemical-Structure.5554.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=17292
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0378-1452-01
PharmGKB
http://www.pharmgkb.org/drug/PA449503
Wikipedia
http://en.wikipedia.org/wiki/Estradiol
RxList
http://www.rxlist.com/cgi/generic3/estrogel.htm
Drugs.com
http://www.drugs.com/estradiol.html
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