Tìm theo
Chlorotrianisene
Các tên gọi khác (10 ) :
  • Chloortrianisestrol
  • Chlorestrolo
  • Chlorotrianisenum
  • Chlorotrianisine
  • Chlorotrianizen
  • Chlortrianisen
  • Chlortrianisestrol
  • Chlortrianisoestrolum
  • Chlortrianizen
  • Clorotrianiseno
Thuốc điều trị ung thư
Thuốc Gốc
Small Molecule
CAS: 569-57-3
ATC: G03CA06
CTHH: C23H21ClO3
PTK: 380.864
A powerful synthetic, non-steroidal estrogen. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C23H21ClO3
Phân tử khối
380.864
Monoisotopic mass
380.117922245
InChI
InChI=1S/C23H21ClO3/c1-25-19-10-4-16(5-11-19)22(17-6-12-20(26-2)13-7-17)23(24)18-8-14-21(27-3)15-9-18/h4-15H,1-3H3
InChI Key
InChIKey=BFPSDSIWYFKGBC-UHFFFAOYSA-N
IUPAC Name
1-[2-chloro-1,2-bis(4-methoxyphenyl)ethenyl]-4-methoxybenzene
Traditional IUPAC Name
chlorotrianisene
SMILES
COC1=CC=C(C=C1)C(Cl)=C(C1=CC=C(OC)C=C1)C1=CC=C(OC)C=C1
Độ tan chảy
113-114
Độ hòa tan
1.99e-04 g/l
logP
6.4
logS
-6.3
pKa (Strongest Basic)
-4.4
PSA
27.69 Å2
Refractivity
119.17 m3·mol-1
Polarizability
41.6 Å3
Rotatable Bond Count
6
H Bond Acceptor Count
3
H Bond Donor Count
0
Physiological Charge
0
Number of Rings
3
Bioavailability
1
Ghose Filter
true
MDDR-Like Rule
true
Dược Lực Học : Chlorotrianisene is a nonsteroidal synthetic estrogen. After menopause, when the body no longer produces estrogen, chlorotrianisene is used as a simple replacement of estrogen. The estrogen-stimulated endometrium may bleed within 48-72 hours after discontinuance of estrogen therapy. Paradoxically, prolonged estrogen therapy may cause shrinkage of the endometrium and an increase in size of the myometrium. Estrogens have a weak anabolic effect and may cause sodium retention with associated fluid retention and edema. Estrogens may also decrease elevated blood cholesterol and phospholipid concentrations. Estrogens affect bone by increasing calcium deposition and accelerating epiphyseal closure, following initial growth stimulation. During the preovulatory or nonovulatory phase of the menstrual cycle, estrogen is the principal determinant in the onset of menstruation. A decline of estrogenic activity at the end of the menstrual cycle also may induce menstruation; however, the cessation of progesterone secretion is the most important factor during the mature ovulatory phase of the menstrual cycle. The benefit derived from estrogen therapy in the prevention of postpartum breast engorgement must be carefully weighed against the potential increased risk of puerperal thromboembolism associated with the use of large doses of estrogens.
Cơ Chế Tác Dụng : A powerful synthetic, non-steroidal estrogen. [PubChem] Chlorotrianisene binds to the estrogen receptor on various estrogen receptor bearing cells. Target cells include cells in the female reproductive tract, the mammary gland, the hypothalamus, and the pituitary. 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 :
Absorption following oral administration is rapid.
▧ Protein binding :
50-80%
▧ Metabolism :
Metabolized principally in the liver, although the kidneys, gonads, and muscle tissues may be involved to some extent. The metabolic fate of the synthetic estrogens has not been fully elucidated.
Độc Tính : Acute overdosage of large doses of oral contraceptives in chidren reportedly produces almost no toxicity except nausea and vomiting. Acute overdosage of estrogens may cause nausea, and withdrawal bleeding may occur in females.
Chỉ Định : Used to treat symptoms of menopause, deficiencies in ovary function (including underdevelopment of female sexual characteristics and some types of infertility), and in rare cases, prostate cancer. Chlorotrianisene may also be used to prevent breast engorgement following childbirth.
Tương Tác Thuốc :
  • Fosphenytoin The enzyme inducer, fosphenytoin, decreases the effect of the hormone agent, chlorotrianisene.
  • Griseofulvin The enzyme inducer, griseofulvin, decreases the effect of the hormone agent, chlorotrianisene.
  • Phenobarbital The enzyme inducer, phenobarbital, decreases the effect of the hormone agent, chlorotrianisene.
  • Phenytoin The enzyme inducer, phenytoin, decreases the effect of the hormone agent, chlorotrianisene.
  • Prednisolone The estrogenic agent, chlorotrianisene, may increase the effect of the corticosteroid, prednisolone.
  • Prednisone The estrogenic agent, chlorotrianisene, may increase the effect of corticosteroid, prednisone.
  • Primidone The enzyme inducer, primidone, decreases the effect of the hormone agent, chlorotrianisene.
  • Raloxifene Association not recommended
Liều Lượng & Cách Dùng : Capsule - Oral
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty : Merrell
    Sản phẩm biệt dược : Merbentul
  • Công ty : Merrell
    Sản phẩm biệt dược : Tace
  • Công ty : Merrell
    Sản phẩm biệt dược : Tace FN
  • Công ty : Gentili
    Sản phẩm biệt dược : Triagen
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00269
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=11289
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508811
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00269
ChemSpider
http://www.chemspider.com/Chemical-Structure.10815.html
PharmGKB
http://www.pharmgkb.org/drug/PA164768822
Wikipedia
http://en.wikipedia.org/wiki/Chlorotrianisene
Drugs.com
http://www.drugs.com/mtm/chlorotrianisene.html
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