Tìm theo
Hydrocortamate
Các tên gọi khác (3) :
  • 17-Hydroxycorticosterone, 21-(diethylamino)acetate
  • Hidrocortamato
  • Hydrocortamatum
anti inflammatory agents, corticosteroids
Thuốc Gốc
Small Molecule
CAS: 76-47-1
CTHH: C27H41NO6
PTK: 475.6175
Hydrocortamate is a synthetic glucocorticoid used for its anti-inflammatory or immunosuppressive properties to treat inflammation due to corticosteroid-responsive dermatoses. Glucocorticoids are a class of steroid hormones characterised by an ability to bind with the cortisol receptor and trigger a variety of important cardiovascular, metabolic, immunologic and homeostatic effects.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C27H41NO6
Phân tử khối
475.6175
Monoisotopic mass
475.293388049
InChI
InChI=1S/C27H41NO6/c1-5-28(6-2)15-23(32)34-16-22(31)27(33)12-10-20-19-8-7-17-13-18(29)9-11-25(17,3)24(19)21(30)14-26(20,27)4/h13,19-21,24,30,33H,5-12,14-16H2,1-4H3/t19-,20-,21-,24+,25-,26-,27-/m0/s1
InChI Key
InChIKey=FWFVLWGEFDIZMJ-FOMYWIRZSA-N
IUPAC Name
2-[(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-2,15-dimethyl-5-oxotetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadec-6-en-14-yl]-2-oxoethyl 2-(diethylamino)acetate
Traditional IUPAC Name
hydrocortamate
SMILES
[H][C@@]12CC[C@](O)(C(=O)COC(=O)CN(CC)CC)[C@@]1(C)C[C@H](O)[C@@]1([H])[C@@]2([H])CCC2=CC(=O)CC[C@]12C
Độ tan chảy
162-163
Độ hòa tan
8.55e-02 g/l
logP
1.2
logS
-3.8
pKa (strongest acidic)
12.61
pKa (Strongest Basic)
6.43
PSA
104.14 Å2
Refractivity
129.48 m3·mol-1
Polarizability
53.29 Å3
Rotatable Bond Count
8
H Bond Acceptor Count
6
H Bond Donor Count
2
Physiological Charge
0
Number of Rings
4
Bioavailability
1
Rule of Five
true
MDDR-Like Rule
true
Dược Lực Học : Hydrocortamate is a synthetic glucocorticoid used for its anti-inflammatory or immunosuppressive properties to treat inflammation due to corticosteroid-responsive dermatoses. Glucocorticoids are a class of steroid hormones characterised by an ability to bind with the cortisol receptor and trigger a variety of important cardiovascular, metabolic, immunologic and homeostatic effects. Glucocorticoids are distinguished from mineralocorticoids and sex steroids by having different receptors, target cells, and effects. Technically, the term corticosteroid refers to both glucocorticoids and mineralocorticoids, but is often used as a synonym for glucocorticoid. Glucocorticoids suppress cell-mediated immunity. They act by inhibiting genes that code for the cytokines IL-1, IL-2, IL-3, IL-4, IL-5, IL-6, IL-8 and TNF-alpha, the most important of which is the IL-2. Reduced cytokine production limits T cell proliferation. Glucocorticoids also suppress humoral immunity, causing B cells to express lower amounts of IL-2 and IL-2 receptors. This diminishes both B cell clonal expansion and antibody synthesis. The diminished amounts of IL-2 also leads to fewer T lymphocyte cells being activated.
Cơ Chế Tác Dụng : Hydrocortamate is a synthetic glucocorticoid used for its anti-inflammatory or immunosuppressive properties to treat inflammation due to corticosteroid-responsive dermatoses. Glucocorticoids are a class of steroid hormones characterised by an ability to bind with the cortisol receptor and trigger a variety of important cardiovascular, metabolic, immunologic and homeostatic effects. Hydrocortamate binds to the cytosolic glucocorticoid receptor. After binding the receptor the newly formed receptor-ligand complex translocates itself into the cell nucleus, where it binds to many glucocorticoid response elements (GRE) in the promoter region of the target genes. The DNA bound receptor then interacts with basic transcription factors, causing the increase in expression of specific target genes. The anti-inflammatory actions of corticosteroids are thought to involve lipocortins, phospholipase A2 inhibitory proteins which, through inhibition arachidonic acid, control the biosynthesis of prostaglandins and leukotrienes. The immune system is suppressed by corticosteroids due to a decrease in the function of the lymphatic system, a reduction in immunoglobulin and complement concentrations, the precipitation of lymphocytopenia, and interference with antigen-antibody binding.
Dược Động Học :

▧ Metabolism :
Primarily hepatic via CYP3A4
Độc Tính : Side effects include burning, itching, irritation, dryness, folliculitis, hypertrichosis, acneiform eruptions, hypopigmentation, perioral dermatitis, allergic contact dermatitis, maceration of the skin, secondary infection, skin atrophy, striae, miliaria.
Chỉ Định : Used topically as an antiinflammatory in the treatment of steroid-responsive dermatoses
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty : Angelini
    Sản phẩm biệt dược : Etacort
  • Công ty : Pfizer
    Sản phẩm biệt dược : Magnacort
  • Công ty :
    Sản phẩm biệt dược : Ulcort
  • Công ty :
    Sản phẩm biệt dược : Ulcort top
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00769
PharmGKB
http://www.pharmgkb.org/drug/PA164745515
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