Tìm theo
Flumethasone Pivalate
Các tên gọi khác (5 ) :
  • Flumetason
  • Flumetasona
  • Flumétasone
  • Flumetasone pivalate
  • Flumetasonum
Thuốc Gốc
Small Molecule
CAS: 2002-29-1
CTHH: C27H36F2O6
PTK: 494.5679
Flumethasone pivalate is a moderately potent difluorinated corticosteroid ester with anti-inflammatory, antipruritic and vasoconstrictive properties. As it is a privalate salt, its anti-inflammatory action is concentrated at the site of application. This local effect on diseased areas results in a prompt decrease in inflammation, exudation and itching.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C27H36F2O6
Phân tử khối
494.5679
Monoisotopic mass
494.247995294
InChI
InChI=1S/C27H36F2O6/c1-14-9-16-17-11-19(28)18-10-15(30)7-8-24(18,5)26(17,29)20(31)12-25(16,6)27(14,34)21(32)13-35-22(33)23(2,3)4/h7-8,10,14,16-17,19-20,31,34H,9,11-13H2,1-6H3/t14-,16+,17+,19+,20+,24+,25+,26+,27+/m1/s1
InChI Key
InChIKey=JWRMHDSINXPDHB-OJAGFMMFSA-N
IUPAC Name
2-[(1R,2S,8S,10S,11S,13R,14R,15S,17S)-1,8-difluoro-14,17-dihydroxy-2,13,15-trimethyl-5-oxotetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadeca-3,6-dien-14-yl]-2-oxoethyl 2,2-dimethylpropanoate
Traditional IUPAC Name
flumethasone pivalate
SMILES
C[C@@H]1C[C@H]2[C@@H]3C[C@H](F)C4=CC(=O)C=C[C@]4(C)[C@@]3(F)[C@@H](O)C[C@]2(C)[C@@]1(O)C(=O)COC(=O)C(C)(C)C
Độ tan chảy
219 °C (base only)
Độ hòa tan
0.392 mg/L
logP
3.86
logS
-4.7
pKa (strongest acidic)
12.44
pKa (Strongest Basic)
-3.4
PSA
100.9 Å2
Refractivity
125.17 m3·mol-1
Polarizability
50.96 Å3
Rotatable Bond Count
5
H Bond Acceptor Count
5
H Bond Donor Count
2
Physiological Charge
0
Number of Rings
4
Bioavailability
1
Rule of Five
true
Dược Lực Học : Flumethasone pivalate is a moderately potent difluorinated corticosteroid ester with anti-inflammatory, antipruritic and vasoconstrictive properties. As it is a privalate salt, its anti-inflammatory action is concentrated at the site of application. This local effect on diseased areas results in a prompt decrease in inflammation, exudation and itching.
Cơ Chế Tác Dụng : Flumethasone pivalate is a moderately potent difluorinated corticosteroid ester with anti-inflammatory, antipruritic and vasoconstrictive properties. As it is a privalate salt, its anti-inflammatory action is concentrated at the site of application. This local effect on diseased areas results in a prompt decrease in inflammation, exudation and itching. Flumethasone is a glucocorticoid receptor agonist. This complex binds to the nucleus causing a variety of genetic activation and repressions. The antiinflammatory 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. Flumethasone binds to plasma transcortin, and it becomes active when it is not bound to transcortin.
Dược Động Học :
▧ Absorption :
Minimal if applied topically
▧ Metabolism :
Primarily hepatic
Độc Tính : Can lead to signs of irritation such as burning sensation, itching or skin rash at the site of application; hypersensitivity reactions.
Chỉ Định : For the treatment of contact dermatitis, atopic dermatitis, exczema, psoriasis, diaper rash and other skin conditions
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty : Riemser
    Sản phẩm biệt dược : Cerson
  • Công ty : Novartis
    Sản phẩm biệt dược : Locacorten
  • Công ty : Novartis
    Sản phẩm biệt dược : Locorten
  • Công ty : Maeda Yakuhin
    Sản phẩm biệt dược : Testohgen
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00663
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=443980
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505121
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D01464
ChemSpider
http://www.chemspider.com/Chemical-Structure.392021.html
PharmGKB
http://www.pharmgkb.org/drug/PA164749388
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