Tìm theo
Enoximone
Các tên gọi khác (1) :
  • Perfan
Thuốc Gốc
Small Molecule
CAS: 77671-31-9
ATC: C01CE03
CTHH: C12H12N2O2S
PTK: 248.301
Enoximone is a selective phosphodiesterase inhibitor with vasodilating and positive inotropic activity that does not cause changes in myocardial oxygen consumption. It is used in patients with congestive heart failure. Trials were halted in the U.S., but the drug is used in various countries.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C12H12N2O2S
Phân tử khối
248.301
Monoisotopic mass
248.061948328
InChI
InChI=1S/C12H12N2O2S/c1-7-10(14-12(16)13-7)11(15)8-3-5-9(17-2)6-4-8/h3-6H,1-2H3,(H2,13,14,16)
InChI Key
InChIKey=ZJKNESGOIKRXQY-UHFFFAOYSA-N
IUPAC Name
4-methyl-5-{[4-(methylsulfanyl)phenyl]carbonyl}-2,3-dihydro-1H-imidazol-2-one
Traditional IUPAC Name
enoximone
SMILES
CSC1=CC=C(C=C1)C(=O)C1=C(C)NC(=O)N1
Độ tan chảy
256 dec °C
Độ hòa tan
6.82e-02 g/l
logP
1.84
logS
-3.6
pKa (strongest acidic)
9.68
pKa (Strongest Basic)
-7.8
PSA
58.2 Å2
Refractivity
70.05 m3·mol-1
Polarizability
25.67 Å3
Rotatable Bond Count
3
H Bond Acceptor Count
2
H Bond Donor Count
2
Physiological Charge
0
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Enoximone is a phosphodiesterase inhibitor (type III) that increases the force of contraction of the heart and dilates blood vessels. In June 2005, Myogen announced that they were discontinuing development of enoximone due to negative results. The drug is approved for use in the UK.
Cơ Chế Tác Dụng : Enoximone is a selective phosphodiesterase inhibitor with vasodilating and positive inotropic activity that does not cause changes in myocardial oxygen consumption. It is used in patients with congestive heart failure. Trials were halted in the U.S., but the drug is used in various countries. Further research is required to determine accurately the mechanism of action of drugs with phosphodiesterase inhibitory activity, however, inhibition of PDE3 inhibits degredation of cGMP. This allows for increased NO release and vascular relaxation.
Dược Động Học :
▧ Absorption :
Bioavailabvility is 50% following oral administration.
▧ Protein binding :
85%
▧ Metabolism :
Hepatic oxidation
▧ Half Life :
4-10 hours
Chỉ Định : For the treatment of congestive heart failure.
Liều Lượng & Cách Dùng : Solution - Oral
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Perfan
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB04880
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=53708
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505575
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D04004
ChemSpider
http://www.chemspider.com/Chemical-Structure.48492.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50241379
PharmGKB
http://www.pharmgkb.org/drug/PA164768794
Wikipedia
http://en.wikipedia.org/wiki/Enoximone
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