Tìm theo
Drotaverine
Các tên gọi khác (2) :
  • Drotaverin
  • Drotin
Thuốc đường tiêu hóa
Thuốc Gốc
Small Molecule
CAS: 985-12-6
ATC: A03AD02
CTHH: C24H31NO4
PTK: 397.5072
Drotaverine (INN, also known as drotaverin) is an antispasmodic drug, structurally related to papaverine. Drotaverine is a selective inhibitor of phosphodiesterase 4, and has no anticholinergic effects. Drotaverine has been shown to possess dose-dependant analgesic effects in animal models. One small study has shown drotaverine to be eliminated mainly non-renally.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C24H31NO4
Phân tử khối
397.5072
Monoisotopic mass
397.225308485
InChI
InChI=1S/C24H31NO4/c1-5-26-21-10-9-17(14-22(21)27-6-2)13-20-19-16-24(29-8-4)23(28-7-3)15-18(19)11-12-25-20/h9-10,13-16,25H,5-8,11-12H2,1-4H3/b20-13-
InChI Key
InChIKey=OMFNSKIUKYOYRG-MOSHPQCFSA-N
IUPAC Name
(1Z)-1-[(3,4-diethoxyphenyl)methylidene]-6,7-diethoxy-1,2,3,4-tetrahydroisoquinoline
Traditional IUPAC Name
drotaverine
SMILES
CCOC1=C(OCC)C=C(\C=C2/NCCC3=CC(OCC)=C(OCC)C=C23)C=C1
Độ hòa tan
2.00e-03 g/l
logP
4.19
logS
-5.3
pKa (Strongest Basic)
7.4
PSA
48.95 Å2
Refractivity
117.99 m3·mol-1
Polarizability
46.99 Å3
Rotatable Bond Count
9
H Bond Acceptor Count
5
H Bond Donor Count
1
Physiological Charge
1
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
MDDR-Like Rule
true
Dược Lực Học : Drotaverine is a spasmolytic agent by inhibiting PDE4 in smooth muscle cells.
Cơ Chế Tác Dụng : Drotaverine (INN, also known as drotaverin) is an antispasmodic drug, structurally related to papaverine. Drotaverine is a selective inhibitor of phosphodiesterase 4, and has no anticholinergic effects. Drotaverine has been shown to possess dose-dependant analgesic effects in animal models. One small study has shown drotaverine to be eliminated mainly non-renally. Drotaverine inhibits phosphodiesterases hydrolysing cAMP, thereby increasing cAMP concentration, decreasing Ca uptake of the cells and changing the distribution of calcium among the cells. It may also have minor allosteric calcium channel blocking properties.
Dược Động Học :
▧ Absorption :
Bioavailability is highly variable
▧ Protein binding :
80 to 95%
▧ Metabolism :
Hepatic
▧ Half Life :
7 to 12 hours
Chỉ Định : Used in the treatment of functional bowel disorders and alleviating pain in renal colic.
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Drotin
  • Công ty : Sanofi-Aventis
    Sản phẩm biệt dược : No-Spa
  • Công ty :
    Sản phẩm biệt dược : Taverin
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB06751
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=1712095
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=99443287
ChemSpider
http://www.chemspider.com/Chemical-Structure.1361582.html
PharmGKB
http://www.pharmgkb.org/drug/PA165958398
Wikipedia
http://en.wikipedia.org/wiki/Drotaverine
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