Tìm theo
Nitrendipine
Các tên gọi khác (9 ) :
  • 1,4-dihydro-2,6-Dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylic acid ethyl methyl ester
  • BAY e 5009
  • Bayotensin
  • Baypress
  • Bylotensin
  • Deiten
  • Nidrel
  • Nitrendipino
  • Nitrendipinum
antihypertensive agents, vasodilator agents, calcium channel blockers
Thuốc Gốc
Small Molecule
CAS: 39562-70-4
ATC: C08CA08
CTHH: C18H20N2O6
PTK: 360.3612
A calcium channel blocker with marked vasodilator action. It is an effective antihypertensive agent and differs from other calcium channel blockers in that it does not reduce glomerular filtration rate and is mildly natriuretic, rather than sodium retentive. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C18H20N2O6
Phân tử khối
360.3612
Monoisotopic mass
360.132136382
InChI
InChI=1S/C18H20N2O6/c1-5-26-18(22)15-11(3)19-10(2)14(17(21)25-4)16(15)12-7-6-8-13(9-12)20(23)24/h6-9,16,19H,5H2,1-4H3
InChI Key
InChIKey=PVHUJELLJLJGLN-UHFFFAOYSA-N
IUPAC Name
3-ethyl 5-methyl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate
Traditional IUPAC Name
nitrendipine
SMILES
CCOC(=O)C1=C(C)NC(C)=C(C1C1=CC(=CC=C1)[N+]([O-])=O)C(=O)OC
Độ tan chảy
156-160 °C
Độ hòa tan
Insoluble
logP
2.88
logS
-4.4
pKa (Strongest Basic)
5.43
PSA
110.45 Å2
Refractivity
96.91 m3·mol-1
Polarizability
36.25 Å3
Rotatable Bond Count
7
H Bond Acceptor Count
5
H Bond Donor Count
1
Physiological Charge
0
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
caco2 Permeability
-4.77
Dược Lực Học : Nitrendipine, a dihydropyridine calcium-channel blocker, is used alone or with an angiotensin-converting enzyme inhibitor, to treat hypertension, chronic stable angina pectoris, and Prinzmetal's variant angina. Nitrendipine is similar to other peripheral vasodilators. Nitrendipine inhibits the influx of extra cellular calcium across the myocardial and vascular smooth muscle cell membranes possibly by deforming the channel, inhibiting ion-control gating mechanisms, and/or interfering with the release of calcium from the sarcoplasmic reticulum. The decrease in intracellular calcium inhibits the contractile processes of the myocardial smooth muscle cells, causing dilation of the coronary and systemic arteries, increased oxygen delivery to the myocardial tissue, decreased total peripheral resistance, decreased systemic blood pressure, and decreased afterload.
Cơ Chế Tác Dụng : A calcium channel blocker with marked vasodilator action. It is an effective antihypertensive agent and differs from other calcium channel blockers in that it does not reduce glomerular filtration rate and is mildly natriuretic, rather than sodium retentive. [PubChem] By deforming the channel, inhibiting ion-control gating mechanisms, and/or interfering with the release of calcium from the sarcoplasmic reticulum, Nitrendipine inhibits the influx of extracellular calcium across the myocardial and vascular smooth muscle cell membranes The decrease in intracellular calcium inhibits the contractile processes of the myocardial smooth muscle cells, causing dilation of the coronary and systemic arteries, increased oxygen delivery to the myocardial tissue, decreased total peripheral resistance, decreased systemic blood pressure, and decreased afterload.
Dược Động Học :

▧ Protein binding :
> 99%
Chỉ Định : For the treatment of mild to moderate hypertension
Tương Tác Thuốc :
  • Cimetidine Cimetidine increases the effect of the calcium channel blocker, nitrendipine.
  • Telithromycin Telithromycin may reduce clearance of Nitrendipine. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Nitrendipine if Telithromycin is initiated, discontinued or dose changed.
  • Thiopental The CYP3A4 inducer, Thiopental, may increase the metabolism and clearance of Nitrendipine, a CYP3A4 substrate. Monitor for changes in the therapeutic/adverse effects of Nitrendipine if Thiopental is initiated, discontinued or dose changed.
  • Tipranavir Tipranavir may decrease the metabolism and clearance of the calcium channel blocker, Nitrendipine. Monitor for changes in Nitrendipine therapeutic and adverse effects if Tipranavir is initiated, discontinued or dose changed.
  • Treprostinil Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
  • Voriconazole Voriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of nitrendipine by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of nitrendipine if voriconazole is initiated, discontinued or dose changed.
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Bayotensin
  • Công ty :
    Sản phẩm biệt dược : Baypress
  • Công ty :
    Sản phẩm biệt dược : Deiten
  • Công ty :
    Sản phẩm biệt dược : Nidrel
  • Công ty :
    Sản phẩm biệt dược : Nitrepin
  • Công ty :
    Sản phẩm biệt dược : Nitrezic
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01054
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=4507
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508817
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07713
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00629
ChemSpider
http://www.chemspider.com/Chemical-Structure.4351.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50012016
PharmGKB
http://www.pharmgkb.org/drug/PA146096020
Wikipedia
http://en.wikipedia.org/wiki/Nitrendipine
... loading
... loading