Tìm theo
Alprenolol
Các tên gọi khác (9 ) :
  • (RS)-1-(2-allylphenoxy)-3-(isopropylamino)propan-2-ol
  • 1-(2-Allylphenoxy)-3-isopropylamino-2-propanol
  • 1-(O-Allylphenoxy)-3-(isopropylamino)-2-propanol
  • Alfeprol
  • Alprenolol
  • Alprénolol
  • Alprenolol
  • Alprenololum
  • Aprenololo
antihypertensive agents, sympatholytics, anti arrhythmia agents, adrenergic beta antagonists
Thuốc Gốc
Small Molecule
CAS: 13655-52-2
ATC: C07AA01
CTHH: C15H23NO2
PTK: 249.3486
One of the adrenergic beta-antagonists used as an antihypertensive, anti-anginal, and anti-arrhythmic agent. Alprenolol is no longer marketed by AstraZeneca, but may still be available in generic varieties.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C15H23NO2
Phân tử khối
249.3486
Monoisotopic mass
249.172878985
InChI
InChI=1S/C15H23NO2/c1-4-7-13-8-5-6-9-15(13)18-11-14(17)10-16-12(2)3/h4-6,8-9,12,14,16-17H,1,7,10-11H2,2-3H3
InChI Key
InChIKey=PAZJSJFMUHDSTF-UHFFFAOYSA-N
IUPAC Name
{2-hydroxy-3-[2-(prop-2-en-1-yl)phenoxy]propyl}(propan-2-yl)amine
Traditional IUPAC Name
alprenolol
SMILES
CC(C)NCC(O)COC1=CC=CC=C1CC=C
Độ tan chảy
107-109 °C
Độ hòa tan
547 mg/L
logP
3.10
logS
-3.1
pKa (strongest acidic)
14.09
pKa (Strongest Basic)
9.67
PSA
41.49 Å2
Refractivity
74.66 m3·mol-1
Polarizability
29.38 Å3
Rotatable Bond Count
8
H Bond Acceptor Count
3
H Bond Donor Count
2
Physiological Charge
1
Number of Rings
1
Bioavailability
1
Rule of Five
true
Ghose Filter
true
caco2 Permeability
-4.62
Dược Lực Học : Alprenolol is a non-selective beta-blocker used in the treatment of hypertension, edema, ventricular tachycardias, and atrial fibrillation. Alprenolol impairs AV node conduction and decreases sinus rate and may also increase plasma triglycerides and decrease HDL-cholesterol levels. Alprenolol is nonpolar and hydrophobic, with low to moderate lipid solubility. Alprenolol has little to no intrinsic sympathomimetic activity and, unlike some other beta-adrenergic blocking agents, alprenolol has little direct myocardial depressant activity and does not have an anesthetic-like membrane-stabilizing action.
Cơ Chế Tác Dụng : One of the adrenergic beta-antagonists used as an antihypertensive, anti-anginal, and anti-arrhythmic agent. Alprenolol is no longer marketed by AstraZeneca, but may still be available in generic varieties. Alprenolol non-selectively blocks beta-1 adrenergic receptors mainly in the heart, inhibiting the effects of epinephrine and norepinephrine resulting in a decrease in heart rate and blood pressure. Also, with a more minor effect, by binding beta-2 receptors in the juxtaglomerular apparatus, alprenolol inhibits the production of renin, thereby inhibiting angiotensin II and aldosterone production and therefore inhibits the vasoconstriction and water retention due to angiotensin II and aldosterone, respectively.
Dược Động Học :

▧ Protein binding :
80-90%
▧ Metabolism :
Hepatic. One of the active metabolites, 4-OH-alprenolol, is an active beta-blocker.
▧ Half Life :
2-3 hours
Độc Tính : LD50=597.0 mg/kg (Orally in rats)
Chỉ Định : For the treatment of hypertension, angina, and arrhythmia
Liều Lượng & Cách Dùng : Capsule - Oral - 200 mg/day in divided doses
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty : AstraZeneca
    Sản phẩm biệt dược : Apllobal
  • Công ty : AstraZeneca
    Sản phẩm biệt dược : Aptin
  • Công ty :
    Sản phẩm biệt dược : Aptine
  • Công ty :
    Sản phẩm biệt dược : Aptol Duriles
  • Sản phẩm biệt dược : Atenenol
  • Công ty : Shyh Dar
    Sản phẩm biệt dược : Elp
  • Công ty :
    Sản phẩm biệt dược : Gubernal
  • Công ty :
    Sản phẩm biệt dược : Regletin
  • Công ty : Kotobuki Seiyaku
    Sản phẩm biệt dược : Skajilol
  • Công ty :
    Sản phẩm biệt dược : Yobir
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00866
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=2119
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506033
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D07156
ChemSpider
http://www.chemspider.com/Chemical-Structure.2035.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=25764
PharmGKB
http://www.pharmgkb.org/drug/PA164750541
Wikipedia
http://en.wikipedia.org/wiki/Alprenolol
Drugs.com
http://www.drugs.com/international/alprenolol.html
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