Tìm theo
Quinethazone
Các tên gọi khác (6 ) :
  • Chinetazone
  • Chinethazonum
  • Hydromox
  • Quinetazona
  • Quinethazon
  • Quinethazonum
sodium chloride symporter inhibitors
Thuốc Gốc
Small Molecule
CAS: 73-49-4
ATC: C03BA02
CTHH: C10H12ClN3O3S
PTK: 289.739
Quinethazone (INN, brand name Hydromox) is a thiazide diuretic used to treat hypertension. Common side effects include dizziness, dry mouth, nausea, and low potassium levels.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C10H12ClN3O3S
Phân tử khối
289.739
Monoisotopic mass
289.028789662
InChI
InChI=1S/C10H12ClN3O3S/c1-2-9-13-7-4-6(11)8(18(12,16)17)3-5(7)10(15)14-9/h3-4,9,13H,2H2,1H3,(H,14,15)(H2,12,16,17)
InChI Key
InChIKey=AGMMTXLNIQSRCG-UHFFFAOYSA-N
IUPAC Name
7-chloro-2-ethyl-4-oxo-1,2,3,4-tetrahydroquinazoline-6-sulfonamide
Traditional IUPAC Name
quinethazone
SMILES
CCC1NC(=O)C2=CC(=C(Cl)C=C2N1)S(N)(=O)=O
Độ tan chảy
251 °C
Độ hòa tan
150 mg/L (at 25 °C)
logP
1.19
logS
-2.1
pKa (strongest acidic)
9.56
pKa (Strongest Basic)
-0.97
PSA
101.29 Å2
Refractivity
69.34 m3·mol-1
Polarizability
27.3 Å3
Rotatable Bond Count
2
H Bond Acceptor Count
4
H Bond Donor Count
3
Physiological Charge
0
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Quinethazone is a thiazide diuretic used to treat hypertension. It inhibits Na+/Cl- reabsorption from the distal convoluted tubules in the kidneys. Thiazides also cause loss of potassium and an increase in serum uric acid. Thiazides are often used to treat hypertension, but their hypotensive effects are not necessarily due to their diuretic activity. Thiazides have been shown to prevent hypertension-related morbidity and mortality although the mechanism is not fully understood. Thiazides cause vasodilation by activating calcium-activated potassium channels (large conductance) in vascular smooth muscles and inhibiting various carbonic anhydrases in vascular tissue.
Cơ Chế Tác Dụng : Quinethazone (INN, brand name Hydromox) is a thiazide diuretic used to treat hypertension. Common side effects include dizziness, dry mouth, nausea, and low potassium levels. As a diuretic, quinethazone inhibits active chloride reabsorption at the early distal tubule via the Na-Cl cotransporter, resulting in an increase in the excretion of sodium, chloride, and water. Thiazides like quinethazone also inhibit sodium ion transport across the renal tubular epithelium through binding to the thiazide sensitive sodium-chloride transporter. This results in an increase in potassium excretion via the sodium-potassium exchange mechanism. The antihypertensive mechanism of quinethazone is less well understood although it may be mediated through its action on carbonic anhydrases in the smooth muscle or through its action on the large-conductance calcium-activated potassium (KCa) channel, also found in the smooth muscle.
Chỉ Định : Used to treat hypertension.
Tương Tác Thuốc :
  • Digoxin Possible electrolyte variations and arrhythmias
  • Lithium The thiazide diuretic, quinethazone, may increase serum levels of lithium.
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Aquamox
  • Công ty :
    Sản phẩm biệt dược : Hydromox
  • Công ty :
    Sản phẩm biệt dược : Idrokin
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01325
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=6307
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507280
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07342
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00461
ChemSpider
http://www.chemspider.com/Chemical-Structure.6068.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=25898
PharmGKB
http://www.pharmgkb.org/drug/PA164760863
Wikipedia
http://en.wikipedia.org/wiki/Quinethazone
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