Tìm theo
Gliquidone
Các tên gọi khác (1) :
  • Glurenorm
antidiabetic agents
Thuốc Gốc
Small Molecule
CAS: 33342-05-1
ATC: A10BB08
CTHH: C27H33N3O6S
PTK: 527.632
Gliquidone is an anti-diabetic drug in the sulfonylurea class. It is used in the treatment of diabetes mellitus type 2. It is an ATP-dependent K+ (KATP) channel blocker. This block causes a depolarization which leads to activation of voltage-dependent Ca channels and Ca2+ influx, and eventually increases insulin release.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C27H33N3O6S
Phân tử khối
527.632
Monoisotopic mass
527.209006493
InChI
InChI=1S/C27H33N3O6S/c1-27(2)23-14-11-20(36-3)17-22(23)24(31)30(25(27)32)16-15-18-9-12-21(13-10-18)37(34,35)29-26(33)28-19-7-5-4-6-8-19/h9-14,17,19H,4-8,15-16H2,1-3H3,(H2,28,29,33)
InChI Key
InChIKey=LLJFMFZYVVLQKT-UHFFFAOYSA-N
IUPAC Name
3-cyclohexyl-1-({4-[2-(7-methoxy-4,4-dimethyl-1,3-dioxo-1,2,3,4-tetrahydroisoquinolin-2-yl)ethyl]benzene}sulfonyl)urea
Traditional IUPAC Name
3-cyclohexyl-1-{4-[2-(7-methoxy-4,4-dimethyl-1,3-dioxoisoquinolin-2-yl)ethyl]benzenesulfonyl}urea
SMILES
COC1=CC2=C(C=C1)C(C)(C)C(=O)N(CCC1=CC=C(C=C1)S(=O)(=O)NC(=O)NC1CCCCC1)C2=O
Độ tan chảy
180-182
Độ hòa tan
2.20e-03 g/l
logP
4.5
logS
-5.4
pKa (strongest acidic)
4.32
pKa (Strongest Basic)
-4.8
PSA
121.88 Å2
Refractivity
139.48 m3·mol-1
Polarizability
57.26 Å3
Rotatable Bond Count
6
H Bond Acceptor Count
6
H Bond Donor Count
2
Physiological Charge
-1
Number of Rings
4
Bioavailability
1
MDDR-Like Rule
true
Dược Lực Học : Gliquidone is an anti-diabetic drug in the sulfonylurea class. In patients with diabetes mellitus, there is a deficiency or absence of a hormone manufactured by the pancreas called insulin. Insulin is the main hormone responsible for the control of sugar in the blood. Gliquidone is an antidiabetic medication which is used in those patients with adult maturity onset or non-insulin dependent diabetes (NIDDM). It works by lowering blood sugar levels by stimulating the production and release of insulin from the pancreas. It also promotes the movement of sugar from the blood into the cells in the body which need it.
Cơ Chế Tác Dụng : Gliquidone is an anti-diabetic drug in the sulfonylurea class. It is used in the treatment of diabetes mellitus type 2. It is an ATP-dependent K+ (KATP) channel blocker. This block causes a depolarization which leads to activation of voltage-dependent Ca channels and Ca2+ influx, and eventually increases insulin release. The mechanism of action of gliquidone in lowering blood glucose appears to be dependent on stimulating the release of insulin from functioning pancreatic beta cells, and increasing sensitivity of peripheral tissues to insulin. Gliquidone likely binds to ATP-sensitive potassium channel receptors on the pancreatic cell surface, reducing potassium conductance and causing depolarization of the membrane. Membrane depolarization stimulates calcium ion influx through voltage-sensitive calcium channels. This increase in intracellular calcium ion concentration induces the secretion of insulin.
Dược Động Học :

▧ Half Life :
The mean terminal half-life was approximately 8 hours (range 5.7-9.4 hours)
Chỉ Định : Used in the treatment of diabetes mellitus type 2.
Dữ Kiện Thương Mại
Nhà Sản Xuất
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01251
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=91610
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508425
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D02430
ChemSpider
http://www.chemspider.com/Chemical-Structure.82719.html
PharmGKB
http://www.pharmgkb.org/drug/PA164744895
Wikipedia
http://en.wikipedia.org/wiki/Gliquidone
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