Tìm theo
Glycodiazine
Các tên gọi khác (2) :
  • Glidiazine
  • Glymidine
Thuốc Gốc
Small Molecule
CAS: 339-44-6
ATC: A10BC01
CTHH: C13H15N3O4S
PTK: 309.341
Glycodiazine is used with diet to lower blood glucose by increasing the secretion of insulin from pancreas and increasing the sensitivity of peripheral tissues to insulin. The mechanism of action of glycodiazine 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. Glycodiazine 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. It is used for the concomitant use with insulin for the treatment of noninsulin-dependent (type 2) diabetes mellitus.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C13H15N3O4S
Phân tử khối
309.341
Monoisotopic mass
309.078326673
InChI
InChI=1S/C13H15N3O4S/c1-19-7-8-20-11-9-14-13(15-10-11)16-21(17,18)12-5-3-2-4-6-12/h2-6,9-10H,7-8H2,1H3,(H,14,15,16)
InChI Key
InChIKey=QFWPJPIVLCBXFJ-UHFFFAOYSA-N
IUPAC Name
N-[5-(2-methoxyethoxy)pyrimidin-2-yl]benzenesulfonamide
Traditional IUPAC Name
glycodiazine
SMILES
COCCOC1=CN=C(NS(=O)(=O)C2=CC=CC=C2)N=C1
Độ tan chảy
220-223
Độ hòa tan
1.24e-01 g/l
logP
1.01
logS
-3.4
pKa (strongest acidic)
6.92
pKa (Strongest Basic)
-1.4
PSA
90.41 Å2
Refractivity
77.01 m3·mol-1
Polarizability
31.29 Å3
Rotatable Bond Count
6
H Bond Acceptor Count
6
H Bond Donor Count
1
Physiological Charge
-1
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Glycodiazine is used with diet to lower blood glucose by increasing the secretion of insulin from pancreas and increasing the sensitivity of peripheral tissues to insulin.
Cơ Chế Tác Dụng : Glycodiazine is used with diet to lower blood glucose by increasing the secretion of insulin from pancreas and increasing the sensitivity of peripheral tissues to insulin. The mechanism of action of glycodiazine 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. Glycodiazine 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. It is used for the concomitant use with insulin for the treatment of noninsulin-dependent (type 2) diabetes mellitus. The mechanism of action of glycodiazine 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. Glycodiazine 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. The rise in intracellular calcium leads to increased fusion of insulin granulae with the cell membrane, and therefore increased secretion of (pro)insulin.
Dược Động Học :
▧ Absorption :
Rapidly and completely absorbed following oral administration.
▧ Protein binding :
90% bound to plasma proteins.
▧ Half Life :
4 hours.
Độc Tính : Severe hypoglycemic reactions with coma, seizure, or other neurological impairment.
Chỉ Định : Glycodiazine is used concomitantly with insulin for the treatment of noninsulin-dependent (type 2) diabetes mellitus.
Tương Tác Thuốc :
  • Acetylsalicylic acid Acetylsalicylic acid increases the effect of sulfonylurea, glycodiazine.
  • Atenolol The beta-blocker, atenolol, may decrease symptoms of hypoglycemia.
  • Bisoprolol The beta-blocker, bisoprolol, may decrease symptoms of hypoglycemia.
  • Carvedilol The beta-blocker, carvedilol, may decrease symptoms of hypoglycemia.
  • Chloramphenicol Chloramphenicol may increase the effect of sulfonylurea, glycodiazine.
  • Clofibrate Clofibrate may increase the effect of sulfonylurea, glycodiazine.
  • Esmolol The beta-blocker, esmolol, may decrease symptoms of hypoglycemia.
  • Labetalol The beta-blocker, labetalol, may decrease symptoms of hypoglycemia.
  • Metoprolol The beta-blocker, metoprolol, may decrease symptoms of hypoglycemia.
  • Nadolol The beta-blocker, nadolol, may decrease symptoms of hypoglycemia.
  • Oxprenolol The beta-blocker, oxprenolol, may decrease symptoms of hypoglycemia.
  • Phenylbutazone Phenylbutazone increases the effect of the hypoglycemic agent
  • Pindolol The beta-blocker, pindolol, may decrease symptoms of hypoglycemia.
  • Propranolol The beta-blocker, propranolol, may decrease symptoms of hypoglycemia.
  • Rifampicin Rifampin may decrease the effect of sulfonylurea, glycodiazine.
  • Timolol The beta-blocker, timolol, may decrease symptoms of hypoglycemia.
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty : Bayer
    Sản phẩm biệt dược : Glycanol
  • Công ty : Bayer
    Sản phẩm biệt dược : Glyconormal
  • Công ty : Schering
    Sản phẩm biệt dược : Gondafon
  • Công ty : Bayer
    Sản phẩm biệt dược : Lycanol
  • Công ty : Bayer
    Sản phẩm biệt dược : Redul
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01382
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=9565
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507076
ChemSpider
http://www.chemspider.com/Chemical-Structure.9190.html
PharmGKB
http://www.pharmgkb.org/drug/PA164748839
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