Tìm theo
Phenformin
Các tên gọi khác (6 ) :
  • DBI
  • Fenformin
  • Fenformina
  • Phenformine
  • Phenforminum
  • β-Phenethybiguanide
Insulin và nhóm Thuốc hạ đường huyết
Thuốc Gốc
Small Molecule
CAS: 114-86-3
ATC: A10BA01
CTHH: C10H15N5
PTK: 205.2596
A biguanide hypoglycemic agent with actions and uses similar to those of metformin. Although it is generally considered to be associated with an unacceptably high incidence of lactic acidosis, often fatal, it is still available in some countries. (From Martindale, The Extra Pharmacopoeia, 30th ed, p290)
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C10H15N5
Phân tử khối
205.2596
Monoisotopic mass
205.132745505
InChI
InChI=1S/C10H15N5/c11-9(12)15-10(13)14-7-6-8-4-2-1-3-5-8/h1-5H,6-7H2,(H6,11,12,13,14,15)
InChI Key
InChIKey=ICFJFFQQTFMIBG-UHFFFAOYSA-N
IUPAC Name
1-carbamimidamido-N-(2-phenylethyl)methanimidamide
Traditional IUPAC Name
phenformin
SMILES
NC(=N)NC(=N)NCCC1=CC=CC=C1
Độ tan chảy
176.5 °C
Độ hòa tan
210 mg/mL
logP
-0.83
logS
-3
pKa (Strongest Basic)
11.97
PSA
97.78 Å2
Refractivity
80.72 m3·mol-1
Polarizability
22.14 Å3
Rotatable Bond Count
3
H Bond Acceptor Count
5
H Bond Donor Count
5
Physiological Charge
2
Number of Rings
1
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Used to treat diabetes, phenformin is a biguanide (contains 2 guanidino groups) hypoglycemic agent with actions and uses similar to those of metformin (Glucophage). Both drugs work by (1) decreasing the absorption of glucose by the intestines, (2) decreasing the production of glucose in the liver, and by (3) increasing the body's ability to use insulin more effectively. More specifically, phenformin improves glycemic control by improving insulin sensitivity. Phenformin is generally considered to be associated with an unacceptably high incidence of actic acidosis. In general biguanides should be used only in stable type II diabetics who are free of liver, kidney and cardiovascular problems and who cannot be controlled with diet.
Cơ Chế Tác Dụng : A biguanide hypoglycemic agent with actions and uses similar to those of metformin. Although it is generally considered to be associated with an unacceptably high incidence of lactic acidosis, often fatal, it is still available in some countries. (From Martindale, The Extra Pharmacopoeia, 30th ed, p290) Phenformin binds to the AMP-activated protein kinase (AMPK). AMPK is an ultra-sensitive cellular energy sensor that monitors energy consumption and down-regulates ATP-consuming processes when activated. The biguanide phenformin has been shown to independently decrease ion transport processes, influence cellular metabolism and activate AMPK. Phenformin's hypoglycemic activity is related the effect it has in activating AMPK and fooling insulin sensitive cells into thinking that insulin levels are low and causing the body to use glucose as if in a state of low caloric consumption. This drug also seems to inhibit several varients of ATP-sensitive potassium channels (namely the receptor subtype Kir6.1).
Chỉ Định : For the reatment of type II diabetes mellitus.
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty : Ciba-Geigy
    Sản phẩm biệt dược : DBI
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00914
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=8249
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505230
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07673
ChemSpider
http://www.chemspider.com/Chemical-Structure.7953.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50240908
PharmGKB
http://www.pharmgkb.org/drug/PA1000
Wikipedia
http://en.wikipedia.org/wiki/Phenformin
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