Tìm theo
Tofisopam
Các tên gọi khác (2) :
  • Emandaxin
  • Tofizopam
Thuốc điều trị về tâm thần
Thuốc Gốc
Small Molecule
CAS: 22345-47-7
ATC: N05BA23
CTHH: C22H26N2O4
PTK: 382.4528
Tofisopam (marketed under brand names Emandaxin and Grandaxin) is a 2,3-benzodiazepine drug which is a benzodiazepine derivative. In contrast to classical 1,4-benzodiazepines, the compound does not bind to the benzodiazepine binding site of the gamma-aminobutyric acid receptor and its psychopharmacological profile differs from such compounds. Although Tofisopam is not approved for sale in North America, it is approved for use in various countries worldwide, including parts of Europe. The D-enantiomer (dextofisopam) is currently in phase II trials in the U.S. for the treatment of irritable bowel syndrome.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C22H26N2O4
Phân tử khối
382.4528
Monoisotopic mass
382.18925733
InChI
InChI=1S/C22H26N2O4/c1-7-15-13(2)23-24-22(14-8-9-18(25-3)19(10-14)26-4)17-12-21(28-6)20(27-5)11-16(15)17/h8-12,15H,7H2,1-6H3
InChI Key
InChIKey=RUJBDQSFYCKFAA-UHFFFAOYSA-N
IUPAC Name
1-(3,4-dimethoxyphenyl)-5-ethyl-7,8-dimethoxy-4-methyl-5H-2,3-benzodiazepine
Traditional IUPAC Name
tofisopam
SMILES
CCC1C2=CC(OC)=C(OC)C=C2C(=NN=C1C)C1=CC(OC)=C(OC)C=C1
Độ tan chảy
156.5 °C
Độ hòa tan
2.39e-03 g/l
logP
3.83
logS
-5.2
pKa (Strongest Basic)
-2.2
PSA
61.64 Å2
Refractivity
109.03 m3·mol-1
Polarizability
42.14 Å3
Rotatable Bond Count
6
H Bond Acceptor Count
6
H Bond Donor Count
0
Physiological Charge
0
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
MDDR-Like Rule
true
Dược Lực Học : Like other benzodiazepines, tofisopam possesses anxiolytic properties but unlike other benzodiazepines it does not have anticonvulsant, sedative, skeletal muscle relaxant, motor skill-impairing or amnestic properties. While it may not be an anticonvulsant in and of itself, it has been shown to enhance the anticonvulsant action of classical 1,4-benzodiazepines such as diazepam (but not sodium valproate, carbamazepine, phenobarbital, or phenytoin).
Cơ Chế Tác Dụng : Tofisopam (marketed under brand names Emandaxin and Grandaxin) is a 2,3-benzodiazepine drug which is a benzodiazepine derivative. In contrast to classical 1,4-benzodiazepines, the compound does not bind to the benzodiazepine binding site of the gamma-aminobutyric acid receptor and its psychopharmacological profile differs from such compounds. Although Tofisopam is not approved for sale in North America, it is approved for use in various countries worldwide, including parts of Europe. The D-enantiomer (dextofisopam) is currently in phase II trials in the U.S. for the treatment of irritable bowel syndrome. Tofisopam does not bind to the benzodiazepine binding site of the gamma-aminobutyric acid receptor. One study (Rundfeldt C. et al.) has shown that tofisopam acts as an isoenzyme-selective inhibitor of phosphodiesterases (PDEs) with highest affinity to PDE-4A1 (0.42 μM) followed by PDE-10A1 (0.92 μM), PDE-3 (1.98 μM) and PDE-2A3 (2.11 μM).
Dược Động Học :

▧ Metabolism :
Hepatic.
▧ Half Life :
6-8 hours
Độc Tính : The onset of impairment of consciousness is relatively rapid in benzodiazepine poisoning. Onset is more rapid following larger doses and with agents of shorter duration of action. The most common and initial symptom is somnolence. This may progress to coma (Grade I or Grade II) following very large ingestions. Oral, rat LD50 is 825 mg/kg.
Chỉ Định : For the treatment of anxiety and alcohol withdrawal.
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Emandaxin
  • Công ty :
    Sản phẩm biệt dược : Grandaxin
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB08811
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D01254
PharmGKB
http://www.pharmgkb.org/drug/PA165958428
Wikipedia
http://en.wikipedia.org/wiki/Tofisopam
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