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

H Bond Acceptor Count

H Bond Donor Count

Physiological Charge

Number of Rings

Bioavailability

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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