Tìm theo
Progabide
Các tên gọi khác (4 ) :
  • Halogabide
  • Progabida
  • Progabide
  • Progabidum
Thuốc chống Parkinson
Thuốc Gốc
Small Molecule
CAS: 62666-20-0
ATC: N03AG05
CTHH: C17H16ClFN2O2
PTK: 334.773
Progabide is an analog and prodrug of gamma-aminobutyric acid. It is commonly used in the treatment of epilepsy. It has agonistic activity for both the GABAA and GABAB receptors. Progabide has been investigated for many diseases besides epilepsy, including Parkinson's disease, schizophrenia, clinical depression and anxiety disorder with varying success.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C17H16ClFN2O2
Phân tử khối
334.773
Monoisotopic mass
334.088433678
InChI
InChI=1S/C17H16ClFN2O2/c18-12-5-3-11(4-6-12)17(21-9-1-2-16(20)23)14-10-13(19)7-8-15(14)22/h3-8,10,21H,1-2,9H2,(H2,20,23)/b17-14+
InChI Key
InChIKey=DWEQWXSKOHHBNT-SAPNQHFASA-N
IUPAC Name
4-{[(4-chlorophenyl)[(1E)-3-fluoro-6-oxocyclohexa-2,4-dien-1-ylidene]methyl]amino}butanamide
Traditional IUPAC Name
progabide
SMILES
NC(=O)CCCN\C(C1=CC=C(Cl)C=C1)=C1/C=C(F)C=CC1=O
Độ tan chảy
133-135 °C
Độ hòa tan
70.9 mg/L
logP
3.06
logS
-4.9
pKa (strongest acidic)
15.32
pKa (Strongest Basic)
4.01
PSA
72.19 Å2
Refractivity
91.22 m3·mol-1
Polarizability
33.21 Å3
Rotatable Bond Count
6
H Bond Acceptor Count
3
H Bond Donor Count
2
Physiological Charge
0
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Progabide, a fatty acid derivative, is a GABA receptor agonist used to treat the symptoms of epilepsy.
Cơ Chế Tác Dụng : Progabide is an analog and prodrug of gamma-aminobutyric acid. It is commonly used in the treatment of epilepsy. It has agonistic activity for both the GABAA and GABAB receptors. Progabide has been investigated for many diseases besides epilepsy, including Parkinson's disease, schizophrenia, clinical depression and anxiety disorder with varying success. Progabide binds to both GABAA and GABAB receptors located on the terminals of primary afferent fibers. Binding to GABAA results in an increased affinity of the GABA receptor for the amino acid, an augmented flux of chloride ions across the terminal membrane, and an increase in the amount of presynaptic inhibition. Activation of the GABAB receptors retards the influx of calcium ions into the terminals, thereby reducing the evoked release of excitatory amino acids and possibly other transmitters.
Dược Động Học :
▧ Absorption :
Well absorbed with a bioavailability of 60%
▧ Protein binding :
95%
▧ Metabolism :
Hepatic
▧ Half Life :
4 hours
Chỉ Định : Indicated for the treatment of epilepsy.
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Gabren
  • Công ty : Sanofi S.A.
    Sản phẩm biệt dược : Gabrene
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00837
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=5361323
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506568
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D05621
ChemSpider
http://www.chemspider.com/Chemical-Structure.4514729.html
PharmGKB
http://www.pharmgkb.org/drug/PA164747990
Wikipedia
http://en.wikipedia.org/wiki/Progabide
... loading
... loading