Tìm theo
Talampanel
Thuốc điều trị ung thư
Thuốc Gốc
Small Molecule
CAS: 161832-65-1
CTHH: C19H19N3O3
PTK: 337.3725
Talampanel is a substance that is being studied in the treatment of brain tumors and other brain disorders, such as epilepsy and Parkinson disease. It is a type of AMPA receptor antagonist.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C19H19N3O3
Phân tử khối
337.3725
Monoisotopic mass
337.142641489
InChI
InChI=1S/C19H19N3O3/c1-11-7-14-8-17-18(25-10-24-17)9-16(14)19(21-22(11)12(2)23)13-3-5-15(20)6-4-13/h3-6,8-9,11H,7,10,20H2,1-2H3/t11-/m1/s1
InChI Key
InChIKey=JACAAXNEHGBPOQ-LLVKDONJSA-N
IUPAC Name
1-[(13R)-10-(4-aminophenyl)-13-methyl-4,6-dioxa-11,12-diazatricyclo[7.5.0.0^{3,7}]tetradeca-1(9),2,7,10-tetraen-12-yl]ethan-1-one
Traditional IUPAC Name
1-[(13R)-10-(4-aminophenyl)-13-methyl-4,6-dioxa-11,12-diazatricyclo[7.5.0.0^{3,7}]tetradeca-1(9),2,7,10-tetraen-12-yl]ethanone
SMILES
C[C@@H]1CC2=CC3=C(OCO3)C=C2C(=NN1C(C)=O)C1=CC=C(N)C=C1
Độ hòa tan
1.26e-01 g/l
logP
2.33
logS
-3.4
pKa (Strongest Basic)
3.38
PSA
77.15 Å2
Refractivity
94.65 m3·mol-1
Polarizability
36.34 Å3
Rotatable Bond Count
1
H Bond Acceptor Count
5
H Bond Donor Count
1
Physiological Charge
0
Number of Rings
4
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Talampanel, a potent and selective alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionate (AMPA)-receptor antagonist, is a potential new antiepileptic drug (AED). Talampanel dosing strategies may be reliant on concomitant AED medication, as enzyme-inducing AEDs enhance, whereas VPA inhibits its metabolism. Talampanel was well tolerated, although adverse events occurred at lower doses compared with those in healthy subjects, probably because of the additive effect of concomitant AEDs.
Cơ Chế Tác Dụng : Talampanel is a substance that is being studied in the treatment of brain tumors and other brain disorders, such as epilepsy and Parkinson disease. It is a type of AMPA receptor antagonist. Talampanel is a potent noncompetitive and selective antagonist of the glutamine AMPA receptors. Studies in primates have shown that the administration of talampanel to parkinsonian monkeys significantly decreased levodopa-induced dyskinesias by 40%. When given alone, talampanel did not modify the severity of parkinsonian symptoms. However, in combination with levodopa, talampanel potentiated the antiparkinsonian action of levodopa by increasing motor activity.
Dược Động Học :
▧ Absorption :
Rapidly absorbed, with maximal plasma concentrations achieved within 1-3 hours.
▧ Half Life :
3-6 hours
Chỉ Định : For the treatment of epilepsy.
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Ampanel
  • Công ty :
    Sản phẩm biệt dược : Kinampa
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB04982
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=164509
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=10255482
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C13670
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D02696
ChemSpider
http://www.chemspider.com/Chemical-Structure.144217.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50173337
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