Talampanel (BioDeep_00000009499)

   


代谢物信息卡片


Talampanel

化学式: C19H19N3O3 (337.1426)
中文名称: (8R)-7-乙酰基-5-(4-氨基苯基)-8,9-二氢-8-甲基-7H-1,3-二氧杂环戊烯并[4,5-H][2,3]苯并二氮杂卓
谱图信息: 最多检出来源 () 0%

分子结构信息

SMILES: CC(=O)N1N=C(c2ccc(N)cc2)c2cc3c(cc2CC1C)OCO3
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

描述信息

C78272 - Agent Affecting Nervous System > C47795 - CNS Stimulant
Same as: D02696
Talampanel (LY300164) is an orally and selective α-amino-3-hydroxy-5-methyl-4-isoxazolepropionate (AMPA) receptor antagonis with anti-seizure activity[1]. Talampanel (IVAX) has neuroprotective effects in rodent stroke models[2]. Talampanel attenuates caspase-3 dependent apoptosis in mouse brain[2].

同义名列表

5 个代谢物同义名

Talampanel; Gyki 53405; GYKI-53773; LY-300164; Talampanel



数据库引用编号

13 个数据库交叉引用编号

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代谢反应

0 个相关的代谢反应过程信息。

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在这里通过桑基图来展示出与当前的这个代谢物在我们的BioDeep知识库中具有相关联信息的其他代谢物。在这里进行关联的信息来源主要有:

  • PubMed: 来源于PubMed文献库中的文献信息,我们通过自然语言数据挖掘得到的在同一篇文献中被同时提及的相关代谢物列表,这个列表按照代谢物同时出现的文献数量降序排序,取前10个代谢物作为相关研究中关联性很高的代谢物集合展示在桑基图中。
  • NCBI Taxonomy: 通过文献数据挖掘,得到的代谢物物种来源信息关联。这个关联信息同样按照出现的次数降序排序,取前10个代谢物作为高关联度的代谢物集合展示在桑吉图上。
  • Chemical Taxonomy: 在物质分类上处于同一个分类集合中的其他代谢物
  • Chemical Reaction: 在化学反应过程中,存在为当前代谢物相关联的生化反应过程中的反应底物或者反应产物的关联代谢物信息。

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亚细胞结构定位 关联基因列表
Cytoplasm 5 CA1, CASP3, GFAP, NAT2, SOD1
Endoplasmic reticulum membrane 2 CD4, GRIA1
Nucleus 3 CASP3, NAT2, SOD1
cytosol 6 CA1, CASP3, GFAP, GRIA1, NAT2, SOD1
dendrite 4 GRIA1, GRIA2, GRIA4, HTR1A
nucleoplasm 3 CASP3, GRIK5, SOD1
Cell membrane 10 CD4, GRIA1, GRIA2, GRIA3, GRIA4, GRID1, GRIK1, GRIK5, HTR1A, NAT2
Early endosome membrane 1 GRIA1
Multi-pass membrane protein 9 GRIA1, GRIA2, GRIA3, GRIA4, GRID1, GRIK1, GRIK5, HTR1A, NAT2
Synapse 3 GRIA1, HTR1A, NPS
cell surface 1 GRIA1
dendritic shaft 1 GRIA1
glutamatergic synapse 4 CASP3, GHRL, GRIA1, GRID1
Golgi apparatus 1 GDNF
Golgi membrane 1 INS
neuromuscular junction 1 GRIA1
neuronal cell body 6 CASP3, GRIA1, GRIA2, GRIA4, NAT2, SOD1
postsynapse 2 GHRL, GRIA2
presynaptic membrane 2 GRIK1, GRIK5
Presynapse 1 GRIA1
plasma membrane 10 CD4, GRIA1, GRIA2, GRIA3, GRIA4, GRID1, GRIK1, GRIK5, HTR1A, NAT2
synaptic vesicle membrane 1 GRIA1
Membrane 5 GRIA1, GRIA2, GRIA4, GRIK5, NAT2
axon 2 GHRL, NAT2
basolateral plasma membrane 1 NAT2
extracellular exosome 4 CA1, GRID1, NAT2, SOD1
endoplasmic reticulum 1 GRIK5
extracellular space 6 CSF3, GDNF, GHRL, INS, PTH, SOD1
lysosomal lumen 1 CSF3
Schaffer collateral - CA1 synapse 1 GHRL
mitochondrion 1 SOD1
protein-containing complex 1 SOD1
intracellular membrane-bounded organelle 1 GRIK1
postsynaptic density 3 CASP3, GRIA1, GRIA2
Single-pass type I membrane protein 1 CD4
Secreted 4 CSF3, GDNF, GHRL, INS
extracellular region 7 CSF3, GDNF, GHRL, INS, NPS, PTH, SOD1
astrocyte end-foot 1 GFAP
excitatory synapse 2 GRIA1, GRIA2
hippocampal mossy fiber to CA3 synapse 1 GRIK5
neuronal cell body membrane 1 GRIA1
mitochondrial matrix 1 SOD1
transcription regulator complex 1 NAT2
external side of plasma membrane 3 CD4, GRIA1, GRIA2
Extracellular vesicle 1 GRIA4
dendritic spine 4 GRIA1, GRIA2, GRIA3, GRIA4
neuronal dense core vesicle lumen 1 GHRL
cytoplasmic vesicle 1 SOD1
axon cytoplasm 1 SOD1
neuron spine 1 GRIA1
Early endosome 1 CD4
cell-cell junction 1 GRIA1
recycling endosome 1 GRIA1
postsynaptic membrane 6 GRIA1, GRIA2, GRIA3, GRIA4, GRID1, GRIK1
presynaptic active zone membrane 1 GRIA1
Membrane raft 1 CD4
GABA-ergic synapse 1 GRID1
Peroxisome 1 SOD1
Cell projection, dendritic spine 1 GRIA1
mitochondrial intermembrane space 1 SOD1
intermediate filament 1 GFAP
Postsynaptic cell membrane 7 GRIA1, GRIA2, GRIA3, GRIA4, GRID1, GRIK1, GRIK5
dendrite cytoplasm 1 SOD1
kainate selective glutamate receptor complex 2 GRIK1, GRIK5
cell projection 2 GFAP, GRIK5
postsynaptic density, intracellular component 1 GRIA1
Recycling endosome membrane 1 GRIA1
endosome lumen 1 INS
AMPA glutamate receptor complex 4 GRIA1, GRIA2, GRIA3, GRIA4
Cell projection, dendrite 3 GRIA1, GRIA4, HTR1A
Presynaptic cell membrane 1 GRIK5
cell body 1 GFAP
intermediate filament cytoskeleton 1 GFAP
synaptic membrane 1 GRIA1
secretory granule lumen 2 GHRL, INS
Golgi lumen 1 INS
endoplasmic reticulum lumen 3 CD4, GHRL, INS
endocytic vesicle membrane 4 GRIA1, GRIA2, GRIA3, GRIA4
transport vesicle 1 INS
Endoplasmic reticulum-Golgi intermediate compartment membrane 2 GRIA1, INS
postsynaptic density membrane 7 GRIA1, GRIA2, GRIA3, GRIA4, GRID1, GRIK1, GRIK5
postsynaptic endocytic zone 1 GRIA2
ER to Golgi transport vesicle membrane 1 GRIA1
parallel fiber to Purkinje cell synapse 1 GRIA3
clathrin-coated endocytic vesicle membrane 1 CD4
external side of apical plasma membrane 1 NAT2
death-inducing signaling complex 1 CASP3
dendritic spine membrane 1 GRIA1
cytoplasmic side of lysosomal membrane 1 GFAP
endocytic vesicle lumen 1 CSF3
T cell receptor complex 1 CD4
asymmetric synapse 1 GRIA2
proximal dendrite 1 GRIA1
NatA complex 1 NAT2
axonal spine 1 GRIA1
perisynaptic space 1 GRIA1


文献列表

  • Robert M Pascuzzi, Jeremy Shefner, Amy S Chappell, John S Bjerke, Roy Tamura, Vinay Chaudhry, Lora Clawson, Lisa Haas, Jeffrey D Rothstein. A phase II trial of talampanel in subjects with amyotrophic lateral sclerosis. Amyotrophic lateral sclerosis : official publication of the World Federation of Neurology Research Group on Motor Neuron Diseases. 2010 May; 11(3):266-71. doi: 10.3109/17482960903307805. [PMID: 19961264]
  • P Buchwald, A Juhász, C Bell, M Pátfalusi, P Kovács, G Hochhaus, J Howes, N Bodor. Influence of the N-acetylation polymorphism on the metabolism of talampanel: an investigation in fasted and fed subjects genotyped for NAT2 variants. Die Pharmazie. 2006 Feb; 61(2):125-34. doi: . [PMID: 16526560]
  • Peter Buchwald, Attila Juhász, Cynthia Bell, Márta Pátfalusi, John Howes, Nicholas Bodor. Unified pharmacogenetics-based parent-metabolite pharmacokinetic model incorporating acetylation polymorphism for talampanel in humans. Journal of pharmacokinetics and pharmacodynamics. 2005 Aug; 32(3-4):377-400. doi: 10.1007/s10928-005-0001-y. [PMID: 16320099]
  • K K Borowicz, M Swiader, M Wielosz, S J Czuczwar. Influence of the combined treatment of LY 300164 (an AMPA/kainate receptor antagonist) with adenosine receptor agonists on the electroconvulsive threshold in mice. European neuropsychopharmacology : the journal of the European College of Neuropsychopharmacology. 2004 Oct; 14(5):407-12. doi: 10.1016/j.euroneuro.2003.12.003. [PMID: 15336302]
  • Yvonne M Langan, Richard Lucas, Haley Jewell, N Toublanc, H Schaefer, Josemir W A S Sander, Philip N Patsalos. Talampanel, a new antiepileptic drug: single- and multiple-dose pharmacokinetics and initial 1-week experience in patients with chronic intractable epilepsy. Epilepsia. 2003 Jan; 44(1):46-53. doi: 10.1046/j.1528-1157.2003.128902.x. [PMID: 12581229]
  • K K Borowicz, M Swiader, W Zgrajka, C Sawulski, W A Turski, S J Czuczwar. Influence of several convulsants on the protective activity of a non-competitive AMPA/kainate antagonist, LY 300164, and lamotrigine against maximal electroshock in mice. Journal of physiology and pharmacology : an official journal of the Polish Physiological Society. 2002 Dec; 53(4 Pt 2):859-69. doi: . [PMID: 12510869]
  • Mariusz Swiader, Kinga K Borowicz, Jacek Porebiak, Zdzisław Kleinrok, Stanisław J Czuczwar. Influence of agents affecting voltage-dependent calcium channels and dantrolene on the anticonvulsant action of the AMPA/kainate receptor antagonist LY 300164 in mice. European neuropsychopharmacology : the journal of the European College of Neuropsychopharmacology. 2002 Aug; 12(4):311-9. doi: 10.1016/s0924-977x(02)00045-7. [PMID: 12126870]
  • K K Borowicz, Z Kleinrok, S J Czuczwar. The AMPA/kainate receptor antagonist, LY 300164, increases the anticonvulsant effects of diazepam. Naunyn-Schmiedeberg's archives of pharmacology. 2000 Jun; 361(6):629-35. doi: 10.1007/s002100000237. [PMID: 10882038]
  • S J Czuczwar, M Swiader, H Kuźniar, M Gasior, Z Kleinrok. LY 300164, a novel antagonist of AMPA/kainate receptors, potentiates the anticonvulsive activity of antiepileptic drugs. European journal of pharmacology. 1998 Oct; 359(2-3):103-9. doi: 10.1016/s0014-2999(98)00632-3. [PMID: 9832379]
  • D Bleakman, B A Ballyk, D D Schoepp, A J Palmer, C P Bath, E F Sharpe, M L Woolley, H R Bufton, R K Kamboj, I Tarnawa, D Lodge. Activity of 2,3-benzodiazepines at native rat and recombinant human glutamate receptors in vitro: stereospecificity and selectivity profiles. Neuropharmacology. 1996; 35(12):1689-702. doi: 10.1016/s0028-3908(96)00156-6. [PMID: 9076748]
  • J A Eckstein, S P Swanson. Determination of a novel alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionate receptor antagonist (LY300164) and its N-acetyl metabolite in mouse, rat, dog, and monkey plasma using high-performance liquid chromatography with ultraviolet detection. Journal of chromatography. B, Biomedical applications. 1995 Jun; 668(1):153-8. doi: 10.1016/0378-4347(95)00058-q. [PMID: 7550972]