Avizafone
Avizafone (Pro-diazepam), a pro-drug of Diazepam, is an anticonvulsant agent. Avizafone can be used as an antidote of nerve agent poisoning. In vivo, Avizafone is rapidly hydrolyzed by aminopeptidase to produce lysine and diazepam. Avizafone has research areas including neurological disease, such as epilepsy.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 65617-86-9
- 分子式: C22H27ClN4O3
- 分子量:430.93
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Guinea pigs (300-350 g)[2]
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Dosage:3.5 mg/kg
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Administration:i.m.; single dose
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Result:Reduced clinical sign severity to score 1 vs. 3 in controls, achieved 0% 24-hour mortality, prevented seizures in 0/8 animals, reduced necrosis to 3/8 animals vs. 4/4 in controls, eliminated perivascular cuffs and edema, prevented seizures in 0/8 animals vs. 4/8 with diazepam, eliminated brain lesions, and showed no significant respiratory parameter modifications.
化学情報
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CAS 番号 65617-86-9
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分子量 430.93
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分子式 C22H27ClN4O3
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SMILES
O=C(CNC([C@H](CCCCN)N)=O)N(C1=CC=C(C=C1C(C2=CC=CC=C2)=O)Cl)C
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別名
Pro-diazepam
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
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Research Protocol for Neurological Diseases
PINK1/Parkin-mediated mitophagy pathway is a mitochondrial quality-control signaling axis in which mitochondrial depolarization stabilizes PINK1 on damaged mitochondria, activates Parkin recruitment and E3 ubiquitin ligase activity, promotes ubiquitination of outer mitochondrial membrane proteins, recruits selective autophagy adaptors, and drives lysosomal degradation of damaged mitochondria. In neurological disease research, this pathway is experimentally important because neurons, especially dopaminergic neurons, are highly dependent on mitochondrial integrity, and defective mitochondrial turnover can lead to mitochondrial dysfunction, oxidative stress, impaired neuronal survival, α-synuclein accumulation, and neuroinflammatory damage-associated signals. The genetic disease link is strongest in Parkinson’s disease because mutations in PRKN/parkin cause autosomal recessive juvenile parkinsonism, mutations in PINK1 cause hereditary early-onset Parkinson’s disease, and Drosophila studie
純度とドキュメンテーション
参考文献
[1]. Clair P, et al. Stability study of a new antidote drug combination (Atropine-HI-6-Prodiazepam) for treatment of organophosphate poisoning. Eur J Pharm Sci. 2000 Jan;9(3):259-63. [Content Brief]
[2]. Lallement G, et al. Compared efficacy of diazepam or avizafone to prevent soman-induced electroencephalographic disturbances and neuropathology in primates: relationship to plasmatic benzodiazepine pharmacokinetics. Arch Toxicol. 2000 Oct;74(8):480-6. [Content Brief]
[3]. Taysse L, et al. Protection against soman-induced neuropathology and respiratory failure: a comparison of the efficacy of diazepam and avizafone in guinea pig. Toxicology. 2006;225(1):25-35. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)