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Avizafone dihydrobromide  (Synonyms: Pro-diazepam dihydrobromide)

目录号: HY-W702001
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Avizafone (Pro-diazepam) dihydrobromide 是地西泮的前体药物,具有抗惊厥作用。Avizafone dihydrobromide 可用作神经毒剂中毒的解毒剂。在体内,Avizafone dihydrobromide 可被氨基肽酶迅速水解,生成赖氨酸和地西泮。Avizafone dihydrobromide 的研究领域包括神经系统疾病,例如癫痫。

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Avizafone dihydrobromide

Avizafone dihydrobromide Chemical Structure

CAS No. : 60067-15-4

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Avizafone (Pro-diazepam) dihydrobromide, a pro-drug of Diazepam, is an anticonvulsant agent. Avizafone dihydrobromide can be used as an antidote of nerve agent poisoning. In vivo, Avizafone dihydrobromide is rapidly hydrolyzed by aminopeptidase to produce lysine and diazepam. Avizafone dihydrobromide has research areas including neurological disease, such as epilepsy[1][2][3].

药代动力学
(Parmacokinetics)[1]
Species Dose Route Indicator value
Monkey 0.7 μmol/Kg i.m. T1/2 (Absorption) 11.50 min
Monkey 0.7 μmol/Kg i.m. Tmax 29.78 min
Monkey 0.7 μmol/Kg i.m. Cmax 0.222122 μM
Monkey 0.7 μmol/Kg i.m. T1/2 (Elimination) 42.68 min
Monkey 0.7 μmol/Kg i.m. CLplasma 36.07 mL/min/kg
Monkey 1 μmol/Kg i.m. T1/2 (Absorption) 20.71 min
Monkey 1 μmol/Kg i.m. Tmax 37.32 min
Monkey 1 μmol/Kg i.m. Cmax 0.28265 μM
Monkey 1 μmol/Kg i.m. T1/2 (Elimination) 39.18 min
Monkey 1 μmol/Kg i.m. CLplasma 36.13 mL/min/kg
体内研究
(In Vivo)

Avizafone dihydrobromide (3.5 mg/kg;肌内注射;单次给药) 可预防 Charles River 豚鼠 (梭曼中毒) 的癫痫发作、减轻临床症状、消除 24 小时死亡率并缓解脑损伤 (24 小时死亡率为 0%)[2]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Guinea pigs (300-350 g)[2]
Dosage: 3.5 mg/kg
Administration: i.m.; single dose
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.
分子量

592.75

Formula

C22H29Br2ClN4O3

CAS 号
性状

固体

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

纯度 & 产品资料
参考文献
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  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Avizafone dihydrobromide
目录号:
HY-W702001
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