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Avizafone dihydrobromide  (Synonyms: Pro-diazepam dihydrobromide)

Cat. No.: HY-W702001
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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.

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Avizafone dihydrobromide

Avizafone dihydrobromide Chemical Structure

CAS No. : 60067-15-4

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Description

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].

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

Avizafone dihydrobromide (3.5 mg/kg; i.m.; single dose) prevents seizures, reduces clinical signs, eliminates 24-hour mortality, and mitigates brain lesions in Charles River guinea pigs (soman poisoned) (with a 24-hour mortality rate of 0%)[2].

MedChemExpress (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.
Masse moléculaire

592.75

Formule

C22H29Br2ClN4O3

CAS No.
Appearance

Solid

SMILES

O=C(CNC([C@H](CCCCN)N)=O)N(C1=CC=C(C=C1C(C2=CC=CC=C2)=O)Cl)C.Br.Br

Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

4°C, sealed storage, away from moisture

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

Pureté et documentation
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    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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Nom du produit:
Avizafone dihydrobromide
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HY-W702001
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