New 2,3-Benzodiazepine Derivative : Synthesis, Activity on Central Nervous System, and Toxicity Study in Mice

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Amaghnouje , A , Bohza , S , Bohdan , N , Es-Safi , I , Kyrylchuk , A , Achour , S , El Fatemi , H , Bousta , D & Grafov , A 2021 , ' New 2,3-Benzodiazepine Derivative : Synthesis, Activity on Central Nervous System, and Toxicity Study in Mice ' , Pharmaceuticals , vol. 14 , no. 8 , 814 . https://doi.org/10.3390/ph14080814

Title: New 2,3-Benzodiazepine Derivative : Synthesis, Activity on Central Nervous System, and Toxicity Study in Mice
Author: Amaghnouje, Amal; Bohza, Serhii; Bohdan, Nathalie; Es-Safi, Imane; Kyrylchuk, Andrii; Achour, Sanae; El Fatemi, Hinde; Bousta, Dalila; Grafov, Andriy
Contributor: University of Helsinki, Department of Chemistry
Date: 2021-08
Language: eng
Number of pages: 13
Belongs to series: Pharmaceuticals
ISSN: 1424-8247
URI: http://hdl.handle.net/10138/334203
Abstract: We report the design and synthesis of a new diazepine derivative, 4-(4-methoxyphenyl)-2,3,4,5-tetrahydro-2,3-benzodiazepin-1-one (VBZ102), and the evaluation of its anxiolytic-like profile, memory impairment effect, and toxicity in Swiss mice. VBZ102 was evaluated for central nervous system effects in an open field, light-dark box, and novel object recognition tests under oral administration for acute and sub-acute treatment. We tested the VBZ102 toxicity in mice through a determination of LD50 values and examination of the biochemical and histopathological parameters. The VBZ102 induced an anxiolytic effect at different doses both in the light-dark box and open field tests. Unlike other benzodiazepines (e.g., bromazepam), a sedative effect was noted only after administration of the VBZ102 at 10.0 mg/kg.
Subject: benzodiazepines
central nervous system
mouse behavioral model
toxicity
OPEN-FIELD TEST
BIOCHEMICAL PARAMETERS
AMPA RECEPTORS
BENZODIAZEPINES
RECOGNITION
BEHAVIOR
ANXIETY
MEMORY
MODEL
DRUG
317 Pharmacy
116 Chemical sciences
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