Neuropharmacological screening of two 1,5-benzodiazepine compounds in mice

被引：18

作者：

Ben-Cherif, Wafa ^{[1
]}

Gharbi, Rafik ^{[2
]}

Sebai, Hichem ^{[3
]}

Dridi, Dorra ^{[1
]}

Boughattas, Naceur A. ^{[1
]}

Ben-Attia, Mossadok ^{[3
]}

机构：

[1] Fac Med Monastir, Pharmacol Lab, Monastir 5019, Tunisia

[2] Fac Sci Monastir, Lab Synth Heterocycl & Subst Nat, Monastir 5019, Tunisia

[3] Fac Sci Bizerte, Lab Biosurveillance Environm, Zarzouna 7021, Tunisia

来源：

COMPTES RENDUS BIOLOGIES | 2010年 / 333卷 / 03期

关键词：

1,5-Benzodiazepine; Hypnotic activity; Anticonvulsant activity; Mice; BENZODIAZEPINE-RECEPTOR LIGANDS; PHARMACOLOGICAL EVALUATION; ANTICONVULSANT ACTIVITY; DERIVATIVES; AGONIST; HETEROARENOBENZODIAZEPINES; PROFILE; DESIGN;

D O I：

10.1016/j.crvi.2009.09.015

中图分类号：

Q [生物科学];

学科分类号：

07 ; 0710 ; 09 ;

摘要：

This work investigates whether the two 1,5-benzodiazepine compounds: 4-(2-hydroxyphenyl)-1,5-benzodiazepin-2-one (RG0501) and Benzopyrano [4,3-c] 1,5-benzodiazepine (RG0502) have any neuropharmacological activities. Diazepam and Flunitrazepam were used as drug references. The investigational 1,5-BDZ were tested in vivo for potentiating hexobarbital-induced sleep and pentylenetetrazole (PTZ)-induced seizures. Our study demonstrated that the increase of sleep duration was significantly higher with RG0501 as compared to RG0502. However, RG0502 anticonvulsant effect was more pronounced than that of RG0501 in the range dose of 6.25-37.5 mg.kg(-1). From the 50 mg.kg(-1) dose, RG0502 offered a protection against clonic-tonic seizures as well as lethality (p <= 0.05). The results showed that the required doses to obtain a pharmacological activity were more than those of the references. This difference could be related to the lack of specific substituants responsible for the pharmacological activity in the tested compounds. (C) 2009 Academie des sciences. Published by Elsevier Masson SAS. All rights reserved.

引用

页码：214 / 219

页数：6

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