Anticonvulsant Activities of 7-phenyl-5H-thiazolo[5,4-e][1,2,3,4]tetrazolo[5,1-c]pyrrolo[1,2-a][1,4]diazepine and 7-phenyl-5H-thiazolo[5,4-e][1,3,4]triazolo[5,1-c] pyrrolo[1,2-a][1,4]diazepines

authors:

avatar Maryam Shekarchi 1 , avatar Marya Binesh Marvasti 1 , avatar Mohammad Sharifzadeh 2 , avatar Abbas Shafiee 1 , *

Department of Medicinal Chemistry and Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran, Iran
Department of Pharmacology and Toxicology, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran
Iranian Journal of Pharmaceutical Research: Vol.4, issue 1; 33-36
published online: November 20, 2010
article type: Research Article
received: May 01, 2004
accepted: July 01, 2005
DOI: https://doi.org/10.22037/ijpr.2010.614

how to cite: Shekarchi M, Binesh Marvasti M, Sharifzadeh M, Shafiee A. Anticonvulsant Activities of 7-phenyl-5H-thiazolo[5,4-e][1,2,3,4]tetrazolo[5,1-c]pyrrolo[1,2-a][1,4]diazepine and 7-phenyl-5H-thiazolo[5,4-e][1,3,4]triazolo[5,1-c] pyrrolo[1,2-a][1,4]diazepines. Iran J Pharm Res. 2005;4(1):e128224. https://doi.org/10.22037/ijpr.2010.614.

Abstract

Anticonvulsant activity of 7-phenyl-5H-thiazolo[5,4-e][1,2,3,4]tetrazolo[5,1-c]pyrrolo[1,2-a][1,4]diazepine (5) and 7-phenyl-5H-thiazolo[5,4-e][1,3,4]triazolo[5,1-c]pyrrolo[1,2-a][1,4]diazepines (6a-d) was measured against pentylenetetrazole (PTZ)-induced seizures in mice. Intraperitoneal injections of different doses (12.5, 25 and 50 mg/kg, i.p.) of test compounds decreased PTZ-induced seizure significantly in a dose-dependent manner.The test compounds were administered 30 min befor PTZ (80 mg/kg, i.p.) injection. The maximum response was obtained with 50 mg/kg of compound 6d that showed more anticonvulsant activity compared to diazepam (0.5 mg/kg). The frequency of mortality was also decreased by all listed compounds. Pretreatment of animals with flumazenile (as a benzodiazepine, BDZ receptor antagonist) decreased, but not completely inhibited the anticonvulsant activity of compound 6d (50 mg/kg). These results indicate that besides BZD receptors, other neurotransmitter systems may be involved in anticonvulsant activity of the tested compounds.