Molecular requirement for anticonvulsant activity in a series of thiazolo-1,4-benzodiazepine derivatives and comparison with classical benzodiazepines

General Pharmacology
G B DeSarroA DeSarro


1. The behavioural and anticonvulsant effects of several thiazolo[3,2-d][1,4]benzodiazepines (TBZ) were studied after intraperitoneal administration in DBA/2 mice, a strain genetically susceptible to sound-induced seizures. 2. Anticonvulsant effects on seizures evoked by means of auditory stimulation (109 dB, 12-16 kHz) were evaluated in DBA/2 mice placed singly under a perspex dome. 3. Hypothermic activity was observed after the highest doses of the benzodiazepines studied. 4. In addition, some TBZ were examined for anticonvulsant properties with respect to clonus induced by pentylenetetrazol. 5. Our study demonstrated that some thiazolobenzodiazepine derivatives were more potent than clobazam, desmethylclobazam and chlordiazepoxide, and less potent than diazepam, desmethyldiazepam and alprazolam. 6. In the series of tricyclic benzodiazepines, thiazole nucleus fusion to the "d" edge of the 7-membered ring results in an effective increase of the energy barrier for the heptatomic system reversal, and is probably responsible for, jointly with the lack of C=N double bonds, lower activity with respect to the 1,4-benzodiazepine precursors. 7. The potency of various thiazolobenzodiazepine derivatives as inhibitors of specific [3H]flu...Continue Reading


Oct 1, 1979·Pharmacology, Biochemistry, and Behavior·C A KlepnerB Beer
Dec 1, 1989·Neuron·M KhrestchatiskyA J Tobin
Sep 1, 1987·Neuropharmacology·G B De SarroG Nistico
Sep 1, 1987·Brain Research Bulletin·A G ChapmanB S Meldrum
Mar 1, 1985·Epilepsia·T N Seyfried, G H Glaser
Feb 1, 1980·The Journal of Pharmacy and Pharmacology·S CacciaS Garattini
Jul 17, 1980·Nature·W Sieghart, M Karobath
Dec 3, 1981·European Journal of Pharmacology·H A RobertsonI L Martin
Jun 11, 1982·Science·C BraestrupE N Petersen
Jan 6, 1983·Nature·L Prado de CarvalhoJ Rossier
Aug 15, 1983·Biochemical Pharmacology·F J EhlertH I Yamamura
Jan 1, 1983·Advances in Biochemical Psychopharmacology·C BraestrupT Honoré
Dec 1, 1983·Neuropharmacology·C A BoastK M Bergen
Mar 23, 1984·European Journal of Pharmacology·L TollG Loew
Jun 1, 1982·Neuropharmacology·N R Oakley, B J Jones


Sep 1, 1996·General Pharmacology·G De SarroA De Sarro
Sep 1, 1997·Pharmacology, Biochemistry, and Behavior·G De SarroA De Sarro
Dec 1, 1993·Bioorganic & Medicinal Chemistry·F CampagnaG B De Sarro
Jul 14, 2001·Indian Journal of Pediatrics·V JainS Singhi
Jun 15, 2012·Archiv der Pharmazie·Awatef A FaragSamir Y Abbas

Related Concepts

Acoustic Stimulation
Injections, Intraperitoneal
Mice, Inbred DBA
Non-epileptic Convulsion

Trending Feeds


Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.

Alzheimer's Disease: MS4A

Variants within the membrane-spanning 4-domains subfamily A (MS4A) gene cluster have recently been implicated in Alzheimer's disease in genome-wide association studies. Here is the latest research on Alzheimer's disease and MS4A.

Pediculosis pubis

Pediculosis pubis is a disease caused by a parasitic insect known as Pthirus pubis, which infests human pubic hair, as well as other areas with hair including eye lashes. Here is the latest research.

Rh Isoimmunization

Rh isoimmunization is a potentially preventable condition that occasionally is associated with significant perinatal morbidity or mortality. Discover the latest research on Rh Isoimmunization here.

Genetic Screens in iPSC-derived Brain Cells

Genetic screening is a critical tool that can be employed to define and understand gene function and interaction. This feed focuses on genetic screens conducted using induced pluripotent stem cell (iPSC)-derived brain cells. It also follows CRISPR-Cas9 approaches to generating genetic mutants as a means of understanding the effect of genetics on phenotype.

Enzyme Evolution

This feed focuses on molecular models of enzyme evolution and new approaches (such as adaptive laboratory evolution) to metabolic engineering of microorganisms. Here is the latest research.

Chronic Fatigue Syndrome

Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.

Pharmacology of Proteinopathies

This feed focuses on the pharmacology of proteinopathies - diseases in which proteins abnormally aggregate (i.e. Alzheimer’s, Parkinson’s, etc.). Discover the latest research in this field with this feed.

Alignment-free Sequence Analysis Tools

Alignment-free sequence analyses have been applied to problems ranging from whole-genome phylogeny to the classification of protein families, identification of horizontally transferred genes, and detection of recombined sequences. Here is the latest research.