Effect of benzothiazole/piperazine derivatives on intracerebroventricular streptozotocin-induced cognitive deficits.

Journal Title: Pharmacological Reports - Year 2012, Vol 64, Issue 4

Abstract

Background: In this study, benzothiazole-piperazine compounds were synthesized by condensing the functional groups of donepezil (DNP), FK-960, and sabeluzole, which are known to have therapeutic potential against Alzheimer's disease, with the aim of obtaining new and potent anti-Alzheimer agents. Methods: Initially, acetylcholinesterase/butyrylcholinesterase enzyme inhibition activities of the synthesized test compounds were investigated by Ellman's method. Effects of the compounds on a streptozotocin (STZ) model of Alzheimer's disease (SMAD) were investigated in rats. SMAD was established by intracerebroventricular (icv) injection of STZ (3 mg/kg), bilaterally. The elevated plus maze, Morris water maze, and active avoidance tests were used to examine the effects of test compounds (1, 5, and 10 mg/kg) on learning and memory parameters of icv STZ-injected rats. Effects of the test compounds on spontaneous locomotor activities of rats were examined with the activity cage test. Results: The compounds B2-B5 and DNP exhibited significant selective inhibitory potencies against acetylcholinesterase. Compounds B2 and B3 at 10 mg/kg doses and compounds B4 and B5 at 5 and 10 mg/kg doses, as well as the reference drug DNP (1 and 3 mg/kg), significantly improved the learning and memory parameters of animals in all cognition tests. None of the test compounds changed spontaneous locomotor activities. Conclusion: Results of the present study revealed that compounds B2-B5 repaired the parameters related to the learning and memory deficits of icv STZ-injected rats. Potencies of these test compounds were comparable to the activity of DNP.

Authors and Affiliations

Umide Özkay, Özgür Can, Yusuf Özkay

Keywords

Related Articles

Effects of diabetes and vascular occlusion on adenosine-induced relaxant response of rat common carotid artery.

Background: The aim of this study was to investigate effect of adenosine on isolated rat common carotid artery (CA) submitted to occlusion in non-diabetic or diabetic animals, and to determine whether endothelium denudat...

Influence of atorvastatin on serum amyloid A-low density lipoprotein complex in hypercholesterolemic patients.

The complex of serum amyloid A(SAA) and low-density lipoprotein (LDL), SAA-LDL, is considered a new and unique marker of oxidatively-modified LDL particles, which is associated with atherosclerotic conditions. This study...

Molecular determinants of heart failure with normal left ventricular ejection fraction.

In population-based studies, heart failure with normal left ventricular (LV) ejection fraction (HFNEF) is now increasingly recognized and referred to as diastolic heart failure. However, the pathogenic mechanisms underly...

Lack of effect of sildenafil on cocaine-induced convulsions in mice.

The convulsant action of cocaine and the proconvulsant effects of sildenafil, a drug which is widely used in the treatment of erectile dysfunction, have been documented both in humans and mice. Since it was reported that...

Bismuth increases hydroxyl radical-scavenging activity of histamine H(2)-receptor antagonists.

The effects of histamine H(2)-receptor antagonists, alone or in a combination with bismuth, on ( )OH-provoked degradation of deoxyribose were studied. The histamine H(2)-receptor antagonists (cimetidine, ranitidine and r...

Download PDF file
  • EP ID EP140596
  • DOI -
  • Views 102
  • Downloads 0

How To Cite

Umide Özkay, Özgür Can, Yusuf Özkay (2012). Effect of benzothiazole/piperazine derivatives on intracerebroventricular streptozotocin-induced cognitive deficits.. Pharmacological Reports, 64(4), 834-847. https://europub.co.uk/articles/-A-140596