New performance of biosensor technology for Alzheimer's disease drugs: in vitro comparison of tacrine and 7-methoxytacrine.

Abstract

Two drugs were tested using electrochemical biosensor with immobilized acetylcholinesterase (AChE). The first was commercialized drug tacrine (known also as Cognex) used for treatment of cognitive manifestation of Alzheimer\'s disease (AD). The second one was its 7-methoxy derivate (7-MEOTA) that has not been marketed. We determined the IC50 (6.67+/-0.92)x10-7 M for tacrine and (1.66+/-1.43)x10-9 M for 7-MEOTA. In this in vitro study, 7-MEOTA acts as stronger inhibitor of AChE and in this way could be more favorable for treatment of cognitive manifestation of AD. Our study shows that biosensor technology could be used as a quick and cheap tool for testing of promising AChE inhibitors (AD drug candidates).

• Authors: Miroslav Pohanka, Kamil Kuca, Jiri Kassa
• Journal: Neuro endocrinology letters (Neuro Endocrinol Lett) Vol. 29 Issue 5 Pg. 755-8 (Oct 2008) ISSN: 0172-780X [Print] Sweden
• PMID: 18987590 (Publication Type: Comparative Study, Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Cholinesterase Inhibitors
• Enzymes, Immobilized
• Nootropic Agents
• Tacrine
• 7-methoxytacrine
• Acetylcholinesterase

Topics

• Acetylcholinesterase (chemistry)
• Algorithms
• Alzheimer Disease (drug therapy)
• Biosensing Techniques
• Cholinesterase Inhibitors (analysis)
• Electrochemistry
• Enzymes, Immobilized (chemistry)
• Humans
• Kinetics
• Nootropic Agents (analysis)
• Tacrine (analogs & derivatives, analysis)