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Chemiluminescent high-throughput microassay for evaluation of acetylcholinesterase inhibitors [An article from: Analytica Chimica Acta]
Book Details
PublisherElsevier
ISBN / ASINB000RR3IPK
ISBN-13978B000RR3IP3
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Description
This digital document is a journal article from Analytica Chimica Acta, published by Elsevier in 2005. The article is delivered in HTML format and is available in your Amazon.com Media Library immediately after purchase. You can view it with any web browser.
Description:
Current drug therapies for Alzheimer's disease (AD) are mainly based on acetylcholinesterase (AChE) inhibitors. However, such inhibitors may possess non-optimal pharmacological properties or cause adverse effects, therefore research for the development of new drugs is still in progress. In this paper, a rapid and simple chemiluminescent (CL) assay for the in vitro evaluation of AChE inhibitors in which the activity of AChE is measured through a series of coupled enzymatic reactions leading to light emission is described. The assay is performed in microtiter plates, both in the 96- and 384-well formats. In the latter format up to 30 compounds can be simultaneously analyzed in a very short time (the chemiluminescence measurement lasts 5min) and using small volumes of samples and reagents (the assay volume is less than 60@mL), thus allowing high-throughput screening (HTS). The assay proved to be reliable, as demonstrated by the analysis of known AChE inhibitors, and the reproducibility of the results was satisfying for a screening assay (CV% in the order of 20%). It could therefore represent a valuable alternative to other methods for the preliminary evaluation of new potential AChE inhibitors.
Description:
Current drug therapies for Alzheimer's disease (AD) are mainly based on acetylcholinesterase (AChE) inhibitors. However, such inhibitors may possess non-optimal pharmacological properties or cause adverse effects, therefore research for the development of new drugs is still in progress. In this paper, a rapid and simple chemiluminescent (CL) assay for the in vitro evaluation of AChE inhibitors in which the activity of AChE is measured through a series of coupled enzymatic reactions leading to light emission is described. The assay is performed in microtiter plates, both in the 96- and 384-well formats. In the latter format up to 30 compounds can be simultaneously analyzed in a very short time (the chemiluminescence measurement lasts 5min) and using small volumes of samples and reagents (the assay volume is less than 60@mL), thus allowing high-throughput screening (HTS). The assay proved to be reliable, as demonstrated by the analysis of known AChE inhibitors, and the reproducibility of the results was satisfying for a screening assay (CV% in the order of 20%). It could therefore represent a valuable alternative to other methods for the preliminary evaluation of new potential AChE inhibitors.
