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In vitro screens and functional assays to assess receptor pharmacology

✍ Scribed by Matthew A. Sills

Publisher
John Wiley and Sons
Year
1994
Tongue
English
Weight
871 KB
Volume
32
Category
Article
ISSN
0272-4391

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✦ Synopsis

Abstract

In the drug discovery process, compounds that demonstrate therapeutic potential must be free of undesirable side effects in order to reach the clinic. Compounds that interact with more than one target, such as a receptor, have the potential to elicit side effects, in comparison to those compounds that are selective for a single target. One predictive measure of whether a compound demonstrates specificity is to profile a compound's activity through a series of receptor binding assays in what is termed a safety screen. If a compound demonstrates activity, further studies are subsequently performed in functional assays in order to determine whether the compound possesses agonist or antagonist activity at that receptor. This article discusses some of the basic tenets of receptor pharmacology and their application to safety assessment.

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