METHODS OF SCREENING COMPOUNDS FOR THEIR PHARMACOLOGICAL RELEVANCE BASED ON DOWNREGULATION OF RECOMBINANT RECEPTORS

摘要

This invention relates to the use of reagents in a novel manner to screen compounds in vitro for their ability to interact with and modulate the functional properties of receptors coupled to guanyl nucleotide-binding regulatory proteins (G-proteins). Methods are described herein for determining the ability of compounds to act as antagonists by observing their ability to downregulate recombinant G-protein coupled receptors in membrane preparations. The methods described permit the downregulation effect to be observed within a time frame that is dramatically accelerated compared to other known methods of testing the same effect, thereby providing novel and improved efficient means of screening compounds for their probable pharmaceutical efficacy. This invention also relates to the use of such reagents and methods in kits.