| 摘要 |
<p>A method to determine the site of action of a receptor modulating compound is disclosed. The method comprises: a) determining the effect of said compound on a first host cell that has been modified to display a mutant form of said receptor, wherein said mutant produces the activated state of its cognate signaling pathway, wherein said determining comprises measuring the intracellular level of cyclic AMP or other post-binding event; b) determining the effect of said compound on a second host cell that has been modified to display a derivative of said receptor which is formed by coupling an agonist for said receptor covalently to said receptor; wherein said determining comprises measuring the intracellular level of cyclic AMP or other post-binding event; and c) comparing the effect of said compound as determined in steps a) and b); whereby a compound that alters the level of cyclic AMP or downstream event in both a) and b) has a site of action at the binding site for agonists, and a compound that alters the level of cyclic AMP or post-binding event in step a) but not in step b) has a site of action other than at the agonist binding site.</p> |
