ELECTROPHYSIOLOGICAL METHOD TO PHARMACOLOGICALLY CLASSIFY LIGANDS FOR GS PROTEIN-COUPLED RECEPTORS

摘要

The invention provides methods for functionally classifying ligands for stimulatory G protein-coupled receptors as full or partial agonists, inverse agonists, or antagonists that comprise providing cells comprising at least one stimulatory G protein, at least one copy of a stimulatory G protein-coupled receptor, and at least one copy of an inwardly rectifying potassium channel; contacting the cells with a ligand for the stimulatory G protein-coupled receptor; measuring the current through the inwardly rectifying potassium channels; and determining whether ligand is full or partial agonist, inverse agonist, or antagonist based upon the level of current measured through the inwardly rectifying potassium channels.