Method to identify ligands for sigma-1 receptors

摘要

An assay for identifying ligands of the à 1 receptor based on a fusion protein comprising the à 1 receptor flanked by two fluorophores, so that said fluorophores are capable of producing constitutive FRET when no ligand is bound to the à 1 receptor. The fusion protein of the invention also allows the simultaneous determination whether the newly determined ligand is an agonist or an antagonist. Said fusion protein has been expressed in a cell, giving rise to a new cellular model useful for identifying à 1 receptor ligands, and additionally for discriminating between agonists and antagonists.