Abstract: The present invention provides a new approach for the treatment of G-protein coupled receptor based disease. This approach comprises altering the physiology of G-protein coupled receptor based responses by exerting chemical control over the cellular distribution of the receptor. This approach allows a method for phenotypic screening for candidate compounds which disrupt GPCR distribution signaling activity and are therefore candidates for the treatment of GPCR related conditions. Compounds that create an altered distribution of GPCR upon exposure to the cell are identified. The method then uses these molecules to alter physiology through their effect on receptor distribution and reduction to practice is demonstrated in an ex-vivo model of G-protein coupled receptor activity.