G protein coupled receptors (GCPRs) are proteins found at the surface of cells are responsible for activating numerous intracellular signaling pathways and thus are involved in regulating about every physiological response. Activation of GPCRs occurs via a diverse array of stimuli as varied as photons, lipids, ions, small hormone or neurotransmitters through to larger peptidic and protein molecules. Currently, GPCRs are currently the target of up to 40% of marketed drugs. Although these drugs were originally believed to function as simple on/off switches able to start or stop GPCR activity, we now know that they produce numerous effects that may lead to undesirable responses. This new knowledge has opened the possibility of developing or identioying unique molecules aimed at specifically blocking or activating the relevant therapeutic responses while reducing deleterious effects. We have developed tools to track these pathways in tissue- and disease-relevant contexts in order to measure the effects of novel compounds and to better design drugs with improved