Traditional pharmacology is inherently limited in achieving precise spatial and temporal control. Photopharmacology offers a transformative solution, leveraging light to confer spatiotemporal precision in modulating biological systems. My doctoral research in Joshua Levitz's laboratory at Weill Cornell Medicine has centered on developing photoswitchable ligands to probe G protein-coupled receptor (GPCR) function with high resolution in living cells. Central to this approach is the incorporation of photoswitchable moieties, such as azobenzene, which undergo reversible structural changes upon exposure to specific wavelengths of light, enabling millisecond-scale temporal control and subcellular spatial targeting. I have focused on two primary avenues to advance photopharmacology for GPCRs. First, I developed and optimized soluble photochromic ligands targeting specific GPCRs. These ligands serve as powerful biophysical probes for structure-function studies and tools for in vivo pharmacological behavioral studies. Second, I designed orthogonally tethered, covalently attached photoswitchable ligands, enabling precise studies of receptor activation and signaling dynamics in neurons with genetic targeting. Through a combination of patch-clamp electrophysiology, molecular docking, and calcium imaging. I screened and optimized soluble ligands, ultimately developing novel photoswitchable compounds targeting the serotonin and opioid receptor systems. This work highlights photopharmacology as a transformative approach for unraveling GPCR function and lays the groundwork for next-generation therapeutic advancements.