AbstractIn this report, the advances of photopharmacology as a method that allows the study of therapeutically relevant target proteins for Alzheimer's disease (AD) with high spatiotemporal resolution through photoswitchable molecules that are manipulated by light irradiation will be presented. The chemical and biophysical basics of the design of photoswitchable drugs are considered, as well as their current specific applications in the development of tool compounds to investigate functions of acetylcholinesterase, muscarinic acetylcholine, cannabinoid, and NMDA receptors, respectively. All of them represent highly important AD targets.