Min Li and a panel of hands-on experimentalists detail state-of-the-art molecular techniques for studying NMDA ligand-gated ion channels and developing assays for nontherapeutic lead selection. The topics range from cDNA cloning to in vitro and in vivo investigation of the channel complex in the mammalian brain. Additional topics include the biochemical analysis of the channel protein and the construction of various heterologous systems for both basic research and high throughput screens (HTS) for pharmaceutical chemicals. Although the focus is on NMDA receptors, the methods are applicable to other ligand-gated ion channels and with some modification may be extended to related membrane signaling receptors. NMDA Receptor Prools offers today's scientists powerful methods for basic research on NMDA receptor structure and function, as well as enormous opportunities for clinical investigation toward the development of novel bioactive compounds.