When glutamate is released from the presynaptic membrane during fast excitatory neurotransmission, it readily diffuses across the synaptic cleft and activates ligand-gated ion channels present at the postsynaptic membrane. These ionotropic glutamate receptors have been divided into three classes based on agonist pharmacology and structure, namely AMPA, kainate, and NMDA receptors. NMDA receptors are critically involved in many important neuronal functions, including frequency encoding of information, synaptic plasticity, and neuronal development. However, NMDA receptors also play overt roles in a variety of neurological and psychiatric disorders in the central nervous system, including depression, schizophrenia, ischemia, seizures, traumatic brain injury, Parkinson’s, Huntington’s, and Alzheimer’s diseases. For these reasons, there has been widespread interest in understanding structure, function, and regulation of NMDA receptors for the purpose of developing new treatments for a number of diseases. The overarching goal of research in the laboratory is to enhance the synthetic pharmacology of NMDA receptors (i.e. to develop novel agonists, antagonists, and modulators), and to identify and validate new strategies and targets that can be exploited for therapeutic intervention. The laboratory uses a multidisciplinary approach (electrophysiology, synthetic biology, molecular screening, biochemistry, structural biology, and molecular modeling) to advance our understanding of the relationships between structure, function, and pharmacology of NMDA receptors.