The brain is different from other organs in the body by its special ability of information processing. This is mainly achieved by interconnected neuronal networks. The building blocks of the neural network are individual neurons. Communication between neurons is the basic form of information processing in the brain. This is mainly mediated by chemical synapse, where one neuron releases neurotransmitter, which binds to its receptor in another neuron to control its excitability to accomplish the inter-neuronal communication. One major class of the neurotransmitter receptors is the family of neurotransmitter-operated ion channels. Binding of neurotransmitters to these receptors opens the channel, which allows charged ions to flow through the channel, modifying electrical properties of the neuron. Dysfunction of these ion channels can severely influence neuronal excitability, resulting in a variety of neurological and psychiatric disorders, such as epilepsy, anxiety, insomnia, and schizophrenia. Thus, gaining insights into the molecular mechanisms of neurotransmitter-operated ion channel function, modulation, and dysfunction is fundamental to the understanding of the pathogenesis of these disorders and new drug discovery. The long-term research goal of this laboratory is to elucidate the structural basis for neurotransmitter-operated ion channel function and their modulation though an interdisciplinary approach. This will set the foundation for future development of the structure-based drug design, and to study the molecular mechanism of neurotransmitter receptor dysfunction, such as epilepsy, anxiety, insomnia, and schizophrenia.