Receptors are a general term for structures that are located on the cell surface, recognize extracellular information substances, specifically bind to them, and transmit that information to the inside of the cell. GABA is a neurotransmitter that acts inhibitory on brain activity, and it is called the GABAA receptor that recognizes this GABA and transmits information.This receptor is a target for the discovery of antipsychotic drugs because it is associated with many psychiatric disorders such as anxiety disorders, sleep disorders, depression and schizophrenia when abnormalities occur.However, GABAA receptors have multiple binding sites, and currently used drugs have the problem of acting on these multiple sites to cause side effects, and the development of drugs that act only on specific GABAA receptors. Was sought after.

　The research group used a uniquely developed method to mark a specific protein for fluorescence, and used it to create a fluorescence sensor for the GABA binding site, which is the drug binding site of the GABAA receptor, and the benzodiazepine (drug that enhances the action of GABA) binding site. Successful.This made it possible to fluoresce in response to drugs that act on these specific binding sites.Furthermore, by this sensor method, we discovered two novel GABAA receptor agonists (PPT and TBB) among 1280 compounds.

　The fluorescent sensor technology constructed this time will lead to the development of GABAA receptor agonists that have no side effects.In addition, the two GABAA receptor agonists discovered are expected to be new candidates for psychotropic drugs in the future.Furthermore, it is expected that this result can be widely applied to drug search targeting other cell membrane receptors for which structural information was insufficient and rational drug design was difficult.

* GABA_AThe receptor GABA "A" is officially written in subscript.