@misc{oai:repo.qst.go.jp:00081542, author = {永井, 裕司 and 宮川, 尚久 and 堀, 由紀子 and 南本, 敬史 and Nagai, Yuji and Miyakawa, Naohisa and Hori, Yukiko and Minamimoto, Takafumi}, month = {Feb}, note = {DREADDs (Designer Receptors Exclusively Activated by Designer Drugs) are genetically modified G-protein coupled receptors that are activated by physiologically inert designer drugs. Two types of muscarinic-based designer receptor, such as hM3Dq (excitatory) and hM4Di (inhibitory), are widely used and remotely modulate the neural activity of a target cell population expressing a "designer receptor" by systemic delivery of a designer drug (CNO). We have shown that positron emission tomography (PET) with [11C]clozapine enables us to monitor the hM4Di expression and the agonist dose–occupancy relationship that provides critical information for successful chemogenetic silencing (Nagai et al., 2016). However, previous designer-drugs suffer from low selectivity and poor metabolic stability. Here we developed a novel ligand, deschloroclozapine (DCZ), served a dual purpose in chemogenetics: (1) as a selective compound for visualization of DREADD expression in vivo by PET and (2) as a selective agonist for muscarinic-based DREADDs., 第6回 CiNet Conference Brain-Machine Interface - Medical Engineering based on Neuroscience -}, title = {A novel chemogenetic agnoist "Deschloroclozapine" selectively visualizes and activates chemogenetic receptors in non-human primates}, year = {2020} }