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A novel chemogenetic agnoist "Deschloroclozapine" selectively visualizes and activates chemogenetic receptors in non-human primates
https://repo.qst.go.jp/records/81542
https://repo.qst.go.jp/records/81542fc5ad68e-b615-4792-8299-d749e30199bc
| Item type | 会議発表用資料 / Presentation(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2021-01-05 | |||||
| タイトル | ||||||
| タイトル | A novel chemogenetic agnoist "Deschloroclozapine" selectively visualizes and activates chemogenetic receptors in non-human primates | |||||
| 言語 | ||||||
| 言語 | eng | |||||
| 資源タイプ | ||||||
| 資源タイプ識別子 | http://purl.org/coar/resource_type/c_c94f | |||||
| 資源タイプ | conference object | |||||
| アクセス権 | ||||||
| アクセス権 | metadata only access | |||||
| アクセス権URI | http://purl.org/coar/access_right/c_14cb | |||||
| 著者 |
永井, 裕司
× 永井, 裕司× 宮川, 尚久× 堀, 由紀子× 南本, 敬史× Nagai, Yuji× Miyakawa, Naohisa× Hori, Yukiko× Minamimoto, Takafumi |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | 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. |
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| 会議概要（会議名, 開催地, 会期, 主催者等） | ||||||
| 内容記述タイプ | Other | |||||
| 内容記述 | 第6回 CiNet Conference Brain-Machine Interface - Medical Engineering based on Neuroscience - | |||||
| 発表年月日 | ||||||
| 日付 | 2020-02-05 | |||||
| 日付タイプ | Issued | |||||
