Global S&T Development Trend Analysis Platform of Resources and Environment
DOI | 10.1126/science.aan2475 |
Chemogenetics revealed: DREADD occupancy and activation via converted clozapine | |
Gomez, Juan L.1; Bonaventura, Jordi1; Lesniak, Wojciech2; Mathews, William B.2; Sysa-Shah, Polina2; Rodriguez, Lionel A.1; Ellis, Randall J.1; Richie, Christopher T.3; Harvey, Brandon K.3; Dannals, Robert F.2; Pomper, Martin G.; Bonci, Antonello4; Michaelides, Michael1,5 | |
2017-08-04 | |
发表期刊 | SCIENCE
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ISSN | 0036-8075 |
EISSN | 1095-9203 |
出版年 | 2017 |
卷号 | 357期号:6350页码:503-+ |
文章类型 | Article |
语种 | 英语 |
国家 | USA |
英文摘要 | The chemogenetic technology DREADD (designer receptors exclusively activated by designer drugs) is widely used for remote manipulation of neuronal activity in freely moving animals. DREADD technology posits the use of "designer receptors," which are exclusively activated by the "designer drug" clozapine N-oxide (CNO). Nevertheless, the in vivo mechanism of action of CNO at DREADDs has never been confirmed. CNO does not enter the brain after systemic drug injections and shows low affinity for DREADDs. Clozapine, to which CNO rapidly converts in vivo, shows high DREADD affinity and potency. Upon systemic CNO injections, converted clozapine readily enters the brain and occupies central nervous system-expressed DREADDs, whereas systemic subthreshold clozapine injections induce preferential DREADD-mediated behaviors. |
领域 | 地球科学 ; 气候变化 ; 资源环境 |
收录类别 | SCI-E |
WOS记录号 | WOS:000406840100038 |
WOS关键词 | BLOOD-BRAIN-BARRIER ; N-OXIDE ; IN-VIVO ; METABOLISM ; DRUGS ; MICE ; RAT |
WOS类目 | Multidisciplinary Sciences |
WOS研究方向 | Science & Technology - Other Topics |
URL | 查看原文 |
引用统计 | |
文献类型 | 期刊论文 |
条目标识符 | http://119.78.100.173/C666/handle/2XK7JSWQ/196597 |
专题 | 地球科学 资源环境科学 气候变化 |
作者单位 | 1.NIDA, Biobehav Imaging & Mol Neuropsychopharmacol, Intramural Res Program, Baltimore, MD 21224 USA; 2.Johns Hopkins Sch Med, Dept Radiol, Baltimore, MD 21205 USA; 3.NIDA, Intramural Res Program, Optogenet & Transgen Technol Core, Baltimore, MD 21224 USA; 4.NIDA, Synapt Plast Sect, Intramural Res Program, Baltimore, MD 21224 USA; 5.Johns Hopkins Sch Med, Dept Psychiat, Baltimore, MD 21205 USA |
推荐引用方式 GB/T 7714 | Gomez, Juan L.,Bonaventura, Jordi,Lesniak, Wojciech,et al. Chemogenetics revealed: DREADD occupancy and activation via converted clozapine[J]. SCIENCE,2017,357(6350):503-+. |
APA | Gomez, Juan L..,Bonaventura, Jordi.,Lesniak, Wojciech.,Mathews, William B..,Sysa-Shah, Polina.,...&Michaelides, Michael.(2017).Chemogenetics revealed: DREADD occupancy and activation via converted clozapine.SCIENCE,357(6350),503-+. |
MLA | Gomez, Juan L.,et al."Chemogenetics revealed: DREADD occupancy and activation via converted clozapine".SCIENCE 357.6350(2017):503-+. |
条目包含的文件 | 条目无相关文件。 |
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