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http://hdl.handle.net/2445/190602| Title: | High-potency ligands for DREADD imaging and activation in rodents and monkeys |
| Author: | Bonaventura, Jordi Eldridge, Mark A.G. Hu, Feng Gomez, Juan L. Sánchez Soto, Marta Abramyan, Ara M. Lam, Sherry Boehm, Matthew A. Ruiz, Christina Farrell, Mitchell R. Moreno, Andrea Galal Faress, Islam Mustafa Andersen, Niels Linm John Y. Moaddel, Ruin Morris, Patrick J. Shi, Lei Sibley, David R. Mahler, Stephen V. Nabavi, Sadegh Pomper, Martin G. Bonci, Antonello Horti, Andrew G. Richmond, Barry J. Michaelides, Michael |
| Keywords: | Animals Antipsicòtics Cervell Drogues de disseny Animals Antipsychotic drugs Brain Designer drugs |
| Issue Date: | 11-Oct-2019 |
| Publisher: | Nature Publishing Group |
| Abstract: | Designer Receptors Exclusively Activated by Designer Drugs (DREADDs) are a popular chemogenetic technology for manipulation of neuronal activity in uninstrumented awake animals with potential for human applications as well. The prototypical DREADD agonist clozapine N-oxide (CNO) lacks brain entry and converts to clozapine, making it difficult to apply in basic and translational applications. Here we report the development of two novel DREADD agonists, JHU37152 and JHU37160, and the first dedicated 18F positron emission tomography (PET) DREADD radiotracer, [18F]JHU37107. We show that JHU37152 and JHU37160 exhibit high in vivo DREADD potency. [18F]JHU37107 combined with PET allows for DREADD detection in locally-targeted neurons, and at their long-range projections, enabling noninvasive and longitudinal neuronal projection mapping. |
| Note: | Reproducció del document publicat a: https://doi.org/10.1038/s41467-019-12236-z |
| It is part of: | Nature Communications, 2019, vol. 10 |
| URI: | http://hdl.handle.net/2445/190602 |
| Related resource: | https://doi.org/10.1038/s41467-019-12236-z |
| ISSN: | 2041-1723 |
| Appears in Collections: | Articles publicats en revistes (Patologia i Terapèutica Experimental) |
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