High-potency ligands for DREADD imaging and activation in rodents and monkeys

Jordi Bonaventura, Mark A. G. Eldridge, Feng Hu, Juan L. Gomez, Marta Sanchez-Soto, Ara M. Abramyan, Sherry Lam, Matthew A. Boehm, Christina Ruiz, Mitchell R. Farrell, Andrea Moreno, Islam Mustafa Galal Faress, Niels Andersen, John Y. Lin, Ruin Moaddel, Patrick J. Morris, Lei Shi, David R. Sibley, Stephen V. Mahler, Sadegh Nabavi, Martin G. Pomper, Antonello Bonci, Andrew G. Horti (), Barry J. Richmond () and Michael Michaelides ()
Additional contact information
Jordi Bonaventura: National Institute on Drug Abuse Intramural Research Program
Mark A. G. Eldridge: National Institute of Mental Health Intramural Research Program
Feng Hu: Department of Radiology Johns Hopkins School of Medicine
Juan L. Gomez: National Institute on Drug Abuse Intramural Research Program
Marta Sanchez-Soto: National Institute of Neurological Disorders and Stroke Intramural Research Program
Ara M. Abramyan: National Institute on Drug Abuse Intramural Research Program
Sherry Lam: National Institute on Drug Abuse Intramural Research Program
Matthew A. Boehm: National Institute on Drug Abuse Intramural Research Program
Christina Ruiz: University of California
Mitchell R. Farrell: University of California
Andrea Moreno: Aarhus University
Islam Mustafa Galal Faress: Aarhus University
Niels Andersen: Aarhus University
John Y. Lin: University of Tasmania
Ruin Moaddel: National Institute on Aging Intramural Research Program
Patrick J. Morris: National Center for Advancing Translational Sciences
Lei Shi: National Institute on Drug Abuse Intramural Research Program
David R. Sibley: National Institute of Neurological Disorders and Stroke Intramural Research Program
Stephen V. Mahler: University of California
Sadegh Nabavi: Aarhus University
Martin G. Pomper: Department of Radiology Johns Hopkins School of Medicine
Antonello Bonci: National Institute on Drug Abuse Intramural Research Program
Andrew G. Horti: Department of Radiology Johns Hopkins School of Medicine
Barry J. Richmond: National Institute of Mental Health Intramural Research Program
Michael Michaelides: National Institute on Drug Abuse Intramural Research Program

Nature Communications, 2019, vol. 10, issue 1, 1-12

Abstract: 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.

Date: 2019
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DOI: 10.1038/s41467-019-12236-z

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