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

@article{Bonaventura:2019aa,

title = {High-potency ligands for DREADD imaging and activation in rodents and monkeys.},

author = {Jordi Bonaventura and Mark A G Eldridge and Feng Hu and Juan L Gomez and Marta Sanchez-Soto and Ara M Abramyan and Sherry Lam and Matthew A Boehm and Christina Ruiz and Mitchell R Farrell and Andrea Moreno and Islam Mustafa Galal Faress and Niels Andersen and John Y Lin and Ruin Moaddel and Patrick J Morris and Lei Shi and David R Sibley and Stephen V Mahler and Sadegh Nabavi and Martin G Pomper and Antonello Bonci and Andrew G Horti and Barry J Richmond and Michael Michaelides},

url = {https://www.ncbi.nlm.nih.gov/pubmed/31604917},

doi = {10.1038/s41467-019-12236-z},

issn = {2041-1723 (Electronic); 2041-1723 (Linking)},

year  = {2019},

date = {2019-10-11},

journal = {Nat Commun},

volume = {10},

number = {1},

pages = {4627},

address = {Biobehavioral Imaging and Molecular Neuropsychopharmacology Unit, National Institute on Drug Abuse Intramural Research Program, Baltimore, MD, 21224, USA.},

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 (18)F positron emission tomography (PET) DREADD radiotracer, [(18)F]JHU37107. We show that JHU37152 and JHU37160 exhibit high in vivo DREADD potency. [(18)F]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.},

keywords = {},

pubstate = {published},

tppubtype = {article}

}