Hot Off the Press! – August 2017
Gomez, Juan L; Bonaventura, Jordi; Lesniak, Wojciech; Mathews, William B; Sysa-Shah, Polina; Rodriguez, Lionel A; Ellis, Randall J; Richie, Christopher T; Harvey, Brandon K; Dannals, Robert F; Pomper, Martin G; Bonci, Antonello; Michaelides, Michael
Chemogenetics revealed: DREADD occupancy and activation via converted clozapine. Journal Article
In: Science, vol. 357, no. 6350, pp. 503–507, 2017, ISSN: 1095-9203 (Electronic); 0036-8075 (Linking).
@article{Gomez2017,
title = {Chemogenetics revealed: DREADD occupancy and activation via converted clozapine.},
author = {Juan L Gomez and Jordi Bonaventura and Wojciech Lesniak and William B Mathews and Polina Sysa-Shah and Lionel A Rodriguez and Randall J Ellis and Christopher T Richie and Brandon K Harvey and Robert F Dannals and Martin G Pomper and Antonello Bonci and Michael Michaelides},
url = {https://www.ncbi.nlm.nih.gov/pubmed/28774929},
doi = {10.1126/science.aan2475},
issn = {1095-9203 (Electronic); 0036-8075 (Linking)},
year = {2017},
date = {2017-08-04},
urldate = {2017-08-04},
journal = {Science},
volume = {357},
number = {6350},
pages = {503--507},
address = {Biobehavioral Imaging and Molecular Neuropsychopharmacology Unit, National Institute on Drug Abuse (NIDA) Intramural Research Program, Baltimore, MD 21224, USA.},
abstract = {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.},
keywords = {},
pubstate = {published},
tppubtype = {article}
}
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.
