Chemogenetics revealed: DREADD occupancy and activation via converted clozapine

Author:

Gomez Juan L.1ORCID,Bonaventura Jordi1ORCID,Lesniak Wojciech2ORCID,Mathews William B.2ORCID,Sysa-Shah Polina2ORCID,Rodriguez Lionel A.1ORCID,Ellis Randall J.1,Richie Christopher T.3ORCID,Harvey Brandon K.3ORCID,Dannals Robert F.2ORCID,Pomper Martin G.2,Bonci Antonello4,Michaelides Michael15ORCID

Affiliation:

1. Biobehavioral Imaging and Molecular Neuropsychopharmacology Unit, National Institute on Drug Abuse (NIDA) Intramural Research Program, Baltimore, MD 21224, USA.

2. Department of Radiology, Johns Hopkins School of Medicine, Baltimore, MD 21205, USA.

3. Optogenetics and Transgenic Technology Core, NIDA Intramural Research Program, Baltimore, MD 21224, USA.

4. Synaptic Plasticity Section, NIDA Intramural Research Program, Baltimore, MD 21224, USA.

5. Department of Psychiatry, Johns Hopkins School of Medicine, Baltimore, MD 21205, USA.

Abstract

DREADD not the designer compound Designer receptors exclusively activated by designer drugs (DREADDs) constitute a powerful chemogenetic strategy that can modulate nerve cell activity in freely moving animal preparations. Gomez et al. used radioligand receptor occupancy measurements and in vivo positron emission tomography to show that DREADDs expressed in the brain are not activated by the designer compound CNO (clozapine N -oxide). Instead, they are activated by the CNO metabolite clozapine, a drug with multiple endogenous targets. This may have important implications for the interpretation of results obtained with this popular technology. Science , this issue p. 503

Funder

National Institute on Drug Abuse Intramural Research Program

Publisher

American Association for the Advancement of Science (AAAS)

Subject

Multidisciplinary

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