[¹¹C]deschloroclozapine is an improved PET radioligand for quantifying a human muscarinic DREADD expressed in monkey brain.

ABSTRACT: Previous work found that [¹¹C]deschloroclozapine ([¹¹C]DCZ) is superior to [¹¹C]clozapine ([¹¹C]CLZ) for imaging Designer Receptors Exclusively Activated by Designer Drugs (DREADDs). This study used PET to quantitatively and separately measure the signal from transfected receptors, endogenous receptors/targets, and non-displaceable binding in other brain regions to better understand this superiority. A genetically-modified muscarinic type-4 human receptor (hM₄Di) was injected into the right amygdala of a male rhesus macaque. [¹¹C]DCZ and [¹¹C]CLZ PET scans were conducted 2-24 months later. Uptake was quantified relative to the concentration of parent radioligand in arterial plasma at baseline (n = 3 scans/radiolig

SUBMITTER: Yan X 

PROVIDER: S-EPMC8504956 | biostudies-literature | 2021 Oct

REPOSITORIES: biostudies-literature