Synthesis and preclinical evaluation of [¹¹C]uPSEM792 for PSAM⁴-GlyR based chemogenetics.

ABSTRACT: Chemogenetic tools are designed to control neuronal signaling. These tools have the potential to contribute to the understanding of neuropsychiatric disorders and to the development of new treatments. One such chemogenetic technology comprises modified Pharmacologically Selective Actuator Modules (PSAMs) paired with Pharmacologically Selective Effector Molecules (PSEMs). PSAMs are receptors with ligand-binding domains that have been modified to interact only with a specific small-molecule agonist, designated a PSEM. PSAM⁴ is a triple mutant PSAM derived from the α7 nicotinic receptor (α7^{L131G,Q139L,Y217F}). Although having no constitutive activity as a ligand-gated ion channel, PSAM⁴ has been coupled to the serotonin 5-HT₃ receptor (5-HT₃

SUBMITTER: Nerella SG 

PROVIDER: S-EPMC10803328 | biostudies-literature | 2024 Jan

REPOSITORIES: biostudies-literature