61. Radiosynthesis and Evaluation of Pet Radioligands for Ion-Channel Based Chemogenetics

Pharmacologically Selective Actuator Molecules(PSAMs) are advanced chemogenetic tools used to manipulate neuronal activity in brain. A triple-mutant PSAM is called PSAM4. Here, PSAM4-GlyR is a chimeric ligand-gated ion channel comprising a mutated a7 nicotinic acetylcholine receptor( α7-nAChR) ligand-binding domain with an inhibitory chloride-selective glycine receptor ion pore. To create an improved PET radioligand for verifying PSAM4 expression, we synthesized two analogs of varenicline, an anti-smoking drug that activates PSAM4 and evaluated their behavior as PET radioligand s in rats, mice, and monkeys.
Source: Biological Psychiatry - Category: Psychiatry Authors: Source Type: research