Synthesis and Characterization of a Specific Iodine-125-Labeled TRPC5 Radioligand.

ABSTRACT: The nonselective Ca²⁺ -permeable transient receptor potential channel subfamily member 5 (TRPC5) belongs to the transient receptor potential canonical (TRPC) superfamily and is widely expressed in the brain. Compelling evidence reveals that TRPC5 plays crucial roles in depression and other psychiatric disorders. To develop a TRPC5 radioligand, following up on our previous effort, we synthesized the iodine compound TZ66127 and its iodine-125-labeled counterpart [¹²⁵ I]TZ66127. The synthesis of TZ66127 was achieved by replacing chloride with iodide in the structure of HC608, and the [¹²⁵ I]TZ66127 was radiosynthesized using its corresponding tributylstannylated precursor. We established a stable human TRPC5-overexpressed HEK293-hTRPC5 cell line and performed

SUBMITTER: Yu Y 

PROVIDER: S-EPMC8544919 | biostudies-literature | 2020 Oct

REPOSITORIES: biostudies-literature