In vitro characterization of [³H]VAT in cells, animal and human brain tissues for vesicular acetylcholine transporter.

ABSTRACT: Vesicular acetylcholine transporter plays a crucial role in the cholinergic system, and its alterations is implicated in several neurodegenerative disorders. We recently developed a PET imaging tracer [¹⁸F]VAT to target VAChT in vivo with high affinity and selectivity. Here we report in vitro characterization of [³H]VAT, a tritiated counterpart of [¹⁸F]VAT. Using human VAChT-rich cell membrane extracts, a saturated binding curve was obtained for [³H]VAT with K_d = 6.5 nM and B_max = 22.89 pmol/mg protein. In the [³H]VAT competition-binding assay with a panel of CNS ligands, binding inhibition of [³H]VAT was observed using VAChT ligands, the K_i values ranged from 5.41 to 33.3 nM. No inhibition w

SUBMITTER: Liang Q 

PROVIDER: S-EPMC8605764 | biostudies-literature | 2021 Nov

REPOSITORIES: biostudies-literature