Evaluation of trans- and cis-4-[¹⁸F]fluorogabapentin for brain PET imaging.

ABSTRACT: Gabapentin, a selective ligand for the α2δ subunit of voltage-dependent calcium channels, is an anticonvulsant medication used in the treatment of neuropathic pain, epilepsy and other neurological conditions. We recently described two radiofluorinated derivatives of gabapentin (trans-4-[¹⁸F]fluorogabapentin, [¹⁸F]tGBP4F, and cis-4-[¹⁸F]fluorogabapentin, [¹⁸F]cGBP4F) and showed that these compounds accumulate in the injured nerves in a rodent model of neuropathic pain. Given the use of gabapentin in brain diseases, here we investigate whether these radiofluorinated derivatives of gabapentin can be used for imaging α2δ receptors in the brain. Specifically, we developed automated radiosynthesis methods for [¹⁸F]tGBP4F and [<

SUBMITTER: Zhou YP 

PROVIDER: S-EPMC10508714 | biostudies-literature | 2023 Oct

REPOSITORIES: biostudies-literature