Synthesis and biological evaluation of PET tracers designed for imaging of calcium activated potassium channel 3.1 (K_Ca3.1) channels in vivo.

ABSTRACT: Expression of the Ca²⁺ activated potassium channel 3.1 (K_Ca3.1) channel (also known as the Gàrdos channel) is dysregulated in many tumor entities and has predictive power with respect to patient survival. Therefore, a positron emission tomography (PET) tracer targeting this ion channel could serve as a potential diagnostic tool by imaging the K_Ca3.1 channel in vivo. It was envisaged to synthesize [¹⁸F]senicapoc ([¹⁸F]1) since senicapoc (1) shows high affinity and excellent selectivity towards the K_Ca3.1 channels. Because problems occurred during ¹⁸F-fluorination, the [¹⁸F]fluoroethoxy senicapoc derivative [¹⁸F]28 was synthesized to generate an alternative PET tracer targeting the K

SUBMITTER: Brommel K 

PROVIDER: S-EPMC9041111 | biostudies-literature | 2021 Sep

REPOSITORIES: biostudies-literature