Chemical and biophysical characterization of novel potassium channel blocker 3-fluoro-5-methylpyridin-4-amine.

ABSTRACT: 4-aminopyridine (4AP) is a potassium (K⁺) channel blocker used clinically to improve walking in people with multiple sclerosis (MS). 4AP binds to exposed K⁺ channels in demyelinated axons, reducing the leakage of intracellular K⁺ and enhancing impulse conduction. Multiple derivatives of 4AP capable of blocking K⁺ channels have been reported including three radiolabeled with positron emitting isotopes for imaging demyelinated lesions using positron emission tomography (PET). However, there remains a demand for novel molecules with suitable physicochemical properties and binding affinity that can potentially be radiolabeled and used as PET radiotracers. In this study, we introduce 3-fluoro-5-methylpyridin-4-amine (5Me3F4AP) as a novel trisubstitute

SUBMITTER: Sun Y 

PROVIDER: S-EPMC11096398 | biostudies-literature | 2024 May

REPOSITORIES: biostudies-literature