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). Here, we describe 3-fluoro-5-methylpyridin-4-amine (5Me3F4AP), a novel K⁺ channel blocker with potential application in PET. 5Me3F4AP has comparable potency to 4AP and the PET tracer 3-fluoro-4-aminopyridine (3F4AP). Compared to 3F4AP, 5Me3F4AP is more lipophilic (l

SUBMITTER: Sun Y 

PROVIDER: S-EPMC10441322 | biostudies-literature | 2023 Aug

REPOSITORIES: biostudies-literature