N-Sulfonylphenoxazines as neuronal calcium ion channel blockers.

ABSTRACT: Neuropathic pain is a type of chronic pain, usually caused by nerve damage, that responds poorly to traditional pain therapies. The N-type calcium channel (Ca_V2.2) is a well-validated pharmacological target to treat this condition. In order to further improve the inhibition of the N-type calcium channel relative to previously described inhibitors, and also address their problematic instability in blood plasma, the development of N-sulfonylphenoxazines as new calcium channel inhibitors was pursued. A series of N-sulfonylphenoxazines bearing ammonium side chains were synthesised and tested for their ability to inhibit both Ca_V2.2 and Ca_V3.2 (T-type) neuronal ion channels. Compounds with low micromolar activity in Ca_V2.2 were identifie

SUBMITTER: Schmit M 

PROVIDER: S-EPMC11253866 | biostudies-literature | 2024 Jul

REPOSITORIES: biostudies-literature