MEPIRAPIM-derived synthetic cannabinoids inhibit T-type calcium channels with divergent effects on seizures in rodent models of epilepsy.

ABSTRACT: Background: T-type Ca²⁺ channels (Ca_v3) represent emerging therapeutic targets for a range of neurological disorders, including epilepsy and pain. To aid the development and optimisation of new therapeutics, there is a need to identify novel chemical entities which act at these ion channels. A number of synthetic cannabinoid receptor agonists (SCRAs) have been found to exhibit activity at T-type channels, suggesting that cannabinoids may provide convenient chemical scaffolds on which to design novel Ca_v3 inhibitors. However, activity at cannabinoid type 1 (CB₁) receptors can be problematic because of central and peripheral toxicities associated with potent SCRAs. The putative SCRA MEPIRAPIM and its analogues were recently identified as Ca<

SUBMITTER: Harman T 

PROVIDER: S-EPMC10110893 | biostudies-literature | 2023

REPOSITORIES: biostudies-literature