VSN16R

VSN16R is an orally available small molecule drug developed as a selective opener of large conductance, calcium-activated potassium (BKCa) channels. It was originally synthesized as an analogue of the endocannabinoid anandamide to control spasticity associated with multiple sclerosis and other neurological disorders, while avoiding the sedative side effects typical of cannabinoid-based therapies[5][6]. Unlike classical cannabinoids, VSN16R does not bind to CB1, CB2, or GPR55 receptors but acts directly on neuronal BKCa channels to induce membrane hyperpolarization and limit excessive neural excitability[3][5][6]. This mechanism underlies its potential for treating spasticity and related symptoms. The drug has demonstrated efficacy in preclinical models and has shown a favorable safety profile in early-phase clinical trials for multiple sclerosis-related spasticity[7]. More recently, it is being investigated for use in Fragile X syndrome[4][7].

Other names

(R,Z)-3-(6-(dimethylamino)-6-oxohex-1-en-1-yl)-N-(1-hydroxypropan-2-yl) benzamide