ASRI reports XOB, a bifunctional 5-HT2A antagonist and sodium channel blocker being investigated for bipolar disorder treatment

The Alexander Shulgin Research Institute reports the discovery of XOB, described as the first compound to combine 5-HT2A receptor antagonism with voltage-gated sodium channel blockade. Electrophysiology studies in cultured cells and neurons found that XOB blocked sodium channels, while separate experiments assessed its serotonin receptor binding and functional effects. The compound is presented as a proof-of-concept for polypharmacology, potentially combining actions associated with medications used in bipolar disorder treatment, such as quetiapine and lamotrigine, at similar concentrations. The findings were published in Molecular Pharmacology and involved researchers from several academic and research institutions. XOB has not yet undergone clinical trials, and its efficacy, safety, and regulatory status remain unestablished.