Computer-aided Discovery of a New Nav1.7 Inhibitor for Treatment of Pain and Itch

Conclusions This study ’s computer-aided drug discovery approach yielded a new Nav1.7 inhibitor that shows analgesic and anti-pruritic activity in mouse models.Editor ’s PerspectiveWhat We Already Know about This TopicThe Nav1.7 sodium ion channel is of critical importance to pain perception and itch in humansSelective Nav1.7 blockers have not become clinically available for use in pain managementWhat This Article Tells Us That Is NewIn silico screening identified several potential Nav1.7 blocking compoundsThe combined use of electrophysiology and behavioral pharmacology demonstrated that one compound, DA-0218, was a potent inhibitor of Nav1.7 channels, pain behaviors, and itch in mice
Source: Anesthesiology - Category: Anesthesiology Source Type: research