A novel α-conopeptide Eu1.6 inhibits N-type (Ca_V2.2) calcium channels and exhibits potent analgesic activity.

ABSTRACT: We here describe a novel α-conopeptide, Eu1.6 from Conus eburneus, which exhibits strong anti-nociceptive activity by an unexpected mechanism of action. Unlike other α-conopeptides that largely target nicotinic acetylcholine receptors (nAChRs), Eu1.6 displayed only weak inhibitory activity at the α3β4 and α7 nAChR subtypes and TTX-resistant sodium channels, and no activity at TTX-sensitive sodium channels in rat dorsal root ganglion (DRG) neurons, or opiate receptors, VR1, KCNQ1, L- and T-type calcium channels expressed in HEK293 cells. However, Eu1.6 inhibited high voltage-activated N-type calcium channel currents in isolated mouse DRG neurons which was independent of GABA_B receptor activation. In HEK293 cells expressing Ca_V2.2 channels alone, Eu1.6 reversibly inhibi

SUBMITTER: Liu Z 

PROVIDER: S-EPMC5772529 | biostudies-literature | 2018 Jan

REPOSITORIES: biostudies-literature