Abstract
Voltage-gated calcium channels (VGCCs) play an important role in the transmission of nociceptive information. Previous studies have focused on targeting the α1 subunit of VGCCs, specifically the N-type and T-type VGCCs, for the development of analgesic drugs. New research has highlighted an underlying role for the auxiliary α2-δ subunit in in vivo models of neuropathic pain. Further evidence that the marketed pain therapies gabapentin and pregabalin target α2-δ subunits within the VGCC to pharmacologically modulate calcium channel signaling and attenuate nociceptive transmission, thus alleviating pain symptoms, has prompted the development of novel α2-δ ligands as candidate analgesics. This article will highlight promising novel compounds emerging in the recent literature.
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