N-type voltage-dependent calcium channel blockers on analgesia:research advances

As a target closely related with pain,N-type voltage-dependent calcium channels distribute in the nociceptive transmission pathways and participate in the pain transduction by causing calcium inward and triggering synaptic vesicles to release pain-related neurotransmitters.Pain,especially chronic pain,can be inhibited by blocking N-type voltage-dependent calcium channels.Ziconotide,a peptide targeting at N-type voltage-dependent calcium channels,has been listed and is used by intrathecal injection to treat the patients with severe chronic pain who are tolerant or refractory to morphine.However its application is limited by the route of administration and side effects.Therefore,the study of small molecule N-type voltage-dependent calcium channel blocker with oral analgesic activity is getting increasing attention.Related progresses in the N-type voltage-dependent calcium channel blockers on analgesia are reviewed.