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. Zico-notide, 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.%N型电压依赖性钙通道作为与疼痛密切相关的靶点,分布于伤害性信息传递的神经通路上,激活后通过引起钙离子内流而触发突触囊泡释放疼痛相关的神经递质,参与痛觉传导.阻断N型电压依赖性钙通道可以产生镇痛作用,特别是针对慢性疼痛.目前,针对该靶点的药物齐考诺肽已经上市,经鞘内给药用于治疗对吗啡镇痛耐受或无效患者的严重慢性疼痛,但其应用却受到给药途径及副作用的限制;因而具有口服镇痛活性的小分子N型电压依赖性钙通道阻断剂的研究越来越受到人们的重视.本文就相关研究进展进行综述.
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