Schaible Hans-Georg, Schmelz Martin, Tegeder Irmgard
Institut für Physiologie, Universität Jena, Teichgraben 8, D-07740 Jena, Germany.
Adv Drug Deliv Rev. 2006 May 20;58(2):323-42. doi: 10.1016/j.addr.2006.01.011. Epub 2006 Feb 28.
Deep somatic pain originating in joints and tendons is a major therapeutic challenge. Spontaneous pain and mechanical hypersensitivity can develop as a consequence of sensitization of primary afferents directly involved in the inflammatory process, but also following sensitization of neuronal processing in the spinal cord (central sensitization) or higher centres. Inflammatory pain is linked to sensitization of sensory proteins at the nociceptive endings whereas pain originating from nerve damage (neuropathic pain) has been linked to changes in axonal ion channels producing ectopic discharge in nociceptors as a source of pain. New targets for analgesic therapy include sensory proteins at the nociceptive nerve endings such as the activating TRPV and ASIC channels, but also inhibitory opioid and cannabinoid receptors. Therapeutic targets are also found among the axonal channels that set membrane potential and modulate discharge frequency such as voltage sensitive sodium channels and various potassium channels.
源自关节和肌腱的深部躯体疼痛是一个重大的治疗挑战。自发痛和机械性超敏反应可能是直接参与炎症过程的初级传入神经纤维致敏的结果,也可能是脊髓(中枢敏化)或更高中枢的神经元加工致敏之后出现的。炎性疼痛与伤害性感受器末梢处感觉蛋白的致敏有关,而源于神经损伤的疼痛(神经性疼痛)则与轴突离子通道的变化有关,这些变化会在伤害感受器中产生异位放电,成为疼痛的来源。镇痛治疗的新靶点包括伤害性神经末梢处的感觉蛋白,如激活的瞬时受体电位香草酸亚型(TRPV)通道和酸敏感离子通道(ASIC),还有抑制性阿片类和大麻素受体。在设定膜电位并调节放电频率的轴突通道中也发现了治疗靶点,如电压敏感性钠通道和各种钾通道。