Baker M D, Wood J N
Dept. of Biology, Medawar Building, University College London, Gower St., WC1E 6BT, London, UK.
Trends Pharmacol Sci. 2001 Jan;22(1):27-31. doi: 10.1016/s0165-6147(00)01585-6.
Voltage-dependent Na+ channels in sensory nerves contribute to the control of membrane excitability and underlie action potential generation. Na+ channel subtypes exhibit a neurone-specific and developmentally regulated pattern of expression, and changes in both channel expression and function are caused by disease. Recent evidence implicates specific roles for Na+ channel subtypes Na(v)1.3 and Na(v)1.8 in pain states that are associated with nerve injury and inflammation, respectively. Insight into the role of Na(v)1.8 in pain pathways has been gained by the generation of a null mutant. Although drugs discriminate poorly between subtypes, the molecular diversity of channels and subtype-specific modulation might provide opportunities to target pain pathways selectively.
感觉神经中的电压依赖性钠通道有助于控制膜兴奋性,并构成动作电位产生的基础。钠通道亚型表现出神经元特异性和发育调节的表达模式,疾病会导致通道表达和功能的改变。最近的证据表明,钠通道亚型Na(v)1.3和Na(v)1.8分别在与神经损伤和炎症相关的疼痛状态中发挥特定作用。通过产生无效突变体,人们对Na(v)1.8在疼痛通路中的作用有了深入了解。尽管药物对不同亚型的区分能力较差,但通道的分子多样性和亚型特异性调节可能为选择性靶向疼痛通路提供机会。