Holzer Peter
Medical University of Graz, Department of Experimental and Clinical Pharmacology, Austria.
Expert Opin Ther Targets. 2004 Apr;8(2):107-23. doi: 10.1517/14728222.8.2.107.
Functional bowel disorders (FBDs) are defined by symptoms of gastrointestinal (GI) dysfunction, discomfort and pain in the absence of a demonstrable organic cause. Since the prevalence of FBDs, particularly functional dyspepsia and irritable bowel syndrome, can be as high as 20%, FBDs represent a significant burden in terms of direct healthcare and productivity costs. There is emerging evidence that the discomfort and pain experienced by many FBD patients is due to persistent hypersensitivity of primary afferent neurons, which may develop in response to infection, inflammation or other insults. This concept identifies vagal and spinal sensory neurons as important targets for novel therapies of GI hyperalgesia. Sensory neuron-specific targets can be grouped into three categories: receptors and sensors at the peripheral nerve terminals, ion channels relevant to nerve excitability and conduction and transmitter receptors. Particular therapeutic potential is attributed to targets that are selectively expressed by afferent neurons, such as the transient receptor potential channel TRPV1, acid-sensing ion channels and tetrodotoxin-resistant Na + channels.
功能性肠病(FBDs)的定义是在没有可证实的器质性病因的情况下出现胃肠(GI)功能障碍、不适和疼痛症状。由于FBDs的患病率,尤其是功能性消化不良和肠易激综合征,可能高达20%,因此FBDs在直接医疗保健和生产力成本方面构成了重大负担。越来越多的证据表明,许多FBD患者所经历的不适和疼痛是由于初级传入神经元的持续超敏反应,这种超敏反应可能是对感染、炎症或其他损伤的反应而产生的。这一概念将迷走神经和脊髓感觉神经元确定为胃肠痛觉过敏新疗法的重要靶点。感觉神经元特异性靶点可分为三类:外周神经末梢的受体和传感器、与神经兴奋性和传导相关的离子通道以及递质受体。具有特定治疗潜力的靶点是由传入神经元选择性表达的,如瞬时受体电位通道TRPV1、酸敏感离子通道和河豚毒素抗性Na+通道。