Role of the transient receptor potential vanilloid 1 in inflammation and sepsis.
Role of the transient receptor potential vanilloid 1 in inflammation and sepsis.
复制标题
瞬态受体电位香草素1在炎症和败血症中的作用。
DOI：
10.2147/jir.s12978
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发表时间：
2011
影响因子：
4.5
通讯作者：
Fernández-Carvajal A
中科院分区：
文献类型：
--
作者：
Devesa I;Planells-Cases R;Fernández-Ballester G;González-Ros JM;Ferrer-Montiel A;Fernández-Carvajal A
瞬时受体电位香草素1(TRPV1)是一种对有害温度以及化学激动剂(如香草素和质子)做出反应的温度感受器。此外，在组织损伤时释放的促炎介质显著增强了其通道活性。TRPV1在前止痛剂对感觉神经元的敏化中的作用已表明该受体是止痛和抗炎药物干预的主要靶点。然而，TRPV1拮抗剂由于其不受欢迎的副作用，在临床和临床前研究中明显失败。最近的报告揭示了以前未知的TRPV1在几种疾病中的抗炎和保护功能。例如，这个通道被认为在脓毒症中起到抗炎作用。因此，考虑到抑制具有保护功能的通道的数量可能产生的有害影响，必须谨慎地考虑使用有效的TRPV1拮抗剂作为治疗炎症的一般策略。TRPV1拮抗剂的使用可能仅限于治疗受体活性增强导致炎症状态的那些病理。或者，治疗方案，如减少炎症介导的细胞表面受体表达增加，可能是防止参与抗炎和保护过程的TRPV1亚群消失的更好策略。
The transient receptor potential vanilloid 1 (TRPV1) is a thermoreceptor that responds to noxious temperatures, as well as to chemical agonists, such as vanilloids and protons. In addition, its channel activity is notably potentiated by proinflammatory mediators released upon tissue damage. The TRPV1 contribution to sensory neuron sensitization by proalgesic agents has signaled this receptor as a prime target for analgesic and anti-inflammatory drug intervention. However, TRPV1 antagonists have notably failed in clinical and preclinical studies because of their unwanted side effects. Recent reports have unveiled previously unrecognized anti-inflammatory and protective functions of TRPV1 in several diseases. For instance, this channel has been suggested to play an anti-inflammatory role in sepsis. Therefore, the use of potent TRPV1 antagonists as a general strategy to treat inflammation must be cautiously considered, given the deleterious effects that may arise from inhibiting the population of channels that have a protective function. The use of TRPV1 antagonists may be limited to treating those pathologies where enhanced receptor activity contributes to the inflamed state. Alternatively, therapeutic paradigms, such as reduction of inflammatory-mediated increase of receptor expression in the cell surface, may be a better strategy to prevent abrogation of the TRPV1 subpopulation involved in anti-inflammatory and protective processes.