Holzer Peter, Izzo Angelo A
Research Unit of Translational Neurogastroenterology, Institute of Experimental and Clinical Pharmacology, Medical University of Graz, Graz, Austria.
Br J Pharmacol. 2014 May;171(10):2469-73. doi: 10.1111/bph.12723.
This themed issue of the British Journal of Pharmacology contains review and research articles on recent advances in transient receptor potential (TRP) channel pharmacology. The review articles, written by a panel of distinguished experts, address the rapid progress in TRP channel research in fields as diverse as oncology, urology, dermatology, migraine, inflammation and pain. These reviews are complemented by original research reports focusing, among others, on the emerging roles of TRPV1 in osteoporosis and cystitis and on evodiamine as a lead structure for the development of potent TRPV1 agonists/desensitizers. Other papers highlight the differences in TRPV3 pharmacology between recombinant and native systems, the mechanisms of TRPM3 activation/inhibition and TRPP2 as a target of naringenin, a dietary flavonoid with anticancer actions. New therapeutic opportunities in pain may arise from the strategy to combine TRP channel and cell membrane impermeant sodium channel blockers to inhibit sensory nerve activity.
本期《英国药理学杂志》主题专刊包含关于瞬时受体电位(TRP)通道药理学最新进展的综述和研究文章。这些综述文章由一批杰出专家撰写,阐述了TRP通道研究在肿瘤学、泌尿学、皮肤病学、偏头痛、炎症和疼痛等不同领域的快速进展。这些综述辅以原创研究报告,其中重点关注TRPV1在骨质疏松症和膀胱炎中的新作用,以及吴茱萸碱作为开发强效TRPV1激动剂/脱敏剂的先导结构。其他论文强调了重组系统和天然系统之间TRPV3药理学的差异、TRPM3激活/抑制的机制,以及TRPP2作为柚皮素(一种具有抗癌作用的膳食黄酮)的靶点。将TRP通道阻滞剂与细胞膜不透性钠通道阻滞剂联合使用以抑制感觉神经活动的策略,可能会带来疼痛治疗的新机遇。