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Resiniferatoxin(超强辣素, RTX,AbMole,M8144)是一种从大戟科植物(如Euphorbia resinifera)中提取的二萜类化合物,作为瞬时受体电位香草酸亚型1(TRPV1)通道的超高效激动剂,在神经生物学与生理学研究中具有重要价值。RTX能与TRPV1通道的香草素结合位点进行高亲和力的结合,诱导通道构象变化,并稳定于开放态,最终触发非选择性阳离子内流(尤其是Ca²⁺)[1]。Resiniferatoxin(CAS No.:57444-62-9)常用于神经信号传导的研究与环路解析,特别是痛觉与温度感觉的调控。
例如Resiniferatoxin已被用于解析受伤时伤害性信号的传导、中枢敏化及神经病理性疼痛模型的分子通路;Resiniferatoxin(超强辣素)还被用于探究TRPV1阳性神经元在膀胱传入活动、交感神经张力调控及体温调节中的作用[2]。此外,Resiniferatoxin(超强辣素, RTX,AbMole,M8144)还具有抗炎活性,在动物实验中(小鼠、大鼠)显著抑制促炎因子(如TNF-α、PGE₂、IL-12、IFN-γ)的释放,并降低嗜酸性粒细胞浸润与肠道病理损伤[3]。此外,在肿瘤相关研究中,Resiniferatoxin还被用于探索TRPV1神经元活化对肺转移模型的影响[4],并在体外评估其对多种癌细胞系(如MDA-MB-231、B16F10-Luc2)的细胞毒性效应[5]。
参考文献及鸣谢
[1] Zhang, F.; Hanson, S. M.; Jara-Oseguera, A.; et al. Engineering vanilloid-sensitivity into the rat TRPV2 channel. eLife 2016, 5.
[2] Aizawa, N.; Fukuhara, H.; Fujimura, T.; et al. Direct influence of systemic desensitization by resiniferatoxin on the activities of Adelta- and C-fibers in the rat primary bladder mechanosensitive afferent nerves. International journal of urology : official journal of the Japanese Urological Association 2016, 23 (11), 952-956.
[3] Munoz-Carrillo, J. L.; Munoz-Lopez, J. L.; Munoz-Escobedo, J. J.; et al. Therapeutic Effects of Resiniferatoxin Related with Immunological Responses for Intestinal Inflammation in Trichinellosis. The Korean journal of parasitology 2017, 55 (6), 587-599.
[4] Meneses, C. S.; Gidcumb, E. M.; Marcus, K. L.; et al. Acute radiotherapy-associated oral pain may promote tumor growth at distant sites. Frontiers in oncology 2023, 13, 1029108.
[5] Rumpa, M. M.; Ngo, N. L.; Maier, C. Euphorbia bicolor Xylene Extract Induces Mitochondrial and Endoplasmic Reticulum Stress-Mediated Apoptotic Pathways in MDA-MB-231 and T47D Cells. International journal of molecular sciences 2026, 27 (2).
细胞实验参考
细胞系:Substantia gelatinosa (SG) neurons
方法:Resiniferatoxin (RTX; 0.5 μM) superfused for 1 min increases the frequency of spontaneous excitatory postsynaptic currents (sEPSCs) with a small increase in amplitude in substantia gelatinosa (SG) neurons.
浓度:0.5 μM
处理时间:1-10 min
参考文献:Neuroscience. 2009 Dec 29;164(4):1833-44.
* 上述方法来自公开文献,仅供相同目的实验参考。如实验目的、材料、方法不同,请参考其他文献。
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