Resiniferatoxin (RTX), an ultrapotent capsaicin analog, is a vanilloid agonist that binds to the transient receptor potential channel, vanilloid subfamily member 1 (TRPV1).Resiniferatoxin activates TRPV1 in an irreversible manner. It also can bind and activate members of the PKC family[1-4].
Resiniferatoxin(0.1-10µM; 24 hours) can induce G0/G1 arrest in non-transformed intestinal epithelial cells[4].
Resiniferatoxin (250ng,50µL;s.c) blocks inflammatory heat hyperalgesia when applied directly to the sciatic nerve in a time and dose dependent fashion[5]. Resiniferatoxin treatment increased serum levels of IL-4, IL-10 and IL-13, and it decreases intestinal eosinophilia, however, favours the mastocytosis, promoting T spiralis intestinal expulsion[6]. Cutaneous injection of Resiniferatoxin(100 µL of RTX 0.002% (2 g); s.c in the plantar skin) completely alleviates and prevents nerve-injury-induced neuropathic pain in rat[7].
References:
[1]. Brown DC. Resiniferatoxin: The Evolution of the "Molecular Scalpel" for Chronic Pain Relief. Pharmaceuticals (Basel). 2016 Aug 11;9(3):47. doi: 10.3390/ph9030047. PMID: 27529257; PMCID: PMC5039500.
[2]. Montell C, Birnbaumer L, et,al. A unified nomenclature for the superfamily of TRP cation channels. Mol Cell. 2002 Feb;9(2):229-31. doi: 10.1016/s1097-2765(02)00448-3. PMID: 11864597.
[3]. Gunthorpe MJ, Benham CD, et,al. The diversity in the vanilloid (TRPV) receptor family of ion channels. Trends Pharmacol Sci 2002, 23:183-191.
[4]. Frey MR, Clark JA, et,al. Cell cycle- and protein kinase C-specific effects of resiniferatoxin and resiniferonol 9,13,14-ortho-phenylacetate in intestinal epithelial cells. Biochem Pharmacol. 2004 May 15;67(10):1873-86. doi: 10.1016/j.bcp.2004.02.006. PMID: 15130764.
[5]. Neubert JK, Mannes AJ, et,al. Perineural resiniferatoxin selectively inhibits inflammatory hyperalgesia. Mol Pain. 2008 Jan 16;4:3. doi: 10.1186/1744-8069-4-3. PMID: 18199335; PMCID: PMC2242785.
[6]. MuÑoz-Carrillo JL, GutiÉrrez-Coronado O, et,al. Resiniferatoxin promotes adult worm expulsion in Trichinella spiralis-infected rats by Th2 immune response modulation. Parasite Immunol. 2021 Aug;43(8):e12840. doi: 10.1111/pim.12840. Epub 2021 May 10. PMID: 33914935.
[7]. Javed H, Johnson AM, et,al. Cutaneous Injection of Resiniferatoxin Completely Alleviates and Prevents Nerve-Injury-Induced Neuropathic Pain. Cells. 2022 Dec 14;11(24):4049. doi: 10.3390/cells11244049. PMID: 36552812; PMCID: PMC9776507.
Resiniferatoxin (RTX)是一种超强辣椒素类似物,是一种结合瞬时受体电位通道,香草蛋白亚家族成员1 (TRPV1)的香草蛋白激动剂。Resiniferatoxin以不可逆的方式激活TRPV1,它还可以结合和激活PKC家族的成员[1-4]。
Resiniferatoxin(0.1 -10µM;24 h)可诱导未转化肠上皮细胞G0/G1阻滞[4]。
Resiniferatoxin (250ng,50µL;s.c)直接作用于坐骨神经时,可阻断炎症性热痛觉过敏,且具有时间和剂量依赖性[5]。Resiniferatoxin治疗可提高血清IL-4、IL-10和IL-13水平,减少肠道嗜酸性粒细胞,但有利于肥大细胞增生,促进螺旋T虫肠道排出[6]。皮下注射Resiniferatoxin (100µL RTX 0.002% (2 g); s.c in the plantar skin)完全缓解和预防大鼠神经损伤性神经性疼痛[7]。