SB 366791 is a potent and selective vanilloid receptor (VR1/TRPV1) antagonist with an IC50 value of 5.7nM [1]. SB 366791 can reduce the release rates of substance P (SP) and calcitonin gene-related peptide (CGRP) and alleviate thermal hyperalgesia [2]. SB 366791 has been widely used to limit morphine addiction in mice and alleviate the behavioral changes caused by opioids [3].
In vitro, SB 366791 (10µM) was pre-treated for 1 hour, which significantly inhibited HT22 cell apoptosis induced by sevoflurane, and reduced the increase in TRPV1 mRNA and protein expression [4]. Treatment with 3µM SB 366791 for 24 hours significantly inhibited the chemotactic activity of mouse-derived microglial cells induced by capsaicin and prevented the decrease in mitochondrial membrane potential[5].
In vivo, SB 366791 treatment via a single intraperitoneal injection at a dose of 500µg/kg for 20 minutes significantly inhibited the hypothermia, wiping movements, and vascular dilation of the knee joint induced by capsaicin in rats[6]. Oral administration of a 10mg/kg/day dose of SB 366791 for 15 days alleviated the epileptic seizures induced by pentylenetetrazole (PTZ) in mice, improved spatial cognitive impairment, and increased GSH levels[7].
References:
[1] Gunthorpe M J, Rami H K, Jerman J C, et al. Identification and characterisation of SB-366791, a potent and selective vanilloid receptor (VR1/TRPV1) antagonist[J]. Neuropharmacology, 2004, 46(1): 133-149.
[2] Mazeto T K, Picada J N, Correa Á P, et al. Antinociceptive and genotoxic assessments of the antagonist TRPV1 receptor SB-366791 on morphine-induced tolerance in mice[J]. Naunyn-Schmiedeberg's Archives of Pharmacology, 2020, 393(3): 481-490.
[3] Ma S X, Kwon S H, Seo J Y, et al. Impairment of opiate‐mediated behaviors by the selective TRPV1 antagonist SB366791[J]. Addiction biology, 2017, 22(6): 1817-1828.
[4] Liu Y, Yang H, Sun C, et al. Protective effects of TRPV1 inhibition against sevoflurane-induced cell death[J]. Neuroscience Letters, 2019, 707: 134270.
[5] Miyake T, Shirakawa H, Nakagawa T, et al. Activation of mitochondrial transient receptor potential vanilloid 1 channel contributes to microglial migration[J]. Glia, 2015, 63(10): 1870-1882.
[6] Varga A, Németh J, Szabó Á, et al. Effects of the novel TRPV1 receptor antagonist SB366791 in vitro and in vivo in the rat[J]. Neuroscience letters, 2005, 385(2): 137-142.
[7] Tian X, Xu X. Therapeutic Investigation of Zingerone Against Pentylenetetrazole-Induced Kindled Seizures in Mice[J]. Iranian Journal of Pharmaceutical Research: IJPR, 2025, 24(1): e162878.
SB 366791是一种强效且选择性的vanilloid receptor（VR1/TRPV1）拮抗剂，IC50值为5.7nM[1]。SB 366791可降低P物质(SP)和降钙素基因相关肽(CGRP)的释放速率，并减轻热痛觉过敏[2]。SB 366791已被广泛用于限制小鼠的吗啡成瘾，并减轻阿片类药物引起的行为改变[3]。
在体外，10µM的SB 366791预处理1小时，显著抑制了sevoflurane诱导的HT22细胞凋亡，并抑制了TRPV1 mRNA和蛋白表达增加[4]。3µM的SB 366791处理24小时，显著抑制了辣椒素(capsaicin)诱导的小鼠来源小胶质细胞的趋化活性，并阻止了线粒体膜电位的下降[6]。
在体外，单次腹腔注射500µg/kg剂量的SB 366791 20分钟，显著抑制了capsaicin诱导的大鼠体温过低、擦拭动作和膝关节血管扩张[6]。每日口服10mg/kg剂量的SB 366791，连续15天，减轻了pentylenetetrazole (PTZ)诱导的小鼠癫痫发作，改善了空间认知障碍，并提高了GSH水平[7]。