SB 366791是一种强效且选择性的vanilloid receptor（VR1/TRPV1）拮抗剂，IC50值为5.7nM。
Cas No.:472981-92-3
Sample solution is provided at 25 µL, 10mM.
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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]。
| Cell experiment [1]: | |
Cell lines | HT22 cells |
Preparation Method | HT22 cells were cultured in DMEM medium supplemented with 100U/ml penicillin and 100mg/ml streptomycin in 5% CO2 at 37°C. Cells were placed in a 6 well-plate at a concentration of 1×106 cells per well for 24h. The cells were pretreated with 10μM SB 366791 for 1h. Then, cells were treated with 4% sevoflurane for 6h under 5% CO2 and 21% O2. The anesthetic sevoflurane was delivered from an anesthesia machine to a custom-made sealed acrylic glass chamber containing the cells in the incubator at 37℃. Cell apoptosis was conducted. |
Reaction Conditions | 10µM; 1h |
Applications | SB 366791 treatment significantly reduced the sevoflurane-induced cell apoptosis in HT22 cells. |
| Animal experiment [2]: | |
Animal models | Male Swiss albino mice |
Preparation Method | Male Swiss albino mice (12 months old; 20-30g) were housed in a specialized animal care facility, in a room with constant temperature (25°C), humidity control, and a 12/12h light/dark cycle with free access to food and water. Mice were subjected to recurrent intraperitoneal (i.p.) treatment with a 35mg/kg dose of PTZ to induce kindled seizures (KS) over three alternate days, i.e., day 1, 3, and 5. The KS-induced mice received oral SB 366791 (10mg/kg/day) for 15 days after the third dose of PTZ (from day 6). Assessment of Kindled Seizures-Induced Spatial Cognition by the Water Y-Maze Test. |
Dosage form | 10mg/kg/day for 15 days; p.o. |
Applications | SB 366791 treatment significantly improved spatial cognitive impairment in KS-induced mice. |
References: | |
| Cas No. | 472981-92-3 | SDF | |
| 别名 | 3-(4-氯苯基)-N-(3-甲氧基苯基)-2-丙烯酰胺 | ||
| 化学名 | (E)-3-(4-chlorophenyl)-N-(3-methoxyphenyl)acrylamide | ||
| Canonical SMILES | ClC1=CC=C(C=C1)/C=C/C(NC2=CC=CC(OC)=C2)=O | ||
| 分子式 | C16H14ClNO2 | 分子量 | 287.75 |
| 溶解度 | ≥ 12.35mg/mL in DMSO | 储存条件 | Store at RT |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.4752 mL | 17.3762 mL | 34.7524 mL |
| 5 mM | 695 μL | 3.4752 mL | 6.9505 mL |
| 10 mM | 347.5 μL | 1.7376 mL | 3.4752 mL |
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动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度： mg/ml；
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