Dexmedetomidine
(Synonyms: 右美托咪定; (+)-Medetomidine; (S)-Medetomidine) 目录号 : GC17494
Dexmedetomidine是一种高选择性α2-肾上腺素能受体激动剂，可在脑内特定区域发挥交感神经抑制作用，具有镇痛、镇静和抗焦虑效应。
Cas No.:113775-47-6
Sample solution is provided at 25 µL, 10mM.
Dexmedetomidine is a highly selective α2-adrenergic receptor agonist that exerts sympatholytic effects in specific brain regions, providing analgesic, sedative, and anxiolytic actions[1-2]. In addition, Dexmedetomidine preconditioning effectively shields the heart against ischemia-reperfusion injury[3].
In vitro, after 3 days of treatment with graded Dexmedetomidine concentrations (0.05μM, 0.1μM, 1μM, 2.5μM, 5μM, or 10μM), cortical neurons showed unchanged viability below 10μM but a significant drop in viability and increased cell death at 10μM[4]. Exposure of PC12 cells to Dexmedetomidine at 50ng/ml, 200ng/ml, or 800ng/ml for 12 or 24h enhanced cell viability in both a time- and dose-dependent manner[5].
In vivo, in acute liver injury (ALI) C57BL/6 mice, a single intraperitoneal dose of Dexmedetomidine (200mg/kg) markedly blunted the rises in ALT and AST and suppressed the ALI-induced elevations of serum IL-6, IL-8, IL-1β, and TNF-α[6]. In male C57BL/6 mice, a single intraperitoneal dose of Dexmedetomidine (40μg/kg) suppresses lipopolysaccharide (LPS)-induced inflammatory factor expression and protects renal cells from apoptosis[7]. Administering Dexmedetomidine (10 or 20μg/kg; i.p.) to Sprague-Dawley rats dose-dependently reduces mortality and suppresses pulmonary inflammation by inhibiting the Toll-like receptor 4 (TLR4)/myeloid differentiation factor 88 (MyD88)/NF-κB pathway[8].
References:
[1] Hou M, Chen F, He Y, et al. Dexmedetomidine against intestinal ischemia/reperfusion injury: A systematic review and meta-analysis of preclinical studies. Eur J Pharmacol. 2023;959:176090.
[2] Dardalas I, Stamoula E, Rigopoulos P, et al. Dexmedetomidine effects in different experimental sepsis in vivo models. Eur J Pharmacol. 2019;856:172401.
[3] Takahashi K, Yoshikawa Y, Kanda M, et al. Dexmedetomidine as a cardioprotective drug: a narrative review. J Anesth. 2023;37(6):961-970.
[4] Jimenez-Tellez N, Iqbal F, Pehar M, et al. Dexmedetomidine does not compromise neuronal viability, synaptic connectivity, learning and memory in a rodent model. Sci Rep. 2021;11(1):16153.
[5] Guo Q, Ma M, Yu H, et al. Dexmedetomidine enables copper homeostasis in cerebral ischemia/reperfusion via ferredoxin 1. Ann Med. 2023;55(1):2209735.
[6] Zhang C, Fan Y, Qin Z, et al. Network pharmacology and experimental validation reveal dexmedetomidine's protective mechanisms against acute liver injury in mice. Sci Rep. 2025;15(1):9044.
[7] Kang K, Gao Y, Wang SC, et al. Dexmedetomidine protects against lipopolysaccharide-induced sepsis-associated acute kidney injury via an α7 nAChR-dependent pathway. Biomed Pharmacother. 2018;106:210-216.
[8] Wu Y, Liu Y, Huang H, et al. Dexmedetomidine inhibits inflammatory reaction in lung tissues of septic rats by suppressing TLR4/NF-κB pathway. Mediators Inflamm. 2013;2013:562154.
Dexmedetomidine是一种高选择性α2-肾上腺素能受体激动剂，可在脑内特定区域发挥交感神经抑制作用，具有镇痛、镇静和抗焦虑效应[1-2]。此外，Dexmedetomidine预处理可有效保护心脏免受缺血-再灌注损伤[3]。
在体外，经0.05、0.1、1、2.5、5或10μM梯度浓度Dexmedetomidine处理3天后，皮层神经元在10μM以下活力无明显变化，而10μM时活力显著下降并出现细胞死亡增加[4]。用50、200或800ng/ml的Dexmedetomidine处理PC12细胞12或24小时，可在时间和剂量依赖性方式下提高细胞活力[5]。
在体内，在急性肝损伤（ALI）C57BL/6小鼠中，单次腹腔注射200mg/kg的Dexmedetomidine可显著降低ALT和AST的升高，并抑制ALI诱导的血清IL-6、IL-8、IL-1β和TNF-α水平[6]。在雄性C57BL/6小鼠中，单次腹腔注射40μg/kg的Dexmedetomidine可抑制脂多糖（LPS）诱导的炎症因子表达并保护肾细胞免于凋亡[7]。对Sprague-Dawley大鼠腹腔给予10或20μg/kg的Dexmedetomidine可剂量依赖性地降低死亡率，并通过抑制Toll样受体4（TLR4）/髓样分化因子88（MyD88）/NF-κB通路减轻肺部炎症[8]。
| Cell experiment [1]: | |
Cell lines | Cortical neurons |
Preparation Method | Sprague-Dawley rat frontal cortices were isolated and cultured. Some cultures were treated with various concentrations of Dexmedetomidine (0.05μM, 0.1μM, 1μM, 2.5μM, 5μM, or 10μM) dissolved in culture media, whereas controls only had culture media. The cells were cultured for 3 or 7 days. |
Reaction Conditions | 0.05μM, 0.1μM, 1μM, 2.5μM, 5μM, or 10μM; 3 or 7 days |
Applications | On days 3 and 7 after Dexmedetomidine exposure, no significant effect on cell viability was observed at concentrations below 10μM. However, at 10μM, Dexmedetomidine markedly reduced cell viability, resulting in increased cell death: the percentage of viable cells on day 3 was significantly lower than that of controls. By day 7, none of the tested concentrations exerted any additional effect on viability. |
| Animal experiment [2]: | |
Animal models | C57BL/6 mice |
Preparation Method | C57BL/6 mice (eight-week-old, male, 22-25g) were housed at an ambient temperature of 22±2°C under a fixed 12h light/dark cycle. Prior to experimentation, animals were randomly assigned into three groups (n=6 per group): Control (Con), acute liver injury (ALI) model, and ALI+Dexmedetomidine: 200mg/kg. The ALI model was induced by intraperitoneally injecting lipopolysaccharide (LPS)/D-galactose (D-Gal) (200μL; 30μg/kg; 600mg/kg) dissolved in PBS. Dexmedetomidine was administered intraperitoneally 1h prior to the LPS/D-Gal challenge. At 6h after LPS/D-Gal treatment, the mice were then anesthetized with isoflurane and subjected to enucleation for exsanguination. Subsequently, the liver tissues were harvested, fixed with formalin, and embedded in paraffin. |
Dosage form | 200mg/kg; administered intraperitoneally |
Applications | Dexmedetomidine treatment significantly suppressed the increases in ALT and AST levels, as well as the elevations of serum IL-6, IL-8, IL-1β, and TNF-α in the ALI model group. |
References: | |
| Cas No. | 113775-47-6 | SDF | |
| 别名 | 右美托咪定; (+)-Medetomidine; (S)-Medetomidine | ||
| 化学名 | 5-[(1S)-1-(2,3-dimethylphenyl)ethyl]-1H-imidazole | ||
| Canonical SMILES | CC1=C(C(=CC=C1)C(C)C2=CN=CN2)C | ||
| 分子式 | C13H16N2 | 分子量 | 200.28 |
| 溶解度 | ≥ 9.95mg/mL in DMSO | 储存条件 | Store at -20°C |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.993 mL | 24.965 mL | 49.9301 mL |
| 5 mM | 0.9986 mL | 4.993 mL | 9.986 mL |
| 10 mM | 0.4993 mL | 2.4965 mL | 4.993 mL |
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