Agomelatine
(Synonyms: 阿戈美拉汀; S-20098) 目录号 : GC17981Agomelatine是一种褪黑素(MT)受体激动剂,对MT1和MT2的Ki值分别为0.1 nM和0.12 nM。Agomelatine也是一种5-羟色胺(5-HT)受体拮抗剂,对5-HT2C 和5-HT2B 的Ki值分别为631 nM和660 nM。
Cas No.:138112-76-2
Sample solution is provided at 25 µL, 10mM.
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Cell experiment [1]: | |
Cell lines | HUVEC cells |
Preparation method | HUVECs were exposed to Ang II (1μM) with or without Agomelatine (10, 20 μM) for 24 h. |
Reaction Conditions | 10, 20 μM; 24 h |
Applications | Introduction of 10 and 20μM Agomelatine prevented the increase in AT1R expression induced by exposure to Ang II, with the higher dose having a more robust inhibitory effect. |
Animal experiment [2]: | |
Animal models | LPS-induced rat model of depression |
Preparation method | Agomelatine was dissolved in 1% hydroxyethyl cellulose (HEC) solution. In all experiments, agomelatine (40mg/kg) was administered via an i.p. injection at 60 min prior to daily LPS procedures. |
Dosage form | 40mg/kg; i.p. |
Applications | Agomelatine can reverse LPS-induced depression-like behavior in rats and reduce the neuroinflammatory response in the DG area of the brain. |
References: [1] Hong N, Ye Z, Lin Y, et al. Agomelatine prevents angiotensin II-induced endothelial and mononuclear cell adhesion[J]. Aging (albany NY), 2021, 13(14): 18515. [2]Lan T, Wu Y, Zhang Y, et al. Agomelatine rescues lipopolysaccharide-induced neural injury and depression-like behaviors via suppression of the Gαi-2-PKA-ASK1 signaling pathway[J]. Journal of neuroinflammation, 2022, 19(1): 117. |
Agomelatine is a melatonin (MT) receptor agonist with Ki values of 0.1 nM and 0.12 nM for MT1 and MT2, respectively[1]. Agomelatine is also a 5-hydroxytryptamine (5-HT) receptor antagonist with Ki values of 631 nM and 660 nM for 5-HT2C and 5-HT2B respectively[2]. Agomelatine can regulate circadian rhythm and enhance mood, and is used in research on major depressive disorder (MDD) [3].
In vitro, Agomelatine (10, 20 μM) treated endothelial cells and monocytes for 24 h, dose-dependently inhibited the angiotensin II-induced increase in the expression of AT1R, VCAM-1 and ICAM-1 and reduced cell adhesion [4]. Agomelatine (8, 16 μM) treated hippocampal neuron HT22 cells for 24 hours, inhibited the neurotoxicity caused by cisplatin injury, and attenuated oxidative stress and inflammatory response [5].
In vivo, Agomelatine (40mg/kg) was treated by intraperitoneal injection in rats with LPS-induced depression and significantly improved the rats' anxiety and depression-like behaviors, reducing neuroinflammation and neuronal damage[6]. Agomelatine (25, 50 or 75 mg/kg; ip) has antioxidant activity in a mouse seizure model [7].
References:
[1] Dridi D, Zouiten A, Mansour H B. Depression: chronophysiology and chronotherapy[J]. Biological rhythm research, 2014, 45(1): 77-91.
[2] Millan M J, Gobert A, Lejeune F, et al. The novel melatonin agonist agomelatine (S20098) is an antagonist at 5-hydroxytryptamine2C receptors, blockade of which enhances the activity of frontocortical dopaminergic and adrenergic pathways[J]. Journal of Pharmacology and Experimental Therapeutics, 2003, 306(3): 954-964.
[3] Smeraldi E, Delmonte D. Agomelatine in depression[J]. Expert opinion on drug safety, 2013, 12(6): 873-880.
[4] Hong N, Ye Z, Lin Y, et al. Agomelatine prevents angiotensin II-induced endothelial and mononuclear cell adhesion[J]. Aging (albany NY), 2021, 13(14): 18515.
[5] Cankara F N, Günaydın C, Çelik Z B, et al. Agomelatine confers neuroprotection against cisplatin-induced hippocampal neurotoxicity[J]. Metabolic brain disease, 2021, 36(2): 339-349.
[6] Lan T, Wu Y, Zhang Y, et al. Agomelatine rescues lipopolysaccharide-induced neural injury and depression-like behaviors via suppression of the Gαi-2-PKA-ASK1 signaling pathway[J]. Journal of neuroinflammation, 2022, 19(1): 117.
[7] Aguiar C C T, Almeida A B, Araújo P V P, et al. Effects of agomelatine on oxidative stress in the brain of mice after chemically induced seizures[J]. Cellular and molecular neurobiology, 2013, 33: 825-835.
Agomelatine是一种褪黑素(MT)受体激动剂,对MT1和MT2的Ki值分别为0.1 nM和0.12 nM[1]。Agomelatine也是一种5-羟色胺(5-HT)受体拮抗剂,对5-HT2C 和5-HT2B 的Ki值分别为631 nM和660 nM[2]。Agomelatine可以调节昼夜节律和提升情绪,应用于重度抑郁症(MDD)研究[3]。
在体外,Agomelatine(10、20μM)处理内皮细胞和单核细胞24h,剂量依赖性地抑制了血管紧张素II诱导的AT1R、VCAM-1和ICAM-1的表达增加,减少了细胞粘附[4]。Agomelatine(8、16μM)处理海马神经元HT22细胞24h,抑制了顺铂损伤引起的神经毒性,减弱了氧化应激和炎症反应[5]。
在体内,Agomelatine(40mg/kg)通过腹膜注射治疗LPS诱导的抑郁症大鼠,显著改善了大鼠的焦虑和抑郁样行为,减轻了神经炎症和神经元损伤[6]。Agomelatine (25、50或75 mg/kg;ip) 在小鼠癫痫发作模型中具有抗氧化活性[7]。
Cas No. | 138112-76-2 | SDF | |
别名 | 阿戈美拉汀; S-20098 | ||
化学名 | N-[2-(7-methoxynaphthalen-1-yl)ethyl]acetamide | ||
Canonical SMILES | CC(=O)NCCC1=CC=CC2=C1C=C(C=C2)OC | ||
分子式 | C15H17NO2 | 分子量 | 243.3 |
溶解度 | ≥ 12.2mg/mL in DMSO | 储存条件 | Store at -20°C |
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1 mM | 4.1102 mL | 20.5508 mL | 41.1015 mL |
5 mM | 0.822 mL | 4.1102 mL | 8.2203 mL |
10 mM | 0.411 mL | 2.0551 mL | 4.1102 mL |
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