计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
有货
概述
Agomelatine is an extremely potent agonist at both melatonin receptors (MT1 and MT2), with additional antagonism at 5HT2C. It is a novel antidepressant with many desired in vivo properties, including neuroprotection and neurogenesis in depression-sensitive brain areas. Agomelatine′s efficacy appears to be due to both melatonergic and serotonergic properties. In neurogenesis assays, both in vitro and in vivo, the compound effects were differentially affected by antagonists for MT1/MT2 and 5HT2C, demonstrating actions throμgh all three receptors.
Information
Agomelatine (S20098) is classified as a norepinephrine-dopamine disinhibitor (NDDI) due to its antagonism of the 5-HT2C receptor.
In vitro
Agomelatine completely normalizes stress-affected cell survival and partly reverses reduced doublecortin expression in the hippocampus of rats subjected to chronic footshock stress.
In vivo
Agomelatine is effective in reversing the transgenic mouse behavioural changes noted in the Porsolt forced swim test as well as in the elevated plus maze. Agomelatine also markedly accelerates readjustment of circadian cycles of temperature and activity following an induced phase shift. Agomelatine enhances cell proliferation and neurogenesis in the ventral hippocampus (VH) of adult rats, a region pertinent to mood disorders. Agomelatine increases the ratio of mature vs immature neurons and enhances neurite outgrowth of granular cells in adult rats, suggesting an acceleration of maturation. Agomelatine also activates several cellular signals (extracellular signal-regulated kinase1/2, protein kinase B, and glycogen synthase kinase 3beta) known to be modulated by antidepressants and implicated in the control of proliferation/survival. Agomelatine enhances the time devoted to active social interaction in unfamiliar pairs of rats exposed to a novel environment. Agomelatine increases cell proliferation and neurogenesis in the ventral dentate gyrus of rats, a region notably implicated in response to emotion, which is consistent with the antidepressant-anxiolytic properties of Agomelatine. Agomelatine increases survival of newly formed neurons in the entire dentate gyrus of rats.
Cell Data
cell lines：
Concentrations：
Incubation Time：
Powder Purity:≥99%
规格
英文别名
N-(2-(7-methoxynaphthalen-1-yl)ethyl)acetamide
规格或纯度
Moligand™, 10mM in DMSO
英文名称
Agomelatine (S20098)
生化机理
阿戈美拉汀（S20098）被归类为去甲肾上腺素-多巴胺抑制剂（NDDI），因为它能拮抗 5-HT2C 受体。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
激动剂
作用机制
羟色胺 2c (5-HT2c) 受体拮抗剂
名称和识别符
EC号
629-727-7
分子类型
小分子
Isomeric SMILES
CC(=O)NCCC1=CC=CC2=C1C=C(C=C2)OC
分子量
243.3
Reaxy-Rn
5813634
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=5813634&ln=
高级数据
产品属性
| ALogP | 2.7 |
|---|
关联靶点（人）
HTR2A
Tclin
5-羟色胺受体 2A(5-hydroxytryptamine receptor 2A)
(1 活性数据)
HTR2C
Tclin
5-羟色胺受体 2C(5-hydroxytryptamine receptor 2C)
(1 活性数据)
HTR2B
Tclin
5-羟色胺受体 2B(5-hydroxytryptamine receptor 2B)
(1 活性数据)
MTNR1A
Tclin
褪黑激素受体 1A 型(Melatonin receptor type 1A)
(16 活性数据)
MTNR1B
Tclin
褪黑激素受体 1B 型(Melatonin receptor type 1B)
(17 活性数据)
化学和物理性质
溶解性
Solubility (25°C) In vitro DMSO: 4 mg/mL (21.72 mM);
熔点
110 °C
安全和危险性（GHS）
象形图
信号词
警告
危险声明
H227: 可燃液体
预防措施声明
P210: 远离热源，热表面，火花，明火和其他点火源。 - 禁止抽烟。
P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。
P370+P378: 火灾时：使用干砂、干粉或抗醇泡沫灭火。
P403+P235: 存放在通风良好的地方。保持低温。
P501: 将内容物/容器送到批准的废物处理厂处理
WGK Germany
3
Merck Index
190
质检证书(CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
技术文档和文章
此产品的引用文献
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