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
为什么选择此级别
Moligand™ 级 ，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 8 篇同行评审文献引用。
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=
技术文档
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）
信号词
Warning
危险声明
H315: 引起皮肤刺激
H319: 引起严重眼睛刺激
H335: 可能引起呼吸道刺激
H400: 对水生生物有剧毒
预防措施声明
P261: 避免吸入灰尘/烟雾/气体/雾/蒸汽/喷雾
P305+P351+P338: 如进入眼睛：用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出，取出隐形眼镜。继续冲洗。
P273: 避免释放到环境中。
P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。
P302+P352: 如皮肤沾染：用水充分清洗。
P321: 特殊处理（请参阅此标签上的...）。
P405: 密闭存放
P501: 将内容物/容器处理到。。。
P264: 处理后要彻底洗手。
P271: 仅在室外或通风良好的地方使用。
P304+P340: 如误吸入：将人转移到空气新鲜处，保持呼吸舒适体位。
P403+P233: 存放在通风良好的地方。保持容器密闭。
P362+P364: 脱掉沾污的衣服，清洗后方可重新使用。
P391: 收集溢出物
P264+P265: 处理后彻底洗手[和…]。不要触摸眼睛。
P337+P317: 如果眼睛刺激持续：寻求医疗帮助。
P332+P317: 如果出现皮肤刺激：请寻求医疗帮助。
P319: 如果你感到不适，请寻求医疗帮助。
WGK Germany
3
Merck Index
190
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