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药物靶标
G蛋白偶联受体（GPCR）
褪黑激素受体
阿戈美拉汀, 羟色胺 2c (5-HT2c) 受体拮抗剂

阿戈美拉汀, 羟色胺 2c (5-HT2c) 受体拮抗剂

强大的MT 1 / MT 2激动剂和5-HT 2C拮抗剂

规格或纯度: ≥98%(HPLC)

CAS编号: 138112-76-2
分子式: C₁₅H₁₇NO₂
分子量: 243.3
MDL号: MFCD00916659
PubChem编号: 82148

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货号 (SKU)	包装规格	是否现货
A124691-5mg	5mg	现货
A124691-25mg	25mg	现货
A124691-50mg	50mg	现货
A124691-250mg	250mg	现货
A124691-1g	1g	现货
A124691-5g	5g	现货
A124691-25g	25g	现货

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基本描述

别名	N-[2-(7-甲氧基-1-萘基)乙基]乙酰胺
英文别名	Agomelatine\|138112-76-2\|Thymanax\|Valdoxan\|N-(2-(7-Methoxynaphthalen-1-yl)ethyl)acetamide\|N-[2-(7-methoxynaphthalen-1-yl)ethyl]acetamide\|S20098\|S-20098\|Agomelatine [INN]\|Melitor\|AGO-178\|S 20098\|Acetamide, N-[2-(7-methoxy-1-naphthalenyl)ethyl]-\|N-(2-(7-meth
规格或纯度	≥98%(HPLC)
英文名称	Agomelatine
生化机理	Agomelatine is a competitive antagonist of human and porcine serotonin (5-HT2C) receptors (pKi = 6.2 and 6.4, respectively) as well as human 5-HT2B receptors (pKi = 6.6). It is classified as a norepinephrine-dopamine disinhibitor (NDDI) due to its antagonism of the 5-HT2C receptor. Activation of 5-HT2C receptors by serotonin inhibits dopamine and norepinephrine release. Antagonism of 5-HT2C results in an enhancement of DA and NE release and activity of frontocortical dopaminergic and adrenergic pathways. Agomelatine is also a potent agonist at melatonin receptors which makes it the first melatonergic antidepressant. Agomelatine is an antidepressant drμg.Potent MT 1 /MT 2 agonist (K i values are 0.1 and 0.12 nM, respectively). 5-HT 2C antagonist (IC 50 = 270 nM). Shows antidepressant effects in vivo . Orally active.
储存温度	2-8°C储存
运输条件	冰袋运输
备注	5mg，25mg，50mg售完停产，不再备货。如果有可能，您尽量在使用的当天配置溶液，并在当天使用完它。但是，如果您需要预先配制储备溶液，我们建议您将溶液等份保存在-20°C的密封小瓶中。通常，它们最多可以使用一个月。在使用前和打开样品瓶之前，我们建议您让您的产品在室温下平衡至少1小时。需要更多关于溶解度，用法和处理的建议吗？请访问我们的常见问题（FAQ）页面以获取更多详细信息。
产品介绍	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. 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 through all three receptors.

产品属性

ALogP	2.7

名称和标识符

PubChem SID	488186059
PubChem SID url	https://pubchem.ncbi.nlm.nih.gov/substance/488186059
IUPAC Name	N-[2-(7-methoxynaphthalen-1-yl)ethyl]acetamide
INCHI	InChI=1S/C15H17NO2/c1-11(17)16-9-8-13-5-3-4-12-6-7-14(18-2)10-15(12)13/h3-7,10H,8-9H2,1-2H3,(H,16,17)
InChi Key	YJYPHIXNFHFHND-UHFFFAOYSA-N
Canonical SMILES	CC(=O)NCCC1=CC=CC2=C1C=C(C=C2)OC
Isomeric SMILES	CC(=O)NCCC1=CC=CC2=C1C=C(C=C2)OC
WGK Germany	3
PubChem CID	82148
分子量	243.3

数据库链接

PubChem CID	82148
Wikipedia	Agomelatine
ChEMBL Ligand	CHEMBL10878
BindingDB Ligand	50035179
DrugBank Ligand	DB06594
CAS Registry No.	138112-76-2
RCSB PDB Ligand	AWY
DrugCentral Ligand	99
GPCRdb Ligand	agomelatine
PubChem SID	488186059

化学和物理性质

溶解性	可溶于甲醇
敏感性	对热敏感
熔点	110 °C

安全和危险性（GHS）

象形图	Environmental Hazard Harmful
信号词	Warning
危险声明	H315: Causes skin irritation H319: Causes serious eye irritation H335: May cause respiratory irritation H400: Very toxic to aquatic life
预防措施声明	P261,P305+P351+P338,P273,P280,P302+P352,P321,P405,P501,P264,P271,P304+P340,P403+P233,P362+P364,P391,P264+P265,P337+P317,P332+P317,P319
WGK Germany	3
Merck Index	190

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参考文献

1. Guardiola-Lemaitre B, De Bodinat C, Delagrange P, Millan MJ, Munoz C, Mocaër E. (2014) Agomelatine: mechanism of action and pharmacological profile in relation to antidepressant properties.. Br J Pharmacol, 171 (15): (3604-19). [PMID:24724693]