A1362
阿戈美拉汀
≥98% (HPLC)
别名:
N-[2-（7-甲氧基-1-萘基）乙基]-乙酰胺, S-20098
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关于此项目
经验公式（希尔记法）:
C15H17NO2
化学文摘社编号:
分子量:
243.30
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
产品名称
阿戈美拉汀, ≥98% (HPLC)
InChI key
YJYPHIXNFHFHND-UHFFFAOYSA-N
SMILES string
COc1ccc2cccc(CCNC(C)=O)c2c1
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)
assay
≥98% (HPLC)
form
powder
color
white to off-white
solubility
DMSO: >50 mg/mL
originator
Servier
storage temp.
2-8°C
Quality Level
Gene Information
human ... HTR2C(3358), MTNR1A(4543), MTNR1B(4544)
相关类别
Application
阿戈美拉汀已被用于：
- 采用应激诱导的大鼠抑郁模型研究其对成年神经形成和海马细胞凋亡的影响
- 探讨其对tau蛋白磷酸化的影响并研究其神经保护机制
- 研究其对大鼠背根神经节（DRG）神经元周围神经元细胞内钙（[Ca2+] i）信号传导的影响
Biochem/physiol Actions
褪黑素受体（MT1 和 MT2）上，阿戈美拉汀是一种非常有效的激动剂，在 5HT2C 上具有额外的拮抗作用。
阿戈美拉汀是两种褪黑素受体（MT1 和 MT2）的强效激动剂，对 5-HT2C 具有额外的拮抗作用。它是一种新型抗抑郁药，具有许多理想的体内特性，包括抑郁敏感脑区的神经保护和神经发生。阿戈美拉汀褪黑素能和 5-羟色胺能都是影响疗效的因素。在体外和体内的神经发生实验中，MT1/MT2 和 5HT2C 的拮抗剂对化合物的影响不同，这表明通过这三种受体的作用。
阿戈美拉汀通过其时相性（chronobiotic）活性来调节睡眠-觉醒周期。它可使抑郁症和季节性情感障碍患者的睡眠模式正常化。
signalword
Warning
hcodes
pcodes
Hazard Classifications
Aquatic Acute 1 - Aquatic Chronic 1
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Alejandro Martínez-Águila et al.
European journal of pharmacology, 701(1-3), 213-217 (2012-12-29)
In the search for new compounds to reduce intraocular pressure (IOP), with fewer side effects, we have found that agomelatine, a melatonin analogue, can reduce IOP being, therefore, interesting for the treatment of ocular hypertension and glaucoma. In normotensive conditions
Siegfried Kasper et al.
International clinical psychopharmacology, 28(1), 12-19 (2012-10-02)
Pooled analysis of individual patient data was used to compare the antidepressant efficacy of agomelatine with that of selective serotonin reuptake inhibitors (SSRIs) and serotonin and noradrenaline reuptake inhibitors (SNRIs). We sought head-to-head, double-blind, randomized studies without a placebo arm
Nikos Maniadakis et al.
BMC health services research, 13, 173-173 (2013-05-15)
Major depressive disorder (MDD) constitutes an important public health problem, as it is highly prevalent in the industrialized world and it is associated with substantial economic consequences for patients, health care providers, insurance and social security organizations and employers. To
Trevor R Norman
Expert opinion on investigational drugs, 22(4), 407-410 (2013-03-15)
Alteration of nocturnal melatonin production, along with circadian rhythm disturbance, has been demonstrated in several psychiatric disorders. It has been postulated that such disturbances might be causal reflecting a more fundamental abnormality of the function of the suprachiasmatic nucleus (SCN).
Michelle Nigri Levitan et al.
Experimental and clinical psychopharmacology, 20(6), 504-509 (2012-10-24)
Agomelatine is an antidepressant with a novel mechanism of being a selective melatonergic MT₁/MT₂ receptor agonist with serotonin 5-HT(2c) receptor antagonist activities. Although the vast majority of the clinical data concerning the effectiveness of agomelatine concern its antidepressant properties, there
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