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AGOMELATINE

Antidepressants Pharmacological effects Health risk Patent cases Uses
AGOMELATINE
AGOMELATINE structure
CAS No.
138112-76-2
Chemical Name:
AGOMELATINE
Synonyms
S 20098;Thymanax;Valdoxan;AGOMELATIN;AGOMELATINE;Agomelantine;Unii-137R1N49ad;Agomelatine, >=99%;Agomelatine (Form I,II );AgoMelatine(S-20098,Valdoxan)
CBNumber:
CB8500647
Molecular Formula:
C15H17NO2
Formula Weight:
243.30098
MOL File:
138112-76-2.mol

AGOMELATINE Properties

Melting point:
107-109°C
storage temp. 
-20°C Freezer
solubility 
DMSO: >50mg/mL
form 
powder
color 
white to off-white
Merck 
14,190
InChIKey
YJYPHIXNFHFHND-UHFFFAOYSA-N
CAS DataBase Reference
138112-76-2(CAS DataBase Reference)
SAFETY
  • Risk and Safety Statements
  • Hazard and Precautionary Statements (GHS)
Hazard Codes  N
Risk Statements  50
Safety Statements  61
RIDADR  UN 3077 9 / PGIII
WGK Germany  3
RTECS  AC5956323
HS Code  29241990
Symbol(GHS):
Signal word: Warning
Hazard statements:
Code Hazard statements Hazard class Category Signal word Pictogram P-Codes
H400 Very toxic to aquatic life Hazardous to the aquatic environment, acute hazard Category 1 Warning P273, P391, P501
Precautionary statements:
P273 Avoid release to the environment.

AGOMELATINE price More Price(7)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich A1362 Agomelatine ≥98% (HPLC) 138112-76-2 5mg $65.4 2018-11-13 Buy
Sigma-Aldrich A1362 Agomelatine ≥98% (HPLC) 138112-76-2 25mg $277 2018-11-13 Buy
TCI Chemical A2606 Agomelatine >98.0%(HPLC)(N) 138112-76-2 1g $237 2018-11-22 Buy
Cayman Chemical 13203 Agomelatine ≥98% 138112-76-2 5mg $61 2018-11-13 Buy
Cayman Chemical 13203 Agomelatine ≥98% 138112-76-2 10mg $116 2018-11-13 Buy

AGOMELATINE Chemical Properties,Uses,Production

Antidepressants

Agomelatine, which is developed by the French Servier company, is the world's first melatonin receptors MT1 and MT2 agonist class of antidepressants. It applies to the treatment of adult patients with severe depressive. We know that melatonin is an endogenous neural hormones. It is only produced by the pineal gland anterior pituitary at night, and acts on the melatonin receptor that focuses on the presence of hypothalamic suprachiasmatic nucleus (SCN). It is involved in mediating the circadian rhythms in mammals. It is the well-known time guardian in the body, which can regulate the biological clock that is modulated by external circadian cycle. However, since that melatonin has high catabolism rate in vivo which mikes its half-life shorter and the selectivity of its receptor located in the SCN poorer, the treatment of circadian rhythms disorders is limited. Therefore, in order to overcome these drawbacks of melatonin, the researchers designed a series of melatonin analogues. Molecular modeling studies have shown that indole ring of melatonin is the structure sites of catabolic inactivation. Indole ring is an ideal site of isosteric modifications. Agomelatine developed by Servier company is melatonin’s naphthalene biological (electronic) isostere analogs. Indole ring is substituted by naphthalene nucleus, which leads it have more metabolic stability than melatonin.

Pharmacological effects

The listing of agomelatine is a new breakthrough in the field of the treatment of depression. It is melatonin MT1/MT2 receptor agonist and serotonin 2c (5-HT2C) receptor antagonist. It can make depressed patients’ biological rhythm disorders return to normal through the synergy between the two and then result in antidepressant efficacy. Its unique mechanism of action has opened up an innovative way to treat depression. Agomelatine’s mechanism of drug action is completely different with antidepressants that are commonly used today, such as selective serotonin reuptake inhibitors (SSRI) and serotonin-norepinephrine reuptake inhibitors (SNRI). SSRI and SNRI antidepressants achieve antidepressant efficacy by increasing concentration of serotonin. But it also brings a lot of side effects, such as weight changes, sexual dysfunction, withdrawal syndrome and the like. The molecular structure of agomelatine directly combines with serotonin 2c (5HT2c) receptor of post-synaptic membrane so as to exert its antidepressant efficacy without increasing serotonin concentration in the synaptic cleft. This unique mechanism of action makes agomelatine quickly and effectively exert its antidepressant efficacy at the same time, and avoid the occurrence of adverse drug reactions to an extreme.
Another unique targets of agomelatine is in melatonin receptors. MT1 and MT2 receptors densely distribute in the human suprachiasmatic nucleus. The nucleus mainly control human sleep rhythm. Agomelatine can well improve the quality of patients’ sleep by agonism on MT1 MT2 receptors, and improve patients’ wakefulness during the day. The quality of sleep has both cause and effect relationship with depression outcomes state. It is reported that 80% of patients with depression have the problems of sleep disorders at different levels. The improvement of sleep quality can directly contribute to the improvement of the overall clinical condition of patients with depression.
The above information is edited by the Chemicalbook of Ge Qian.

Health risk

October 30, 2012, the British Medicines and Healthcare Products Agency (MHRA) released agomelatine (agomelatine, Valdoxan/Thymanax) security information. MHRA found that several cases appears serious reports of liver toxicity with agomelatine, including six cases of liver failure patients within worldwide report. Agomelatine's drug information already includes in the recommendations that all patients need liver function tests at the start of treatment and during treatment. Now liver function tests should also be recommended when the drug dose is increased. MHRA recommends that if the patients have potential liver damage symptoms or signs, or that the increases of serum transaminase beyond the upper limit of normal (ULN) three times is found in the function tests, it should be immediately suspended.

Patent cases

The earliest agomelatine compound patent is French Patent FR902393, which is applied in February 27, 1990. This patent has the same patent family in Europe, USA, Canada, Japan and Australia. But there is no Chinese patent. The above patents were all authorized after January 1, 1993. Therefore China is also ineligible for administrative protection. Agomelatine has both technology patent and polymorph patent in China. But it also can be avoided.

Uses

Melatonin drugs.

Chemical Properties

White Solid

Uses

Agomelatine is an antidepressant drug. 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

Uses

Agomelatine is a melatoninergic agonist and selective antagonist of 5-HT2C receptors, and has been shown to be active in several animal models of depression. Agomelatine (S20098) displayed pKi values of 6.4 and 6.2 at native (porcine) and cloned, human (h)5-hydroxytryptamine (5-HT)2C receptors, respectively.

AGOMELATINE Preparation Products And Raw materials

Raw materials

Preparation Products


AGOMELATINE Suppliers

Global( 269)Suppliers
Supplier Tel Fax Email Country ProdList Advantage
Lianyungang happen teng technology co., LTD
15950718863
wang666xt@163.com CHINA 305 58
Liaoning Benyuan Pharmaceutical Co., Ltd
024-45627555
024-45627566 sales@benyuanpharm.com China 62 50
Shenzhen Sendi Biotechnology Co.Ltd.
0755-23311925 18102838259
0755-23311925 Abel@chembj.com CHINA 3203 55
Henan DaKen Chemical CO.,LTD.
+86-371-55531817
info@dakenchem.com CHINA 21935 58
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com CHINA 20676 55
Mainchem Co., Ltd.
+86-0592-6210733
+86-0592-6210733 sales@mainchem.com CHINA 32452 55
Nanjing Finetech Chemical Co., Ltd.
025-85710122 17714198479
025-85710122 sales@fine-chemtech.com CHINA 892 55
ATK CHEMICAL COMPANY LIMITED
+86 21 5161 9050/ 5187 7795
+86 21 5161 9052/ 5187 7796 ivan@atkchemical.com CHINA 24196 60
Zjartschem
+86-571-8723 8903 jocelynpan@zjarts.com
+86-571-87063838 jocelynpan@zjarts.com CHINA 998 58
Xiamen AmoyChem Co., Ltd
+86 (0)592-605 1114
sales@amoychem.com CHINA 6374 58

View Lastest Price from AGOMELATINE manufacturers

Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
2018-08-16 AGOMELATINE
138112-76-2
US $11.00 / KG 1KG 99% 1000KG career henan chemical co

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