Agomelatine - CAS 138112-76-2
Not Intended for Therapeutic Use. For research use only.
Category:
Inhibitor
Product Name:
Agomelatine
Catalog Number:
138112-76-2
Synonyms:
trade names: Valdoxan, Melitor, Thymanax.
CAS Number:
138112-76-2
Description:
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.
COA:
Inquire
MSDS:
Inquire
Targets:
5-HT Receptor
Chemical Structure
CAS 138112-76-2 Agomelatine

Related 5-HT Receptor Products


CAS 866933-46-2 Velusetrag

Velusetrag
(CAS: 866933-46-2)

Velusetrag is a selective, 5-HT4receptor agonist. Phase II clinical trials for the treatment of gastroparesis are on-going. Clnical trials for Alzheimer's disea...

Asenapine hydrochloride
(CAS: 1412458-61-7)

Asenapine hydrochloride, also called Org 5222 and HSDB 8061, shows high affinity for numerous receptors including 5-HT receptor and adrenergic receptor. (pKi: 5...

CAS 479683-64-2 CP 809101 hydrochloride

CP 809101 hydrochloride
(CAS: 479683-64-2)

CP-809101 is a potent and selective 5-HT2C receptor agonist (pEC50=9.96).

CAS 222551-17-9 Adoprazine

Adoprazine
(CAS: 222551-17-9)

Adoprazine, also known as SLV 313, with potential antipsychotic property, is a agonist of cloned h5-HT(1A) receptors (pEC(50)=9.0) and a full antagonist of hD(2...

Iloperidone hydrochloride
(CAS: 1299470-39-5)

The hydrochloride salt form of Iloperidone which is a antagonist of both D2 and 5-HT2 receptor and has been commonly used against schizophrenia. IC50: 10-100 nm...

Mirisetron maleate
(CAS: 148611-75-0)

Mirisetron maleate, an oxoquinoline derivative, has been found to be a 5-HT3 receptor antagonist that could probably be effective against anxiety disorders and ...

CAS 34233-69-7 Clozapine N-oxide

Clozapine N-oxide
(CAS: 34233-69-7)

Clozapine N-oxide is a major metabolite of clozapine that can be detected in the earliest excretion time interval after clozapine administration. It is produced...

SB-269970
(CAS: 201038-74-6)

SB-269970 is a selective 5-HT7 receptor antagonist (pKi of 8.3) with >50-fold selectivity against other receptors, on amphetamine and ketamine-induced hyperacti...

CAS 115956-13-3 Dalasetron Mesylate

Dalasetron Mesylate
(CAS: 115956-13-3)

The mesylate salt form of Dolasetron which is a pseudopelletierine derivative and could be used to relieve the nausea and vomiting caused by chemotherapy for be...

CAS 179756-85-5 Eptapirone

Eptapirone
(CAS: 179756-85-5)

Eptapirone, a triazine derivative, has been found to be a 5-HT1A receptor agonist and was once studied as an antidepressant agent. pKi: 8.33.

Agomelatine hydrochloride
(CAS: 1176316-99-6)

The hydrochloride salt form of Agomelatine that is an antidepressant agent for acting as an antagonism of the 5-HT2C receptor. It is also an antagonist of 5-HT2...

CAS 740873-06-7 Naluzotan

Naluzotan
(CAS: 740873-06-7)

Naluzotan is a selective 5-HT1A receptor partial agonist under the development of EPIX Pharmaceuticals. It is a serotonergic drug for the treatment of generaliz...

CAS 467458-02-2 Lu AE58054 HCl salt

Lu AE58054 HCl salt
(CAS: 467458-02-2)

Lu AE58054 hydrochloride is an in-vitro potency and selectivity, in-vivo binding affinity and effect of the 5-HT(6)R antagonist with a Ki value of 0.83 nM.

CAS 162760-96-5 WAY-100635

WAY-100635
(CAS: 162760-96-5)

WAY-100635 is an achiral analogue of WAY-100135 which is significantly more potent and selective than the latter compound and which displays unequivocal 5-HTIA ...

CAS 839712-12-8 Cariprazine

Cariprazine
(CAS: 839712-12-8)

Cariprazine is an orally active D2/D3 dopamine receptor antagonist exhibits high selectivity and affinity to dopamine D3(Ki=0.09 nM) and D2 (Ki=0.5 nM) receptor...

CAS 105826-92-4 Tropisetron HCl

Tropisetron HCl
(CAS: 105826-92-4)

Tropisetron is a selective 5-HT3 receptor antagonist and α7-nicotinic receptor agonist with an IC50 of 70.1 ± 0.9 nM for 5-HT3 receptor. It is used mainly as a...

Quetiapine D4 fumarate
(CAS: 1287376-15-1)

The isotope labelled form of Quetiapine fumarate, a 5-HT receptor antagonist, is widely used as an antipsychotic drug.

LY 293284
(CAS: 141318-62-9)

LY-293284 is a Serotonin 1A receptor agonist developed by Eli Lilly. It is a selective 5-HT1A receptor full agonist. LY-293284 is far more selective for 5-HT1A ...

CAS 122852-69-1 Alosetron HCl

Alosetron HCl
(CAS: 122852-69-1)

The hydrochloride salt form of Alosetron which is an effective 5-HT3 receptor antagonist and could be commonly used against irritable bowel syndrome.

CAS 87760-53-0 Tandospirone

Tandospirone
(CAS: 87760-53-0)

Tandospironeis a potent and selective 5-HT1A receptor partial agonist with Ki of 27 nM. It significantly reduces haloperidol-induced bradykinesia in a dose depe...

Reference Reading


1. Novel difluoroacetamide analogues of agomelatine and melatonin: probing the melatonin receptors for MT1 selectivity
Darius P. Zlotos,* Noura M. Riad, Mai B. Osman, Bala R. Dodda and Paula A. Witt-Enderby. Med. Chem. Commun.,2015, 6, 1340–1344
Agomelatine was synthesized according to our previously reported procedure. 5-Methoxytryptamine and N-desacetyl-agomelatine were prepared by amide hydrolysis of melatonin and agomelatine, respectively, using ethanolic KOH. Trifluoroagomelatine was prepared by acylation of using trifluoroacetic anhydride in pyridine as previously reported. Difluoroagomelatine (ref. 14) and dichloroagomelatine were obtained by acylation of using methyl difluoroacetate, and methyl dichloroacetate, respectively (Scheme 1).
2. Iodine salts of the pharmaceutical compound agomelatine: the effect of the symmetric H-bond on amide protonation
Eliška Skořepová,* Michal Hušák, Luděk Ridvan. CrystEngChem.,2016, 18,4518–4529
Since the existence of agomelatine hydrochloride and hydrobromide was described in the patent literature, we attempted to prepare the hydriodide AGI as well. Due to favorable reaction conditions described later, we prepared not only AGI but also three novel and structurally different iodine salts of agomelatine. Here, we present their synthesis and characterization, a comparison of crystal structures and a detailed discussion on the ionization state of the agomelatine molecule.
3. Design, synthesis and biological evaluation of fluorescent ligands for MT1 and/or MT2
G. Viault, S. Poupart, F. Suzenet*. RSC Adv.,2016, 6, 62508–62521
Melatonin (N-acetyl-5-methoxytryptamine, Scheme 1) is a neurohormone synthesized by the pineal gland during the dark period in all animal species and immediately released. The rhythm of melatonin synthesis is directly controlled by photoperiodism. Melatonin secretion both in blood and in cerebrospinal fluid transduces the photoperiodicmessage to all central or peripheral structures expressing melatoninergic receptors or binding sites, allowing synchronization of several cellular and physiological events to a given daylength. Melatonin rhythm synchronizes a wide range of physiological functions including among others circadian rhythms or seasonal reproduction. Anarchic melatonin secretion also accounts for disorders of sleep/wake rhythms associated or not with depression. Melatonin receptors play an important role in the mode of action of a few drugs such as ramelteon (Rozerem®), a melatonin agonist, employed to treat insomnia and nocturia and agomelatine (Valdoxan®), a melatonin agonist and 5-HT2C antagonist, indicated for the treatment of depression.