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 158876-82-5 Rupatadine

Rupatadine
(CAS: 158876-82-5)

Rupatadine, with the potential to treat allergic rhinitis and urticaria, is a potent and long-lasting dual antagonist of PAF/H1. in vitro: Without affecting con...

CAS 152811-62-6 Piboserod

Piboserod
(CAS: 152811-62-6)

Piboserod is a highly and potent selective 5-HT4 receptor antagonist which as been studied in vitro as well as in vivo as a pharmacological tool to evaluate the...

CP-809101 hydrochloride
(CAS: 1215721-40-6)

The hydrochloride salt form of CP-809101 which is a selective 5-HT2C receptor agonist which probably shows antipsychotic activity and restrains amphetamine-stim...

CAS 107007-99-8 Granisetron HCl

Granisetron HCl
(CAS: 107007-99-8)

Granisetron HCl is a serotonin 5-HT3 receptor antagonist.

Ziprasidone-d8
(CAS: 1126745-58-1)

A labelled form of Ziprasidone which is an antagonist of both 5-HT and dopamine receptor and it has been studied to show effective antipsychotic activity.

CAS 30123-17-2 Tianeptine sodium

Tianeptine sodium
(CAS: 30123-17-2)

Tianeptine sodium is a selective serotonin reuptake enhancer (SSRE), used for treating major depressive episodes.

CAS 133454-47-4 Iloperidone

Iloperidone
(CAS: 133454-47-4)

Iloperidone displays high affinity (Ki < 10 nM) for norepinephrine alpha(1)-adrenoceptors, dopamine D(3) and serotonin 5-HT(2A) receptors.

CAS 133025-23-7 Way 100135

Way 100135
(CAS: 133025-23-7)

Way 100135 is a selective 5-HT1A receptor antagonist originated by Wyeth with IC50 value of 15 nM. IC 50 values for 5-HT1B, 1C, 2,α1, α2 and D2 receptors are ov...

Agomelatine L(+)-Tartaric acid
(CAS: 824393-18-2)

Agomelatine L(+)-Tartaric acid is classified as a norepinephrine-dopamine disinhibitor (NDDI) due to its antagonism of the 5-HT2C receptor. It is used as an ant...

CAS 607742-69-8 SB742457

SB742457
(CAS: 607742-69-8)

SB742457 is a selective 5-HT6 receptor antagonist with potential cognition, memory, and learning-enhancing effects.It was under development by GlaxoSmithKline f...

CAS 866206-54-4 PRX 08066

PRX 08066
(CAS: 866206-54-4)

PRX 08066, a selective 5-hydroxytryptamine receptor 2B(5-HT2BR) antagonist, causes selective vasodilation of pulmonary arteries. Its IC50 value is 3.4 nM. It ca...

CAS 193611-72-2 BRL-15572

BRL-15572
(CAS: 193611-72-2)

BRL-15572 displays high affinity and selectivity for h5-HT1D receptors. BRL-15572 has 60-fold higher affinity for h5-HT1D than 5-HT1B receptors.

CAS 123040-16-4 Azasetron hydrochloride

Azasetron hydrochloride
(CAS: 123040-16-4)

Azasetron HCl is a selective 5-HT3 receptor antagonist with IC50 of 0.33 nM used in the management of nausea and vomiting induced by cancer chemotherapy.

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...

CAS 706779-91-1 Pimavanserin

Pimavanserin
(CAS: 706779-91-1)

Pimavanserin is a potent and selective 5-HT2A receptor inverse agonist used in the treatment of Parkinson’s disease psychosis.

CAS 146939-27-7 Ziprasidone

Ziprasidone
(CAS: 146939-27-7)

Ziprasidone is a combined 5-HT (serotonin) and dopamine receptor antagonist like other atypical antipsychotic agents. Ziprasidone targets dopamine neurotransmis...

CAS 10457-90-6 Bromperidol

Bromperidol
(CAS: 10457-90-6)

Bromperidol, a derivative of butyrophenone, is an antipsychotic commonly used in the treatment of schizophrenia as it could bind to the D2 dopamine and 5-HT2A s...

CAS 170381-16-5 Zicronapine

Zicronapine
(CAS: 170381-16-5)

Zicronapine, an inden derivative, has been found to be neurotransmitter receptor modulators of sorts of neurotransmitter and was studied against Schizophrenia.

CAS 59729-32-7 Citalopram hydrobromide

Citalopram hydrobromide
(CAS: 59729-32-7)

Citalopram Hydrobromide is an inhibitor of serotonin (5-HT) uptake used as an antidepressant.

CAS 122852-43-1 Alosetron (Z)-2-butenedioate

Alosetron (Z)-2-butenedioate
(CAS: 122852-43-1)

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

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.