Mucoadhesive olaminosomes are novel nanocarriers designed to control agomelatine release and enhance its bioavailability. Olaminosomes were prepared using oleic acid, oleylamine and sorbitan monooleate adopting thin film hydration technique. Chitosan HCl was added to impart the mucoadhesive prop...

Agomelatine is an antidepressant with a novel mechanism of action. It is a melatonergic agonist for MT1 and MT2 receptors and a serotonin (5-HT2C) receptor antagonist. Agomelatine has been suggested not to have adverse effects on sexual functions. However, the effects of chronic agomelatine admi...

PurposeThe purpose of this work is to investigate the effect of agomelatine on functioning compared with placebo in patients suffering from Major Depressive Disorder (MDD).

Rapid changes in the light–dark cycle cause circadian desynchronization between rhythms of spike–wave discharges (SWDs) and motor activity in genetic epileptic rats, and this is accompanied by an increase in epileptic activity. Given the close relationship between absence seizures and sleep–w...

Brain-derived neurotrophic factor (BDNF) is a neurotrophin that serves as a survival factor for neurons. Agomelatine is a novel antidepressant as well as a potent agonist of melatonin (MT), MT1 and MT2 receptor types and an antagonist of the serotonin (5HT), 5-HT2C receptor. The study herein est...

BackgroundThe novel antidepressant drug agomelatine has been observed to cause adverse effect of hepatotoxicity in clinical applications. This study was designed to explore protective agents and investigated the underlying mechanism on L02 cells.

Agomelatine is a new antidepressant drug acting as an antagonist of 5-hydroxytryptamine receptor 2C (5-HTR2C) and agonist of melatonergic receptors 1 and 2 (MT1 and MT2). Because of this dual action, it is an atypical antidepressant. The aim of this study was to investigate chronic anticonvulsan...

In this study, agomelatine Form I was selectively recrystallized from molten state induced by ethyl cellulose (EC). It was found EC could effectively inhibit the transformation process of Form I to Form II. The effect of EC on the recrystallization of agomelatine from molten state was studied in...

The effects of melatonin and melatonin analogs in experimental Parkinson’s disease (PD) models remain controversial. Agomelatine, a novel analog of melatonin, is both agonists for melatonin-1 and melatonin-2 receptors and antagonist of 5-HT2C receptors. While agomelatine has been commonly used ...

SummaryIn the research for more potent antagonists of the luteinizing hormone releasing hormone (LHRH), 13 new peptides with emphasis on arginine in position 8 were designed, synthesized and tested for anti-ovulatory activity (AOA). Two very potent analogs were achieved. N-Ac-D-3-Qal, D-pClPhe, ...

Deuterium, carbon-13 and proton spin-lattice relaxation times at two fields are reported for dilute solutions of 1,1-dichloro-2,2,-bis(4-hydroxyphenyl)ethylene polyformal. The carbon-13 and proton relaxation measurements were made at a concentration of 10% (w/w) in deuterated s-tetrachloroethane...

1,2,4-Thiadiazine derivatives, like 3-methyl-7-chlorobenzo-4H-1,2,4-thiadiazine 1,1-dioxide, diazoxide and 7-chloro-3-isopropylamino-4H-benzo-1,2,4-thiadiazine 1,1-dioxide, BPDZ 73, are potent openers of Kir6.2/SUR1 KATP channels. To explore the structure–activity relationship of this series of...

A small library of emetine dithiocarbamate ester derivatives were synthesized in 25–86% yield via derivatization of the N2′- position of emetine. Anticancer evaluation of these compounds in androgen receptor positive LNCaP and androgen receptor negative PC3 and DU145 prostate cancer cell lines...

A series of esters of 4-acetyl, 4-trifluoroacetyl- and 4-(3-chloropropionyl)aminobenzenethiosulfoacids (twenty-four compounds) were synthesized and characterized by elemental analysis, 1H NMR and IR spectroscopy. The antibacterial activity of the novel candidates has been screened using the agar...

A number of novel indomethacin glycolamide esters were synthesized and tested for their cyclooxygenase (COX-1 and COX-2) inhibition properties in vitro. Many of these compounds proved to be selective COX-2 inhibitors, and subtle structural changes in the substituents on the glycolamide ester moi...

Several phenylalanine analogs have been synthesized through a four-step route starting from easily available ethyl acetamidocyanoacetate. In a first reaction, and making use of phase transfer catalysts, this compound reacted with several alkyl halides, being benzyltributylammonium chloride ident...

[18F]-N-(p-nitrobenzyl)spiperone, [18F]PNBS, was prepared and its in vivo uptake in rat brain was measured. A temporal increase in striatum:cerebellum ratio and frontal cortex:cerebellum (FC:Cb) ratio was observed. Blocking studies suggested the formation of a radiolabeled metabolite, presumably...

Preparation and property of Co(III) complex of an optically active 12-membered macrocyclic lignad (tecyclen) are reported.

A synthesis of the 5R, 8R, 9S, 11R dephosphorylated derivative of CI-920 is described. It is shown to be different from the naturally occuring dephosphorylated CI-920 where only the 5R stereochemistry has been demosntrated.

Since Factor Xa (FXa) is well known to play a central role in thrombosis and hemostasis, inhibition of FXa is an attractive target for antithrombotic strategies. As a part of our investigation of a non-peptide, orally available FXa inhibitor, we found that a series of N-[(7-amidino-2-naphthyl)me...