Synthesis, chiral resolution, absolute configuration assignment and pharmacological evaluation of a series of melatoninergic ligands

MedChemComm ◽  
2014 ◽  
Vol 5 (9) ◽  
pp. 1303-1308 ◽  
Author(s):  
Mohamed Ettaoussi ◽  
Basile Pérès ◽  
Christian Jarry ◽  
Olivier Nosjean ◽  
Jean A. Boutin ◽  
...  

(−)-R-Enantiomers of agomelatine analogues were more potent at serotonin 5-HT2C receptors than (+)-S-enantiomers, and showed antidepressant-like properties in a tail suspension test.

MedChemComm ◽  
2014 ◽  
Vol 5 (10) ◽  
pp. 1590-1590
Author(s):  
Mohamed Ettaoussi ◽  
Basile Pérès ◽  
Christian Jarry ◽  
Viviane Pallage ◽  
Olivier Nosjean ◽  
...  

Heliyon ◽  
2017 ◽  
Vol 3 (6) ◽  
pp. e00316 ◽  
Author(s):  
Kentaro Hiraoka ◽  
Keisuke Motomura ◽  
Satoru Yanagida ◽  
Ayako Ohashi ◽  
Nozomi Ishisaka-Furuno ◽  
...  

Author(s):  
Ajoy Borah ◽  
Binita Singha ◽  
Swopna Phukan

Objective: Depression is a major psychiatric disorder affecting nearly 350 million people worldwide and imposes a substantial health burden on the society. Ceftriaxone has demonstrated neuroprotective effects in animals. It has also undergone trials as a treatment option for amyotrophic lateral sclerosis. This study was therefore undertaken to evaluate the antidepressant-like effect of ceftriaxone in mice.Methods: Ceftriaxone was administered at three different doses (0.130, 0.195 and 0.260g/kg) to Swiss albino mice of either sex by intra peritoneal (i. p.) route. The period of immobility in control and drug-treated mice were recorded in forced swimming test (FST) and tail suspension test (TST). The antidepressant effect of ceftriaxone indicated by the decrease in duration of immobility was compared to that of fluoxetine (0.020 g/kg, i. p.).Results: Ceftriaxone decreased the duration of immobility in mice. It showed a significant dose-dependent antidepressant effect. The antidepressant effect of 0.260g/kg of ceftriaxone was comparable to that of fluoxetine in the TST but not in the FST.Conclusion: The results of the present study indicate antidepressant activity of Ceftriaxone. The study shows that ceftriaxone has additional action on the central nervous system other than neuroprotection. Ceftriaxone therapy in cases of encephalomeningitis and in various cases of hemorrhages in the brain can, therefore, prevent the development of depression in future


2007 ◽  
Vol 62 (1) ◽  
pp. 81-91 ◽  
Author(s):  
Xiaoqing Liu ◽  
Devin Stancliffe ◽  
Samuel Lee ◽  
Shelly Mathur ◽  
Howard K. Gershenfeld

2019 ◽  
pp. 01-12
Author(s):  
Rui Li ◽  
Wai-Kin Mat ◽  
Wing-Man Chan ◽  
T Yiu-Cheong Ho ◽  
Rigil K Yeung ◽  
...  

The racemate dl-tetrahydropalmatine (dl-THP) is known for its analgesic and sedative effects, and has been shown by us to be a potential agent for the treatment of anxiety.Herein, to delineate the therapeutic potentials of its different isomeric forms, the behavioral effects of l-THP, dl-THP and d-THP were compared regarding their anxiolytic and antidepressant properties in mouse behavioral models using the elevated plus-maze test and tail suspension test respectively. The anxiolytic and antidepressant effects of both l-THP and dl-THP were evident in forty-five minutes following oral administration. Moreover, l-THP exhibited much greater anxiolytic potency in the elevated plus-maze (0.1-2.5 mg/kg) and antidepressant potency in the tail suspension test (0.5-5.0 mg/kg) than dl-THP, whereas d-THP was inactive in either of these tests. As well, l-THP enhanced sociability and preference for social novelty at 0.1-0.5 mg/kg in Crawley’s three-chamber behavioral tests, and inhibited the amphetamine-induced manic-like hyperactivity of amphetamine-sensitized mice at 0.05-0.2 mg/kg. These pharmacological actions of l-THP were unaccompanied by any significant locomotor or myorelaxant side-effects. Co-administration of flumazenil, a GABAA receptor antagonist, inhibited the anxiolytic and antidepressant effects of l-THP, even though the binding affinity of l-THP was higher for dopamine D2-like receptors than for GABAA receptors. On this basis, l-THP displayed potential as a fast-acting drug for the treatment of anxiety, depression and bipolar disorder. Keywords: l-THP; dl-THP; Anxiolysis; Antidepressant; GABAA receptor; Fast-acting


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