We investigated the antidepressant-like action of 5 compounds belonging to the selenophene class. The involvement of ERK and CREB activation in this action was also demonstrated. In the experiment 1, time-course and dose-response effect of H-DPS, CH3-DPS, Cl-DPS, F-DPS and CF3-DPS were accompanied in the mouse forced swimming test (FST). Firstly, animals received compounds at a dose of 50mg/kg, by intragastric (i.g.) route, at different times (15-240 min) before test. Results showed that the peak of maximum anti-despair behavior induced by Cl-DPS, F-DPS and CF3-DPS was at 30 min; maximum effect of H-DPS and CH3-DPS was found at 60 min, which was maintained until 120 min. Regarding dose-response effect, all compounds reduced immobility time and increased latency for the first episode of immobility at a dose of 50mg/kg. In addition, F-DPS also showed antidepressant-like action at a dose of 25mg/kg, whilst H-DPS, CH3-DPS, Cl-DPS and CF3-DPS were not effective at lower doses. Thus, F-DPS was chosen for further investigation of its mechanism of action. Experiment 2 showed that treatment of animals with F-DPS (50 mg/kg, i.g.) significantly increased phosphorylated ERK1/2 levels in the prefrontal cortex and hippocampus; however, pCREB levels were not affected. Additionally, in the experiment 3 anti-immobility effect of F-DPS was completely blocked by pretreatment of animals with PD 98,059, an inhibitor of ERK phosphorylation, suggesting that ERK signalling activation is involved in its antidepressant-like action in mice. Together our data appoint F-DPS as a promising molecule for the development of a new antidepressant therapy.
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http://dx.doi.org/10.1016/j.ejphar.2014.04.033 | DOI Listing |
Dokl Biochem Biophys
January 2025
Center for Strategic Planning and Management of Biomedical Health Risks, Federal Medical and Biological Agency, Moscow, Russia.
Unlabelled: The association of the pathogenesis of neurodegenerative diseases, depression, anxiety, and cognitive disorders with neurotrophin-3 deficiency determines the prospect of creating drugs with a similar mechanism of action. Since the use of full-length NT-3 is limited by unsatisfactory pharmacokinetic properties, the creation of low-molecular mimetics of neurotrophin-3 that are active when administered systemically is relevant. The Federal Research Center for Innovator and Emerging Biomedical and Pharmaceutical Technologies has created a dimeric dipeptide mimetic of the 4th loop of NT-3, hexamethylenediamide bis-(N-γ-oxybutyryl-L-glutamyl-L-asparagine) with the laboratory code GTS-302, which activates TrkC and TrkB receptors.
View Article and Find Full Text PDFPharmaceuticals (Basel)
December 2024
School of Life Sciences, Guangzhou University, Guangzhou 510006, China.
Background: Durazz. is one of the most popular herbs used for depression treatment, but the molecular basis for its mechanism of action has not been fully addressed. Previously, we isolated and identified two lignan glycoside derivatives that were shown to noncompetitively inhibit serotonin transporter (SERT) activity but with a relatively low inhibitory potency compared with those of conventional antidepressants.
View Article and Find Full Text PDFJ Ethnopharmacol
December 2024
School of Life Sciences & School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing, 100029, People's Republic of China. Electronic address:
Ethnopharmacological Relevance: Cornus officinalis Sieb. et Zucc has significant neuroprotective activity and has been widely studied for its potential to improve cognitive function. Our team's previous research has found that loganin isolated from Cornus officinalis has an antidepressant effect.
View Article and Find Full Text PDFNeuropharmacology
March 2025
Instituto de Farmacologia e Neurociências, Faculdade de Medicina, Universidade de Lisboa, Avenida Professor Egas Moniz, Edifício Egas Moniz, 1649-028, Lisboa, Portugal; Gulbenkian Institute for Molecular Medicine, Avenida Professor Egas Moniz, 1649-028, Lisboa, Portugal; Centro Cardiovascular da Universidade de Lisboa, CCUL (CCUL@RISE), Faculdade de Medicina, Universidade de Lisboa, Avenida Professor Egas Moniz, Edifício Egas Moniz, 1649-028, Lisboa, Portugal. Electronic address:
Psychedelic Med (New Rochelle)
December 2024
Departments of Anesthesiology and Critical Care, Perelman School of Medicine, University of Pennsylvania, Philadelphia, Pennsylvania, USA.
Introduction: Psychedelic-induced experiences are thought to play an important role in the therapeutic actions of rapid-acting antidepressants. General anesthesia is one scenario in which patients can be rendered unconscious and masked to the psychedelic treatment, providing a simple yet effective method to examine drug-induced changes in the brain devoid of experiences.
Methods: Chronically stressed adult C57/BL6 male mice were given subhypnotic ketamine alone or ketamine and GABAergic anesthetic isoflurane at sedative (0.
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