Category Ranking
98%
Total Visits
921
Avg Visit Duration
2 minutes
Citations
20
Article Abstract
A series of arylpiperazinylbutyl derivatives of 4,5-dihydro-1,2,4-triazine-6(1H)-ones was designed and synthesized according to the new solid-supported methodology. In this approach, triazinone scaffold was constructed from the Fmoc-protected glycine. The library representatives showed different levels of affinity for 5-HT7 and 5-HT1A receptors; compounds 13, 14 and 18-20 were classified as dual 5-HT7 /5-HT1A receptors ligands. The structure-affinity relationship analysis revealed that the receptor affinity and selectivity of the tested compounds depended on the kind of substituent in position 3 of triazinone fragment as well as substitution pattern of the phenylpiperazine moiety.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1111/cbdd.12539 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Role of 5-HT and 5-HT Receptors in Memory Regulation and the Importance of Their Coexpression: A Systematic Review.
Biomolecules
May 2025
Obesity and Asthma Research Laboratory, Hospital Infantil de México Federico Gómez, Mexico City 06720, Mexico.
The 5-HT and 5-HT receptors play a key role in regulating cognitive processes and have been widely linked to the pathophysiology of depression, anxiety, and schizophrenia-disorders often associated with memory impairment. Recently, interest has grown in understanding how the coexpression of these receptors contributes to cognitive decline. This review explores the individual roles of 5-HT and 5-HT receptors, as well as their coexpression, in memory regulation.
View Article and Find Full Text PDFTherapeutic Effects of Pharmacological Modulation of Serotonin Brain System in Human Patients and Animal Models of Fragile X Syndrome.
Int J Mol Sci
March 2025
Department of Clinical and Experimental Medicine, University of Messina, 98125 Messina, Italy.
The brain serotonin (5-HT) system modulates glutamatergic and GABAergic transmission in almost every brain area, crucially regulating mood, food intake, body temperature, pain, hormone secretion, learning and memory. Previous studies suggest a disruption of the brain 5-HT system in Fragile X Syndrome, with abnormal activity of the 5-HT transporter leading to altered 5-HT brain levels. We provide an update on therapeutic effects exerted by drugs modulating serotonergic transmission on Fragile X patients and animal models.
View Article and Find Full Text PDFBehavioral Consequences of Hippocampal 5-HT7 Receptors Blockade in Stressed Rats.
Hippocampus
January 2025
Laboratório de Neurobiologia Do Estresse e da Depressão, Faculdade de Filosofia, Ciências e Letras de Ribeirão Preto, Universidade de São Paulo, Ribeirão Preto, SP, Brazil.
Serotonin (5-HT) has long been involved in response to stress and its effect may be, in part, mediated by 5-HT1a and 5-HT7 receptor subtypes in different brain structures. Both pre- and post-synaptic activation of 5-HT1a receptor, respectively, in the rat median raphe nucleus (MnRN) and hippocampus, lead to adaptation to acute inescapable stressors such as restraint and forced swim. 5-HT7 receptor (5HT7r), a stimulatory G-protein coupled receptor, has also been investigated as a possible candidate for mediating stress response.
View Article and Find Full Text PDFTargeting serotonin receptors with phytochemicals - an in-silico study.
Sci Rep
December 2024
Department of Management, Bar-Ilan University, Ramat Gan, 5290002, Israel.
Article Synopsis
- * An evaluation of 88 phytochemicals identified five (Genistein, Kaempferol, Daidzein, Peonidin, and glycitein) with strong pharmacokinetic properties and effective binding to serotonin receptors.
- * The study suggests these phytochemicals, commonly found in soybeans and various plants, could lead to natural depression treatments, but more research is needed to confirm their effectiveness in real-world applications.
Vortioxetine-Induced Bleeding Tendency in a Young Woman with Depression: A Case Report.
Psychiatry Clin Psychopharmacol
November 2024
Department of Psychiatry and Psychiatric Research Center, Taipei Medical University Hospital, Taipei, Taiwan.
Vortioxetine, which functions as a 5-HT3, 5-HT1D, and 5-HT7 antagonist, a 5-HT1A agonist, and a 5-HT1B partial agonist, is a recently launched antidepressant approved by the United States Food and Drug Administration for treating adult major depressive disorder. Although hematological adverse effects have been associated with antidepressants, massive bleeding is a rare but potentially life-threatening complication. In this case report, we present a young woman who experienced abnormal bleeding tendencies, with manifestations including tarry stools, ecchymosis, and massive uterine bleeding, while undergoing vortioxetine treatment.
View Article and Find Full Text PDF