We examined the effect of chronic administration of imipramine and bupropion, monoamine reuptake inhibitors, on the duration of immobility in the forced swim test and serotonin (5-HT)(2A) receptor function in the form of 5-HT(2A) receptor mRNA levels in rats chronically treated with adrenocorticotropic hormone (ACTH). The immobility-decreasing effect of bupropion without imipramine did not influence the chronic ACTH treatment. The effect on the expression of 5-HT(2A) receptor mRNA of chronic ACTH treatment was decreased by bupropion, but not imipramine. These results suggest that bupropion has the effect of reducing immobility time in the forced swim test in the tricyclic antidepressant-resistant depressive model induced by chronic ACTH treatment in rats, and that decreased 5-HT(2A) receptor mRNA levels may be involved in this phenomenon.
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http://dx.doi.org/10.1248/bpb.31.246 | DOI Listing |
Brain Res
December 2024
Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen 2100, Denmark. Electronic address:
Psychedelics show promise in treating psychiatric disorders. Therapeutic effects appear to involve activation of the 5-Hydroxytryptamine 2A receptor (5-HTR), a G protein-coupled receptor (GPCR). Several SNPs of the 5-HTR naturally occur, which are associated with differences in receptor function and altered responsiveness to treatments.
View Article and Find Full Text PDFAnn Med
December 2025
Department of Anatomy, College of Medicine, King Khalid University, Abha, Saudi Arabia.
Background: Substance use disorders are multifaceted conditions influenced by both genetic and environmental factors. Serotonergic pathways are known to be involved in substance use disorder susceptibility, with genetic markers within serotonin receptor genes identified as potential risk factors.
Methods: To further explore this relationship, we conducted a study to investigate the association between several polymorphisms in five serotonin receptor genes (, , ) and substance use disorders (SUD) in Jordanian males by sequencing genotypes in 496 SUD patients and 496 healthy controls.
Expert Opin Pharmacother
December 2024
Department of Psychiatry, Yale University School of Medicine, New Haven, CT, USA.
Introduction: Substance use disorders (SUDs) are a public health issue, with only some having FDA-approved indicated treatments and these having high attrition. Consequently, there has been interest in novel interventions (e.g.
View Article and Find Full Text PDFExpert Opin Drug Saf
December 2024
Shanghai Mental Health Center, Shanghai Jiao Tong University School of Medicine, Shanghai, China.
Background: Sexual dysfunction (SD) is a commonly occurring yet often underestimated adverse event associated with the use of antidepressants. This study aimed to analyze the reporting of SD associated with the use of antidepressants in comparison with one another, and to explore potential receptor mechanisms based on the real-world data from the Food and Drug Administration Adverse Event Reporting System (FAERS).
Methods: Disproportionality analysis was conducted based on FAERS reports (2004 Q1 to 2024 Q2) using reporting odds ratios (ROR) and information components (IC) methods.
ACS Chem Neurosci
December 2024
Designer Drug Research Unit, National Institute on Drug Abuse, Intramural Research Program, Baltimore, Maryland 21224, United States.
5-methoxy-,-dimethyltrytpamine (5-MeO-DMT) analogs are used as recreational drugs, but they are also being developed as potential medicines, warranting further investigation into their pharmacology. Here, we investigated the neuropharmacology of 5-MeO-DMT and several of its -alkyl, -allyl, and 2-methyl analogs, with three major aims: 1) to determine in vitro receptor profiles for the compounds, 2) to characterize in vitro functional activities at serotonin (5-HT) 2A receptors (5-HT) and 1A receptors (5-HT), and 3) to examine the influence of 5-HT on 5-HT-mediated psychedelic-like effects in the mouse head twitch response (HTR) model. In vitro receptor binding and functional assays showed that all 5-MeO-DMT analogs bind with high affinity and activate multiple targets (e.
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