Starting from a high throughput screening hit, a series of 3,4-dihydro-2H-benzoxazinones has been identified with both high affinity for the 5-HT(1A) receptor and potent 5-HT reuptake inhibitory activity. The 5-(2-methyl)quinolinyloxy derivative combined high 5-HT(1A/1B/1D) receptor affinities with low intrinsic activity and potent inhibition of the 5-HT reuptake site (pK(i)8.2). This compound also had good oral bioavailability and brain penetration in the rat.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.bmcl.2004.11.030 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Advances in Antidepressant Therapy: Comparing the Efficacy of Selective Serotonin Reuptake Inhibitors (SSRIs), Serotonin-Norepinephrine Reuptake Inhibitors (SNRIs), and Novel Agents.
Cureus
December 2024
Family Medicine, Holy Family Hospital, Rawalpindi, PAK.
Introduction Depression is a prevalent and debilitating condition that often requires long-term medication management. Selective serotonin reuptake inhibitors (SSRIs) and serotonin-norepinephrine reuptake inhibitors (SNRIs) are commonly used but have limitations in efficacy and tolerability for some individuals. New antidepressant drugs targeting multiple pathways have shown potential in recent research.
View Article and Find Full Text PDFSSRI is not associated with the intensity of romantic love, obsessive thinking about a loved one, commitment, or sexual frequency in a sample of young adults experiencing romantic love.
J Affect Disord
January 2025
Discipline of Psychology, Faculty of Health, University of Canberra, Bruce, ACT, Australia; Justice and Society, University of South Australia, Magill, SA, Australia.
For >15 years, researchers have speculated that selective serotonin reuptake inhibitor (SSRI) use is associated with negative romantic love outcomes. No one has empirically investigated this, however. Drawing on 810 participants from the Romantic Love Survey 2022, we used binary logistic regression to identify differences between young adults experiencing romantic love who were and were not taking SSRIs.
View Article and Find Full Text PDFDoes Concomitant Use of Antidepressants and Direct Oral Anticoagulants Increase the Risk of Bleeding?: A Systematic Review and Meta-Analysis.
J Clin Psychopharmacol
January 2025
Department of Pharmacy, Lishui City Maternal and Child Health Care Hospital, Lishui City, Zhejiang Province, China.
Purpose: To evaluate the risk of bleeding associated with the simultaneous administration of antidepressants (ADs) and direct oral anticoagulants (DOACs).
Methods: PubMed, Embase, and Scopus databases were searched for papers that focused on the concomitant administration of ADs and DOACs and presented data on the bleeding outcomes. The comparator group of interest consisted of subjects who received only DOACs.
Challenges in the Management of Severe Serotonin Syndrome: A Case Report.
Cureus
December 2024
Psychiatry and Behavioral Sciences, Kaweah Delta Health Care District, Visalia, USA.
Serotonin syndrome (SS) is a potentially life-threatening condition that can result from excessive serotonergic activity, often due to SSRIs, formally known as selective serotonin reuptake inhibitors. The syndrome and its effects are often secondary to drug-drug interactions or dose-related. This case highlights a 47-year-old female who presents with a history of major depressive disorder, generalized anxiety disorder, and severe alcohol use disorder.
View Article and Find Full Text PDFRisk factors for hepatocellular carcinoma: an umbrella review of systematic review and meta-analysis.
Ann Med
December 2025
Department of Hepatobiliary and Pancreatic Surgery, Ningbo Medical Center Lihuili Hospital, Ningbo, Zhejiang, China.
Background: Numerous meta-analyses have identified various risk factors for hepatocellular carcinoma (HCC), prompting a comprehensive study to synthesize evidence quality and strength.
Methods: This umbrella review of meta-analyses was conducted throughout PubMed, EMBASE, Web of Science, and Cochrane Database of Systematic Reviews. Evidence strength was evaluated according to the evidence categories criteria.
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!