Investigation of a series 6-[2-(4-aryl-1-piperazinyl)ethyl]-2H-1,4-benzoxazin-3(4H)-ones has led to the discovery of potent 5-HT(1A/1B/1D) receptor antagonists with and without additional SerT affinity. Modulation of the different target activities gave compounds with a range of profiles suitable for further in vivo characterization.

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.bmcl.2008.08.084DOI Listing

Publication Analysis

Top Keywords

receptor antagonists
8
6-[2-4-aryl-1-piperazinylethyl]-2h-14-benzoxazin-34h-ones dual-acting
4
dual-acting 5-ht1
4
5-ht1 receptor
4
antagonists serotonin
4
serotonin reuptake
4
reuptake inhibitors
4
inhibitors investigation
4
investigation series
4
series 6-[2-4-aryl-1-piperazinylethyl]-2h-14-benzoxazin-34h-ones
4

Similar Publications

Article Synopsis
  • The negative symptoms of schizophrenia, like lack of emotion and motivation, are hard to treat and significantly impact daily functioning.
  • This review highlights current research on treatment options for these symptoms, categorizing them into different types and evaluating various assessment scales.
  • Although no treatments are conclusively proven as the best for these symptoms, some off-label and investigational medications show promise, including cariprazine and memantine, and further research is needed to explore new therapeutic possibilities.
View Article and Find Full Text PDF

[A Review of progresses in research on delayed resistance to EGFR-TKI by Traditional Chinese medicine via inhibiting cancer stem cells properties].

Xi Bao Yu Fen Zi Mian Yi Xue Za Zhi

January 2025

Department of Integrated Traditional Chinese and Western Medicine, Shandong First Medical University Affiliated Cancer Hospital, Jinan 250117, China. *Corresponding author, E-mail:

It has been popular and challenging to undertake researches on the delay of acquired resistance of epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKI). As key cells for tumor initiation, cancer stem cells (CSC) play an important role in the process of resistance to EGFR-TKI. Although preliminary studies found that traditional Chinese medicine (TCM) could inhibit CSC properties and delay EGFR-TKI resistance, the specific molecular mechanism remains unclear.

View Article and Find Full Text PDF
Article Synopsis
  • The study explores the effectiveness and safety of combining nivolumab, an immunotherapy drug, with chemotherapy in patients with a specific type of metastatic gastric cancer co-expressing FGFR2 and PD-L1.
  • A total of 23 patients were treated, showing a 1-year progression-free survival (PFS) rate of 30.4% and a median overall survival (OS) of 15.1 months, though the primary endpoint of improved 1-year PFS was not achieved.
  • The results highlight the need for future research on patient selection and potential combination therapies to enhance treatment outcomes in this patient population.
View Article and Find Full Text PDF

Background: Myasthenia gravis (MG) is an autoimmune disorder affecting neuromuscular junctions, leading to fluctuating muscle weakness. While many patients respond well to standard immunosuppression, a substantial subgroup faces ongoing disease activity. Emerging treatments such as complement factor C5 inhibition (C5IT) and neonatal Fc receptor (FcRn) antagonism hold promise for these patients.

View Article and Find Full Text PDF

Background: We report our experience of patients with generalised myasthenia gravis (gMG) treated with efgartigimod, an neonatal Fc receptor antagonist, under the Early Access to Medicine Scheme (EAMS) in the UK.

Methods: Data from all UK patients treated with efgartigimod under the EAMS July 2022 to July 2023 were collected retrospectively. Efgartigimod was administered as per the ADAPT protocol (consisting of a treatment cycle of four infusions at weekly intervals with further cycles given according to clinical need).

View Article and Find Full Text PDF

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!