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.
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http://dx.doi.org/10.1016/j.bmcl.2008.08.084 | DOI Listing |
CNS Drugs
January 2025
New York State Psychiatric Institute, 1051 Riverside Drive, New York, NY, 10032, USA.
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 PDFJ Neurol Neurosurg Psychiatry
January 2025
Department of Neurology, Medical Faculty, Heinrich Heine University Düsseldorf, Düsseldorf, Germany
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 PDFJ Neurol Neurosurg Psychiatry
January 2025
Department for Neuromuscular Disease, National Hospital for Neurology and Neurosurgery, Queen Square, London, UK.
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).
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