کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1373604 | 981903 | 2007 | 7 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: M4 agonists/5HT7 antagonists with potential as antischizophrenic drugs: Serominic compounds M4 agonists/5HT7 antagonists with potential as antischizophrenic drugs: Serominic compounds](/preview/png/1373604.png)
Chronic low-dose treatment of rats with the psychomimetic drug, phencyclidine, induces regionally specific metabolic and neurochemical changes in the CNS that mirror those observed in the brains of schizophrenic patients. Recent evidence suggests that drugs targeting serotoninergic and muscarinic receptors, and in particular 5-HT7 antagonists and M4 agonists, exert beneficial effects in this model of schizophrenia. Compounds that display this combined pattern of activity we refer to as serominic compounds. Based upon leads from natural product screening, we have designed and synthesised such serominic compounds, which are principally arylamidine derivatives of tetrahydroisoquinolines, and shown that they have the required serominic profile in ligand binding assays and show potential antipsychotic activity in functional assays.
Based upon the activity of natural products, new compounds with activity in an in vivo model of schizophrenia have been designed and synthesised.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 9, 1 May 2007, Pages 2649–2655