| Title : M4 agonists\/5HT7 antagonists with potential as antischizophrenic drugs: serominic compounds - Suckling_2007_Bioorg.Med.Chem.Lett_17_2649 |
| Author(s) : Suckling CJ , Murphy JA , Khalaf AI , Zhou SZ , Lizos DE , van Nhien AN , Yasumatsu H , McVie A , Young LC , McCraw C , Waterman PG , Morris BJ , Pratt JA , Harvey AL |
| Ref : Bioorganic & Medicinal Chemistry Lett , 17 :2649 , 2007 |
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Abstract :
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-HT(7) antagonists and M(4) 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. |
| PubMedSearch : Suckling_2007_Bioorg.Med.Chem.Lett_17_2649 |
| PubMedID: 17317171 |
Suckling CJ, Murphy JA, Khalaf AI, Zhou SZ, Lizos DE, van Nhien AN, Yasumatsu H, McVie A, Young LC, McCraw C, Waterman PG, Morris BJ, Pratt JA, Harvey AL (2007)
M4 agonists\/5HT7 antagonists with potential as antischizophrenic drugs: serominic compounds
Bioorganic & Medicinal Chemistry Lett
17 :2649
Suckling CJ, Murphy JA, Khalaf AI, Zhou SZ, Lizos DE, van Nhien AN, Yasumatsu H, McVie A, Young LC, McCraw C, Waterman PG, Morris BJ, Pratt JA, Harvey AL (2007)
Bioorganic & Medicinal Chemistry Lett
17 :2649