Novel Aza-analogous Ergoline Derived Scaffolds as Potent Serotonin 5-HT6 and Dopamine D2 Receptor Ligands.

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• 作者：Niels Krogsgaard-Larsen ; Anders A. Jensen ; Tenna J. Schr酶der ; Claus. T. Christoffersen ; Jan Kehler
• 刊名：Journal of Medicinal Chemistry
• 出版年：2014
• 出版时间：July 10, 2014
• 年：2014
• 卷：57
• 期：13
• 页码：5823-5828
• 全文大小：322K
• ISSN：1520-4804

文摘

By introducing distal substituents on a tetracyclic scaffold resembling the ergoline structure, two series of analogues were achieved exhibiting subnanomolar receptor binding affinities for the dopamine D₂ and serotonin 5-HT₆ receptor subtype, respectively. While the 5-HT₆ ligands were antagonists, the D₂ ligands displayed intrinsic activities ranging from full agonism to partial agonism with low intrinsic activity. These structures could potentially be interesting for treatment of neurological diseases such as schizophrenia, Parkinson鈥檚 disease, and cognitive deficits.