（±）-南天竹宁类似物作为人5-羟色胺（2A）受体拮抗剂：C1及柔性类似物
(+/-)-Nantenine analogs as antagonists at human 5-HT(2A) receptors: C1 and flexible congeners.
作者信息
Chaudhary Sandeep, Pecic Stevan, Legendre Onica, Navarro Hérnan A, Harding Wayne W
机构信息
Department of Chemistry, Hunter College, and the Graduate Center of the City University of New York, 695 Park Avenue, New York, NY 10065, USA.
出版信息
Bioorg Med Chem Lett. 2009 May 1;19(9):2530-2. doi: 10.1016/j.bmcl.2009.03.048. Epub 2009 Mar 16.
Abstract
C1 and flexible analogs of (+/-)-nantenine were synthesized and evaluated for antagonist activity at human 5-HT(2A) receptors in a calcium mobilization assay. This work has resulted in the identification of the most potent 5-HT(2A) antagonist known based on an aporphine. Our results also suggest that the C1 position may be a key site for increasing 5-HT(2A) antagonist activity in this compound series. In addition, the structural rigidity of the aporphine core appears to be required for nantenine to function as a 5-HT(2A) antagonist.
摘要
合成了（±）-南天竹宁的C1及柔性类似物，并在钙动员试验中评估了它们对人5-HT（2A）受体的拮抗活性。这项工作已鉴定出基于阿朴啡的已知最强效5-HT（2A）拮抗剂。我们的结果还表明，在该化合物系列中，C1位可能是增强5-HT（2A）拮抗活性的关键位点。此外，阿朴啡核心的结构刚性似乎是南天竹宁发挥5-HT（2A）拮抗剂功能所必需的。
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