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Literature DB >> 19328689

(+/-)-Nantenine analogs as antagonists at human 5-HT(2A) receptors: C1 and flexible congeners.

Sandeep Chaudhary¹, Stevan Pecic, Onica Legendre, Hérnan A Navarro, Wayne W Harding.

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.

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Year: 2009 PMID： 19328689 PMCID： PMC2677726 DOI： 10.1016/j.bmcl.2009.03.048

Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823

31 in total

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