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

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

  • Bioorg Med Chem Lett. 2009 May 1;19(9):2530-2. doi: 10.1016/j.bmcl.2009.03.048.
Sandeep Chaudhary 1,  Stevan Pecic,  Onica Legendre,  Hérnan A Navarro,  Wayne W Harding
Affiliations

Affiliation

  • 1 Department of Chemistry, Hunter College, and the Graduate Center of the City University of New York, 695 Park Avenue, New York, NY 10065, USA.
PMID: 19328689 DOI: 10.1016/j.bmcl.2009.03.048
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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