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Updated: Jun 24, 2026

A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
Published on: February 20, 2018
(+/-)-Nantenine analogs as antagonists at human 5-HT(2A) receptors: C1 and flexible congeners
Sandeep Chaudhary1, Stevan Pecic, Onica Legendre
1Department of Chemistry, Hunter College, and the Graduate Center of the City University of New York, 695 Park Avenue, New York, NY 10065, USA.
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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