(+/-)-Nantenine analogs as antagonists at human 5-HT(2A) receptors: C1 and flexible congeners.
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.
Chaudhary
Sandeep
S
Department of Chemistry, Hunter College, and the Graduate Center of the City University of New York, 695 Park Avenue, New York, NY 10065, USA.
Pecic
Stevan
S
Legendre
Onica
O
Navarro
Hérnan A
HA
Harding
Wayne W
WW