2-Aryl Tryptamines: Selective High-Affinity Antagonists For The H5-Ht2a Receptor

Graeme I Stevenson,Adrian L Smith,Stephen Lewis,Stephen G Michie,Joseph G Neduvelil,Smita Patel,Rosemarie Marwood,Shil Patel,José L Castro

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS（2000）

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摘要

A series of 2-aryl tryptamines have been identified as high-affinity h6-HT2A antagonists. Structure-activity relationship studies have shown that h5-HT2A affinity can be attained via modifications to the tryptamine side chain and that selectivity over h5-HT2C and hD(2) receptors can be controlled by suitable C-2 aryl groups. (C) 2000 Elsevier Science Ltd. All rights reserved.

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