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Synthesis of 3H- and 14C-labeled AR-A000002, a new and selective 5-HT1B/1D ligand

✍ Scribed by Tom Werner; Stefan Berg; Rolf Johansson

Publisher
John Wiley and Sons
Year
2004
Tongue
French
Weight
94 KB
Volume
47
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

AR‐A000002 is a novel and selective high‐affinity 5‐HT~1B/1D~ receptor antagonist. The compound has been shown to enhance 5‐HT turnover in the guinea pig brain in vivo and to increase the extracellular concentration of 5‐HT and the metabolite 5‐hydroxyindoleacetic acid (5‐HIAA) in guinea pig frontal cortex. The observed effects suggest that the compound could be used for the treatment of affective disorders.

The syntheses of labeled AR‐A000002 analogues as needed for the further pharmacological evaluation of this selective 5‐HT~1B/1D~ antagonist, are described. Copyright Β© 2004 John Wiley & Sons, Ltd.

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