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Synthesis of 3 H‐ and 14 C‐labeled AR‐A000002, a new and selective 5‐HT 1B/1D ligand
Author(s) -
Werner Tom,
Berg Stefan,
Johansson Rolf
Publication year - 2004
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.810
Subject(s) - chemistry , antagonist , metabolite , in vivo , guinea pig , ligand (biochemistry) , extracellular , cortex (anatomy) , pharmacology , receptor , receptor antagonist , stereochemistry , biochemistry , neuroscience , medicine , psychology , microbiology and biotechnology , biology
AR‐A2 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‐A2 analogues as needed for the further pharmacological evaluation of this selective 5‐HT 1B/1D antagonist, are described. Copyright © 2004 John Wiley & Sons, Ltd.