Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 20, Issue 11, Pages 3405-3408Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.04.008
Keywords
Schizophrenia; Antipsychotic; Neurokinin receptor; Dual ligand
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During a program directed at selective NK1 receptor antagonists, we serendipitously discovered an NK1 receptor ligand with additional affinity for the NK3 receptor. Recognising an opportunity for a drug discovery program aiming for dual NK1/NK3 receptor antagonists, we prepared a series of analogues from a novel, versatile building block. From this series emerged compounds with high and balanced affinities for the NK1 and the NK3 receptors. Typical representatives of this series were active in the gerbil foot tapping assay after oral administration. (C) 2010 Elsevier Ltd. All rights reserved.
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