4.5 Article

Discovery of GlyT1 inhibitors with improved pharmacokinetic properties

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 19, Issue 5, Pages 1492-1495

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.01.015

Keywords

GlyT1; Schizophrenia; NMDA pharmacokinetics; Cassette dosing

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Glycine transporter 1 (GlyT1) represents a novel target for the treatment of schizophrenia via the potentiation of glutamatergic NMDA receptors. The discovery of 4,4-disubstituted piperidine inhibitors of GlyT1 which exhibit improved pharmacokinetic properties, including oral bioavailability, is discussed. (C) 2009 Elsevier Ltd. All rights reserved.

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