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Glycine transporters as novel therapeutic targets in schizophrenia, alcohol dependence and pain
Journal article   Peer reviewed

Glycine transporters as novel therapeutic targets in schizophrenia, alcohol dependence and pain

Robert J Harvey and B K Yee
Nature Reviews Drug Discovery, Vol.12(11), pp.866-885
2013
url
https://doi.org/10.1038/nrd3893View
Published Version

Abstract

2 chloro n [alpha (2 piperidinyl)benzyl] 3 trifluoromethylbenzamide 6 dichloro 3 (2 oxo 1 phenyl 3 pyrrolidinylidenemethyl) 1h indole 2 carboxylic acid amg 747 amphetamine bitopertin clonazepam clozapine dextro serine dopamine dopamine 2 recept
Glycine transporters are endogenous regulators of the dual functions of glycine, which acts as a classical inhibitory neurotransmitter at glycinergic synapses and as a modulator of neuronal excitation mediated by NMDA (N-methyl-D-aspartate) receptors at glutamatergic synapses. The two major subtypes of glycine transporters, GlyT1 and GlyT2, have been linked to the pathogenesis and/or treatment of central and peripheral nervous system disorders, including schizophrenia and related affective and cognitive disturbances, alcohol dependence, pain, epilepsy, breathing disorders and startle disease (also known as hyperekplexia). This Review examines the rationale for the therapeutic potential of GlyT1 and GlyT2 inhibition, and surveys the latest advances in the biology of glycine reuptake and transport as well as the drug discovery and clinical development of compounds that block glycine transporters. © 2013 Macmillan Publishers Limited. All rights reserved.

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