A novel glycine transporter-1 (GlyT1) inhibitor, ASP2535 (4-[3-isopropyl-5-(6-phenyl-3-pyridyl)-4H-1, 2, 4-triazol-4-yl]-2, 1, 3-benzoxadiazole), improves cognition in …
K Harada, K Nakato, J Yarimizu, M Yamazaki… - European journal of …, 2012 - Elsevier
Hypofunction of brain N-methyl-d-aspartate (NMDA) receptors has been implicated in
psychiatric disorders such as schizophrenia and Alzheimer's disease. Inhibition of glycine …
psychiatric disorders such as schizophrenia and Alzheimer's disease. Inhibition of glycine …
Differential effects of the tricyclic antidepressant amoxapine on glycine uptake mediated by the recombinant GLYT1 and GLYT2 glycine transporters
E Núñez, B López‐Corcuera, J Vázquez… - British journal of …, 2000 - Wiley Online Library
We examined the effects of nine different tricyclic antidepressant drugs on the glycine uptake
mediated by the glycine transporter 1b (GLYT1b) and glycine transporter 2a (GLYT2a) stably …
mediated by the glycine transporter 1b (GLYT1b) and glycine transporter 2a (GLYT2a) stably …
Characterization of SSR103800, a selective inhibitor of the glycine transporter-1 in models predictive of therapeutic activity in schizophrenia
D Boulay, P Pichat, G Dargazanli… - Pharmacology …, 2008 - Elsevier
On native human, rat and mouse glycine transporter-1 (GlyT1), SSR130800 behaves as a
selective inhibitor with IC50 values of 1.9, 5.3 and 6.8 nM, respectively. It reversibly blocked …
selective inhibitor with IC50 values of 1.9, 5.3 and 6.8 nM, respectively. It reversibly blocked …
Glycine modulators in schizophrenia.
DC Javitt - Current Opinion in Investigational Drugs (London …, 2002 - europepmc.org
N-methyl-D-aspartate (NMDA) receptor dysfunction may play a key role in the
pathophysiology of schizophrenia. Recent studies have investigated the ability of …
pathophysiology of schizophrenia. Recent studies have investigated the ability of …
The glycine transporter-1 inhibitors NFPS and Org 24461: a pharmacological study
LG Harsing Jr, I Gacsalyi, G Szabo, E Schmidt… - Pharmacology …, 2003 - Elsevier
The in vitro and in vivo pharmacology of two glycine transporter-1 (GlyT1) inhibitors, N [3-
(4′-fluorophenyl)-3-(4′-phenylphenoxy)-propyl] sarcosine (NFPS) and R, S-(+/−) N-methyl …
(4′-fluorophenyl)-3-(4′-phenylphenoxy)-propyl] sarcosine (NFPS) and R, S-(+/−) N-methyl …
Selective GlyT1 Inhibitors: Discovery of [4-(3-Fluoro-5-trifluoromethylpyridin-2-yl)piperazin-1-yl][5-methanesulfonyl-2-((S)-2,2,2-trifluoro-1-methylethoxy)phenyl] …
E Pinard, A Alanine, D Alberati, M Bender… - Journal of medicinal …, 2010 - ACS Publications
The GlyT1 transporter has emerged as a key novel target for the treatment of schizophrenia.
Herein, we report on the optimization of the 2-alkoxy-5-methylsulfonebenzoylpiperazine …
Herein, we report on the optimization of the 2-alkoxy-5-methylsulfonebenzoylpiperazine …
SLC6A20 transporter: a novel regulator of brain glycine homeostasis and NMDAR function
M Bae, JD Roh, Y Kim, SS Kim, HM Han… - EMBO Molecular …, 2021 - embopress.org
Abstract Glycine transporters (GlyT1 and GlyT2) that regulate levels of brain glycine, an
inhibitory neurotransmitter with co‐agonist activity for NMDA receptors (NMDARs), have …
inhibitory neurotransmitter with co‐agonist activity for NMDA receptors (NMDARs), have …
Procognitive and antipsychotic efficacy of glycine transport 1 inhibitors (GlyT1) in acute and neurodevelopmental models of schizophrenia: latent inhibition studies in …
Rationale SSR103800 and SSR504734 are novel glycine transport 1 (GlyT1) inhibitors with
therapeutic potential for the treatment of schizophrenia. Objective The present studies …
therapeutic potential for the treatment of schizophrenia. Objective The present studies …
Glycine transport inhibitors and the treatment of schizophrenia
DC Javitt - Biological psychiatry, 2008 - biologicalpsychiatryjournal.com
The potential role of N-methyl-D-aspartate (NMDA)-type glutamate receptors in the
pathogenesis of schizophrenia was first proposed almost 20 years ago on the basis of …
pathogenesis of schizophrenia was first proposed almost 20 years ago on the basis of …
Dose-related target occupancy and effects on circuitry, behavior, and neuroplasticity of the glycine transporter-1 inhibitor PF-03463275 in healthy and schizophrenia …
DC D'Souza, RE Carson, N Driesen, J Johannesen… - Biological …, 2018 - Elsevier
Abstract Background Glycine transporter-1 (GlyT1) inhibitors may ameliorate cognitive
impairments associated with schizophrenia. The dose-related occupancy and target …
impairments associated with schizophrenia. The dose-related occupancy and target …