From revolution to evolution: the glutamate hypothesis of schizophrenia and its implication for treatment

B Moghaddam, D Javitt - Neuropsychopharmacology, 2012 - nature.com
Glutamate is the primary excitatory neurotransmitter in mammalian brain. Disturbances in
glutamate-mediated neurotransmission have been increasingly documented in a range of …

Multi-target-directed ligands in Alzheimer's disease treatment

M Bajda, N Guzior, M Ignasik… - Current medicinal …, 2011 - ingentaconnect.com
Among the various drug discovery methods, a very promising modern approach consists in
designing multi-target-directed ligands (MTDLs). This methodology has been specifically …

[HTML][HTML] In-silico screening based on molecular simulations of 3, 4-disubstituted pyrrolidine sulfonamides as selective and competitive GlyT1 inhibitors

M Er-rajy, WA Eltayb, M Kara, A Assouguem… - Arabian Journal of …, 2023 - Elsevier
A systematic in-silico study based on molecular modeling techniques was conducted on
thirty 3, 4-disubstituted pyrrolidine sulfonamides derivatives to identify the drug candidate for …

Transport mechanism and pharmacology of the human GlyT1

Y Wei, R Li, Y Meng, T Hu, J Zhao, Y Gao, Q Bai, N Li… - Cell, 2024 - cell.com
Summary The glycine transporter 1 (GlyT1) plays a crucial role in the regulation of both
inhibitory and excitatory neurotransmission by removing glycine from the synaptic cleft …

Use of an iridium-catalyzed redox-neutral alcohol-amine coupling on kilogram scale for the synthesis of a GlyT1 inhibitor

MA Berliner, SPA Dubant, T Makowski… - … Process Research & …, 2011 - ACS Publications
A recent development for the efficient and environmentally friendly synthesis of aliphatic
amines is the transition-metal-catalyzed redox-neutral coupling of an alcohol and an amine …

Glycine transport inhibitors in the treatment of schizophrenia

DC Javitt - Novel antischizophrenia treatments, 2012 - Springer
Schizophrenia is a severe neuropsychiatric disorder without adequate current treatment.
Recent theories of schizophrenia focus on disturbances of glutamatergic neurotransmission …

Pharmacology of GPR55 in yeast and identification of GSK494581A as a mixed-activity glycine transporter subtype 1 inhibitor and GPR55 agonist

AJ Brown, DA Daniels, M Kassim, S Brown… - … of Pharmacology and …, 2011 - ASPET
GPR55 is a G protein-coupled receptor activated by l-α-lysophosphatidylinositol and
suggested to have roles in pain signaling, bone morphogenesis, and possibly in vascular …

Synthesis and Biological Evaluation of 3-Biphenyl-4-yl-4-phenyl-4H-1,2,4-triazoles as Novel Glycine Transporter 1 Inhibitors

T Sugane, T Tobe, W Hamaguchi… - Journal of medicinal …, 2011 - ACS Publications
We describe the preparation and evaluation of a novel series of glycine transporter 1 (GlyT1)
inhibitors derived from a high-throughput screening hit. The SAR studies resulted in the …

Recent advances in the discovery of D-amino acid oxidase inhibitors and their therapeutic utility in schizophrenia

DV Ferraris, T Tsukamoto - Current pharmaceutical design, 2011 - ingentaconnect.com
D-Amino acid oxidase (DAAO) catalyzes the oxidative metabolism of D-amino acids
including D-serine, a full agonist at the allosteric glycine binding site of the NMDA receptor …

Glycine transporter-1: a new potential therapeutic target for schizophrenia

K Hashimoto - Current pharmaceutical design, 2011 - ingentaconnect.com
The hypofunction hypothesis of glutamatergic neurotransmission via N-methyl-D-aspartate
(NMDA) receptors in the pathophysiology of schizophrenia suggests that increasing NMDA …