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Literature DB >> 22860161

ACS chemical neuroscience molecule spotlight on RG1678.

Abstract

RG1678 is a glycine transporter-1 inhibitor currently in Phase III trials for the treatment of the negative symptoms of schizophrenia and is being developed by Roche (in combination with Chugai). Recent Phase II data shows that RG1678 is effective in reducing the negative symptoms when given in combination with second generation antipsychotics.

Entities: Disease

Keywords: GlyT1; RG1678; Schizophrenia; glycine transporter-1 inhibitor; negative symptoms

Mesh：

Substances：

Year: 2011 PMID： 22860161 PMCID： PMC3369722 DOI： 10.1021/cn200108z

Source DB: PubMed Journal: ACS Chem Neurosci ISSN： 1948-7193 Impact factor: 4.418

4 in total

Review 1. Glycine and N-methyl-D-aspartate receptors: physiological significance and possible therapeutic applications.

Authors: W Danysz; C G Parsons
Journal: Pharmacol Rev Date: 1998-12 Impact factor: 25.468

2. The economic burden of schizophrenia in the United States in 2002.

Authors: Eric Q Wu; Howard G Birnbaum; Lizheng Shi; Daniel E Ball; Ronald C Kessler; Matthew Moulis; Jyoti Aggarwal
Journal: J Clin Psychiatry Date: 2005-09 Impact factor: 4.384

3. 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]methanone (RG1678), a promising novel medicine to treat schizophrenia.

Authors: Emmanuel Pinard; Alexander Alanine; Daniela Alberati; Markus Bender; Edilio Borroni; Patrick Bourdeaux; Virginie Brom; Serge Burner; Holger Fischer; Dominik Hainzl; Remy Halm; Nicole Hauser; Synese Jolidon; Judith Lengyel; Hans-Peter Marty; Thierry Meyer; Jean-Luc Moreau; Roland Mory; Robert Narquizian; Mathias Nettekoven; Roger D Norcross; Bernd Puellmann; Philipp Schmid; Sebastien Schmitt; Henri Stalder; Roger Wermuth; Joseph G Wettstein; Daniel Zimmerli
Journal: J Med Chem Date: 2010-06-24 Impact factor: 7.446

4. Glycine transport inhibitors for the treatment of schizophrenia.

Authors: Kenji Hashimoto
Journal: Open Med Chem J Date: 2010-05-27

4 in total

6 in total

ACS chemical neuroscience molecule spotlight on RG1678.

Review 1. Glycine and N-methyl-D-aspartate receptors: physiological significance and possible therapeutic applications.

2. The economic burden of schizophrenia in the United States in 2002.

3. 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]methanone (RG1678), a promising novel medicine to treat schizophrenia.

4. Glycine transport inhibitors for the treatment of schizophrenia.

1. Chiral proton catalysis of secondary nitroalkane additions to azomethine: synthesis of a potent GlyT1 inhibitor.

2. Effects of D-amino acid oxidase inhibition on memory performance and long-term potentiation in vivo.

Review 3. Emerging approaches for treatment of schizophrenia: modulation of glutamatergic signaling.

4. Glycine transporter 1 is a target for the treatment of epilepsy.

Review 5. Schizophrenia: synthetic strategies and recent advances in drug design.

6. Two grams of sarcosine in schizophrenia - is it too much? A potential role of glutamate-serotonin interaction.