The present invention provides compounds that are glycine transporter 1 (hereinafter referred to as GlyT-1) inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of GlyT1 such as cognitive disorders associated with Schizophrenia, ADHD (attention deficit hyperactivity ...
Introduction: Numerous research groups have developed GlyT-1 inhibitors in the pursuit of providing a novel antipsychotic treatment for schizophrenia. Despite multiple compounds advancing into clinical trials, a GlyT-1 inhibitor has yet to emerge to treat patients. However, the approach remains heavily...
4. A compound according to claim 1 wherein R1 is C3-6cycloalkyl. 5. A compound according to claim 1 wherein R2 is phenyl substituted by R2a, R2b and R2c which are independently selected from hydrogen, fluoro, chloro, bromo, OCH3, CF3, OCF3 and NH2. 6. A compound according to cla...
These findings provide preliminary support for further study of the antipsychotic potential of GlyT1 inhibitors. Neuropsychopharmacology (2012) 37, 1036–1046; doi:10.1038/npp.2011.295; published online 23 November 2011 Keywords: ORG 25935; glycine transporter inhibitor; ketamine; healthy subjects; ...
Glycine Transporter-1 Inhibition Promotes Striatal Axon Sprouting via NMDA Receptors in Dopamine Neurons (2013) Glycine transporter-1 inhibition promotes striatal axon sprouting via NMDA receptors in dopamine neurons. J. Neurosci. 33, 16778-16789... Y.,Schmitz,C.,... - 《Journal of Neuroscience...
levels of synaptic glycine are tightly controlled by the specific transporter GlyT1 localized on glial cells and neurons closely associated with the NMDA receptor10. Several well tolerated, high affinity GlyT1 inhibitors have been developed and shown to increase central glycine levels for a positive ...
This chapter discusses the recent developments made in glycine transporter–1 inhibitor. The growing body of evidence implicating N-methyl-D-aspartate (NMDA) glutamate receptor hypofunction as an underlying cause of schizophrenia has led to a paradigm shift in the search for safer and more ef...
The screening campaign identified 300 small molecules as selective GlyT1 inhibitors for lead optimization, demonstrating the utility of this cost-effective method. 展开 关键词: glycine transporter uptake high-throughput screen small-molecule inhibitor IC(50 ...
Glycine transporter inhibitors as a novel drug discovery strategy for neuropathic pain 2009, Pharmacology and Therapeutics Show abstract The antinociceptive effect of intrathecal administration of glycine transporter-2 inhibitor ALX1393 in a rat acute pain model 2010, Anesthesia and Analgesia Show abstract ...
211 EFFECTS OF GLYCINE TRANSPORTER INHIBITORS ON BLADDER OVERACTIVITY IN RATS WITH CYCLOPHOSPHAMIDE-INDUCED CYSTITIS Satoru Yoshikawa*, Tomohiko Oguchi, Naoki Yoshimura, Pittsburgh, PA INTRODUCTION AND OBJECTIVES: Glycine is a major inhib- itory neurotransmitter that modulates various physiological and patho...