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Glycine reuptake inhibitor

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A glycine reuptake inhibitor (GRI) is a type of drug which inhibits the reuptake of the neurotransmitter glycine by blocking one or more of the glycine transporters (GlyTs). Examples of GRIs include bitopertin (RG1678), iclepertin (BI-425809), ORG-24598, ORG-25935, ALX-5407, and sarcosine, which are selective GlyT1 blockers, and ORG-25435 and N-arachidonylglycine, which are selective GlyT2 blockers. Some weak and/or non-selective GlyT blockers include amoxapine and ethanol (alcohol).

See also

References

  1. Harsing LG, Juranyi Z, Gacsalyi I, Tapolcsanyi P, Czompa A, Matyus P (2006). "Glycine transporter type-1 and its inhibitors". Curr. Med. Chem. 13 (9): 1017–44. doi:10.2174/092986706776360932. PMID 16611082.
  2. Harvey RJ, Yee BK (November 2013). "Glycine transporters as novel therapeutic targets in schizophrenia, alcohol dependence and pain". Nat Rev Drug Discov. 12 (11): 866–85. doi:10.1038/nrd3893. PMID 24172334. S2CID 28022131.
  3. Harald Sitte, Michael Freissmuth (2 August 2006). Neurotransmitter Transporters. Springer Science & Business Media. pp. 472–. ISBN 978-3-540-29784-0.


Glycine receptor modulators
Receptor
(ligands)
GlyRTooltip Glycine receptor
NMDARTooltip N-Methyl-D-aspartate receptor
Transporter
(blockers)
GlyT1Tooltip Glycine transporter 1
GlyT2Tooltip Glycine transporter 2
See also
Receptor/signaling modulators
GABA receptor modulators
GABAA receptor positive modulators
Ionotropic glutamate receptor modulators


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