Glycine Transporters

Glycine transporters (GlyTs) belong to a family of high affinity Na+- and Cl--dependent neurotransmitter transporters proteins. There are two subtypes of glycine transporters; GlyT1 and GlyT2. GlyT1s are predominantly located on glia within caudal brain areas.

Products
Background
Literature
Gene Data

Inhibitors

Cat No Product Name / Activity
1757 ALX 5407 hydrochloride
Selective non-transportable GlyT1 inhibitor
1445 N-Arachidonylglycine
Endogenous GlyT2 inhibitor; also GPR18 agonist
5308 ASP 2535
Potent and selective GlyT1 inhibitor
3397 LY 2365109 hydrochloride
Potent and selective GlyT1 inhibitor
2789 NFPS
Selective non-transportable GlyT1 inhibitor
4447 Org 24598
Inhibitor of GlyT1; derivative of Org 24598 (Cat. No. 4035).
4035 Org 24598 lithium salt
Selective GlyT1 inhibitor
4782 Org 25543 hydrochloride
Potent and selective GlyT2 inhibitor
2975 Sarcosine
GlyT1 inhibitor

Related Targets

    Glycine transporters (GlyTs) belong to a family of high affinity Na+- and Cl--dependent neurotransmitter transporters proteins. There are two subtypes of glycine transporters; GlyT1 and GlyT2.

    GlyT1s are predominantly located on glia within caudal brain areas, the diencephalon and olfactory bulb. They regulate synaptic glycine concentration, influencing NMDA receptor-mediated neurotransmission and are important in neonatal life for regulating glycine concentrations at inhibitory glycinergic synapses. GlyT2s are predominantly located on neurons within caudal brain areas, the spinal cord, brainstem and cerebellum. They are crucial for efficient transmitter loading of synaptic vesicles and lack-of-function mutations are fatal in the early neonatal period. Both GlyT1 and GlyT2 are unevenly distributed across the cell surface, which is thought to optimize the removal of glycine from the extracellular compartment.

    Transport of glycine involves co-transport of Na+ and Cl- ions. The Na+ concentration gradient is maintained by the plasma membrane Na+,K+-ATPase and allows the accumulation of glycine against its concentration gradient. GlyTs are glycosylated and this is necessary for the protein trafficking to the plasma membrane. Further regulatory mechanisms of GlyTs include the presence of PKC, PKA and CaMK consensus sites, pH and syntaxin1 levels.

    Pharmacologically, glycine transporter inhibitors may have applications in the treatment of muscle tone defects, epilepsy, schizophrenia, pain and neurodegenerative disorders.

    External sources of pharmacological information for Glycine Transporters :

      Literature for Glycine Transporters

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      Glycine Transporter Gene Data

      Gene Species Gene Symbol Gene Accession No. Protein Accession No.
      GlyT1 Human SLC6A9 NM_201649 P48067
      Mouse Slc6a9 NM_008135 P28571
      Rat Slc6a9 NM_053818 P28572
      GlyT2 Human SLC6A5 NM_004211 Q9Y345
      Mouse Slc6a5 NM_148931 Q761V0
      Rat Slc6a5 NM_203334 P58295