Members of the Na+/Cl-dependent transporter family called glycine transporters (GlyTs) have activities and subcellular distributions that are controlled by phosphorylation and interactions with other proteins. GlyTs are made up of glycine transporters of type 1 (SLC6A9; GlyT1) and type 2 (SLC6A5; Glyt2). There are numerous splice variants of both GlyTs. It has been thought that glyTs that control brain glycine levels—an inhibitory neurotransmitter with co-agonist activity for NMDA receptors (NMDARs)—are crucial targets for the treatment of mental illnesses with suppressed NMDAR function, like schizophrenia.
Both astrocytes and neurons express GlyT1 and GlyT2, but in brain tissue, their pattern of expression is primarily connected to neurotransmission. In the brainstem, spinal cord, and cerebellum, GlyT2 is highly expressed and is in charge of glycine uptake into glycinergic and GABAergic terminals. Neocortex, thalamus, and hippocampal regions are all rich in GlyT1, which is expressed in astrocytes and is involved in glutamatergic neurotransmission. GlyT1 and GlyT2, which are found in glial cells and neurons, respectively, play crucial roles in glycinergic neurotransmission regulation by either clearing synaptically released glycine or supplying glycine to glycinergic neurons. Inhibiting GlyTs could therefore be used to alter how pain signals are transmitted to the spinal cord.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V77270 | ALX-1393 TFA | ALX-1393 TFA is a selective GlyT2 inhibitor (antagonist) with antinociceptive effects on thermal, mechanical and chemical stimuli in a rat model of acute pain. | |
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V70302 | ALX-5407 hydrochloride ((R)-NFPS hydrochloride) | 200006-08-2 | ALX-5407 ((R)-NFPS) HCl is a selective, orally bioactive inhibitor of the glycine transporter GlyT1 with IC50 of 3 nM. |
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V7169 | Bitopertin (RG-1678; RO-4917838) | 845614-11-1 | Bitopertin (Paliflutine; RG1678; RO4917838; RG-1678; RO-4917838)is a novel, potent and non-competitive glycine reuptake inhibitor that inhibits human GlyT1 with an IC50 of 25 nM. |
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V24677 | LY2365109 | 1779796-27-8 | LY2365109 (LY-2365109) is a novel and potent glycine transporter 1 (GlyT1) inhibitor (IC50 = 15.8 nM) with the potential to be used as anantiictogenic drug. |
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V2873 | LY2365109 hydrochloride | 1779796-27-8 | LY2365109 is a novel, potent and selective inhibitor of GlyT1 (glycine transporter 1) with IC50 value of 15.8 nM. |
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V70301 | PF-03463275 | 1173239-39-8 | PF-03463275 is a CNS-permeable (penetrable), orally bioactive, selective, competitive and reversible inhibitor of glycine transporter-1 (GlyT1) with a Ki of 11.6 nM. |
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