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GlyT

Glycine transporters (GlyTs) are plasmalemmal neurotransmitter transporters. They serve to terminate the signaling of glycine by mediating its reuptake from the synaptic cleft back into the presynaptic neurons. There are two glycine transporters: glycine transporter 1 (GlyT1) and glycine transporter 2 (GlyT2).

  • ALX-1393
    T14198949164-09-4In house
    ALX-1393 is a selective GlyT2 inhibitor that effectively reduces neuronal action potential activity in a concentration-dependent manner and inhibits the activity of spontaneous networks by inducing glycinergic tetanic currents in the abdominal horn of the spinal cord. Antiinjurious effects on thermal, mechanical and chemical stimuli in rat models of acute pain.
    • $1,380
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  • Org 25543 hydrochloride
    T22126495076-64-7
    Org 25543 hydrochloride is a potent and selective glycine transporter type 2 (GlyT2) inhibitor (IC50 = 16 nM for hGlyT2). Displays no activity at GlyT1 or 56 other common biological targets (≥ 100 μM), in a glycine uptake assay in CHO cells.
    • $97
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  • Opiranserin hydrochloride
    T98331440796-75-7
    Opiranserin (VVZ-149) hydrochloride is a dual antagonist of glycine transporter type 2 (GlyT2) and serotonin receptor 2A (5HT2A), with IC50s of 0.86 and 1.3 μM, respectively. It shows antagonistic activity on rP2X3 (IC50=0.87 μM). It is development as an injectable agent for the treatment of postoperative pain.
    • $97
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    TargetMol | Inhibitor Sale
  • Tilapertin
    T170961000690-85-6
    Tilapertin is an oral glycine transporter type-1 inhibitor.
    • $1,520
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  • Opiranserin
    T163991441000-45-8
    Opiranserin is a development as an injectable agent for the treatment of postoperative pain. Opiranserin is a non-opioid and non-NSAID analgesic candidate and is a dual antagonist of glycine transporter type 2 (GlyT2) and serotonin receptor 2A (5HT2A) (IC50s: 0.86 and 1.3 μM, respectively). Opiranserin displays antagonistic activity on rP2X3 (IC50=0.87 μM).
    • $1,520
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  • Bitopertin
    T6788845614-11-1
    Bitopertin (Paliflutine) (RG1678, RO-4917838) is a potent inhibitor of glycine transporter 1 (GlyT1), with Ki of 8.1 nM for human hGlyT1b and IC50 of 22-25 nM in Chinese hamster ovary cells.
    • $35
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  • Bitopertin (R enantiomer)
    T10552845614-12-2
    Bitopertin R enantiomer (RG1678 R enantiomer) is the R-enantiomer of Bitopertin. Bitopertin is a noncompetitive glycine reuptake inhibitor and inhibits glycine uptake at human GlyT1 (IC50: 25 nM).
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  • PF-03463275
    T615641173239-39-8
    PF-03463275 is an orally active and selective reversible inhibitor of competitive glycine transporter protein-1 (GlyT1) with a Ki of 11.6 nM.PF-03463275 has CNS permeability and may be used to ameliorate cognitive deficits associated with schizophrenia.
    • $51
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  • Iclepertin
    T370891421936-85-7
    Iclepertin (BI-425809) is an orally active and selective inhibitor of glycine transporter protein 1 (GlyT1).Iclepertin is used for the treatment of central nervous system disorders such as Alzheimer;s disease. Iclepertin is used for central nervous system disorders such as Alzheimer;s disease, schizophrenia and cognitive disorders.
    • $226
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  • ASP2535
    T14334374886-51-8
    ASP2535 is a potent, selective, orally bioavailable, brain permeable and centrally-active glycine transporter-1 (GlyT1) inhibitor.ASP2535 can improve cognitive impairment in animal models of schizophrenia and Alzheimer's disease[1].
    • $1,520
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  • Amoxapine
    T156814028-44-5
    Amoxapine (CL-67772) exerts its antidepressant effect by inhibiting the re-uptake of norepinephrine and, to a lesser degree, of serotonin, at adrenergic nerve endings and blocks the response of dopamine receptors to dopamine. Amoxapine is a tricyclic antidepressant of the dibenzoxazepine class. This drug is used to treat symptoms of depression and may cause tardive dyskinesia. Amoxapine also binds to alpha-adrenergic, histaminergic, and cholinergic receptors which accounts for many of the side effects seen with this agent.
    • $64
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  • LY2365109 hydrochloride
    T119081779796-27-8
    LY2365109 hydrochloride is a potent and selective GlyT1 inhibitor, with an IC50 of 15.8 nM for glycine uptake in cells over-expressing hGlyT1a.
    • $34
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  • Sarcosine
    T6975107-97-1
    Sarcosine (Methylglycine) is a competitive inhibitor of the type I glycine transporter (GlyT1) and an N-methyl-D-aspartate receptor (NMDAR) co-agonist.
    • $39
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