GlyT

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.

N-Arachidonylglycine (NA-Gly) is a heat-dependent circulating metabolite with anti-inflammatory, anticancer, antidiabetic and antioxidant activities.

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.

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.

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.

GlyT1 Inhibitor 1 is a selective and potent GlyT1 inhibitor, inhibiting rGlyT1, used in research on neurological disorders.

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.

Sarcosine (Methylglycine) is a competitive inhibitor of the type I glycine transporter (GlyT1) and an N-methyl-D-aspartate receptor (NMDAR) co-agonist.

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.

LY2365109 hydrochloride is a potent and selective GlyT1 inhibitor, with an IC50 of 15.8 nM for glycine uptake in cells over-expressing [hGlyT1a].

SSR504734 is an orally active, selective, and reversible inhibitor of human, rat, and mouse GlyT1 (IC50 = 18, 15, and 38 nM, respectively). SSR504734 exhibits activity in schizophrenia, anxiety, and depression models [1].

Stearoyl-L-carnitine chloride (Acylcarnitine C18:0) is a long-chain acylcarnitine found in the cerebellum that inhibits GlyT2 and is an important component in the study of lipid metabolism.

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.

Tilapertin is an oral glycine transporter type-1 inhibitor.

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).

NFPS exerts neuroprotection via glyR alpha1 subunit in the rat model of transient focal cerebral ischaemia and reperfusion. NFPS is a selective and non-competitive glycine transporter-1 (GlyT1) inhibitor (IC50s: 2.8 nM and 9.8 nM for hGlyT1 and rGlyT1, respectively).

glycine transporter 1 (GlyT1) inhibitor

DCCCyb is an orally bioavailable and selective GlyT1 Inhibitor. DCCCyb demonstrated excellent in vivo occupancy of GlyT1 transporters in rhesus monkeys as determined by the displacement of a PET tracer ligand.

Potent and selective inhibitor of the glial glycine transporter GlyT1b (IC50 = 6.9 nM). Displays negligible activity at GlyT-2, adrenoreceptors, dopamine, 5HT receptors and noradrenaline, dopamine, 5HT and GABA transporters (pIC50 in vivo. Chue et al (2013) Glycine reuptake inhibition as a new therapeutic approach in schizophrenia: focus on the glycine transporter 1 (GlyT1). Curr.Pharm.Des. 19 1311 PMID:23194655 |Brown et al (2001) Discovery and SAR of org 24598-a selective glycine uptake inhibitor. Bioorg.Med.Chem.Lett. 11 2007 PMID:11454468 |Williams et al (2003) Development of a scintillation proximity assay for analysis of Na+/Cl- -dependent neurotransmitter transporter activity. Anal. Biochem. 321 31 PMID:12963052

PF-03463275 is an orally available, CNS-penetrant inhibitor of SLC6A9, a GlyT1 glycine transporter.

SSR504734 is a novel potent glycine transporter 1 (GlyT1) inhibitor.

Bitopertin R enantiomer (RG1678 R enantiomer) is the R-enantiomer of Bitopertin, a noncompetitive glycine reuptake inhibitor that inhibits glycine uptake at human GlyT1 (IC50: 25 nM).

Org-25935, a GlyT-1 inhibitor, is used potentially for the treatment of schizophrenia and alcohol dependence.

VVZ-149 is an antagonist of both serotonin receptor 2A (5HT2A) and glycine transporter type 2 (GlyT2), with potential anti-nociceptive activity.