glyt

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

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

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.

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.

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

RPI-GLYT2-82 is a reversible GlyT2 allosteric inhibitor capable of crossing the blood-brain barrier, with an IC50 value of 554 nM. It also inhibits 5-HT2AR and SERT, with IC50 values of 1.9 μM and 4.7 μM, respectively. RPI-GLYT2-82 can suppress pain signals and alleviate allodynia without target-related side effects or addiction at its maximum analgesic dose. This compound is suitable for research into neuropathic 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.

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].

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.

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

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

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).

MPDC acts as a competitive inhibitor against the Na+-dependent high-affinity glutamate transporter within forebrain synaptosomes.

ASP2535 is a potent, selective, orally bioavailable, brain-permeable, and centrally-active glycine transporter-1 (GlyT1) inhibitor that can improve cognitive impairment in animal models of schizophrenia and Alzheimer's disease[1].

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.

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).

Tilapertin is an oral glycine transporter type-1 inhibitor.

Stearoylcarnitine (Stearoyl-L-carnitine) is a fatty ester lipid molecule, a human endogenous metabolite that serves as a biomarker for early-onset preeclampsia and late-onset preeclampsia.

ALX-5407 ((R)-NFPS) is a selective and orally active GlyT1 inhibitor with an IC50 of 3 nM. It is utilized in research focused on the function of N-methyl-D-aspartate receptors and its relation to schizophrenia.

glycine transporter 1 (GlyT1) inhibitor

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

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.

GSK494581A is a GPR55 agonist and glycine transporter subtype 1 inhibitor.

GSK931145 is a positron emission tomography (PET) radioligand, it is suitable for quantifying glycine transporter (GlyT1) availability in the living brain.