glyt2

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.

Yoda 1 is an agonist of the Piezo1 channel that agonizes human- and mouse-derived Piezo1 (EC50=17.1 26.6 μM). Yoda 1 is also an inhibitor of glycine transporter protein 2 (GlyT2).

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.

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).

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

Oleoyl-D-lysine, a lipid-based selective Glycine Transporter-2 (GlyT2) inhibitor, effectively reverses neuropathic pain and exhibits an antidrowsiness effect in mice with chronic neuropathic pain. It is considered safe and efficacious, without causing respiratory depression [1].

(Rac)-Oleoylcarnitine, an endogenous acylcarnitine, acts as a potential non-competitive inhibitor of glycine transporter 2 (GLYT2) and can be used as a pain suppressant.

TCID (UCH-L3 Inhibitor)(IC50=0.6 μM) is a DUB inhibitor of ubiquitin C-terminal hydrolase L3. It has the 125-fold selectivity to L1.

Oleoyl-L-carnitine, a long-chain acylcarnitine, acts as a selective inhibitor of glycine transporter 2 (GlyT2; IC50 = 340 nM) while demonstrating significantly lesser affinity for GlyT1 (IC50 = >10,000 nM). Elevated plasma levels of this compound have been observed in patients suffering from chronic kidney disease or end-stage renal disease undergoing initial hemodialysis, correlating with an increased risk of cardiovascular mortality.

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.

GT-0198 is a novel glycine transporter 2 inhibitor showed activity in a mouse model of neuropathic pain. GT-0198 inhibited the function of glycine transporter 2 (GlyT2) in human GlyT2-expressing HEK293 cells and did not bind various major transporters or receptors of neurotransmitters in a competitive manner. GT-0198 is considered to be a comparatively selective GlyT2 inhibitor. GT-0198 is a structurally novel GlyT2 inhibitor bearing a phenoxymethylbenzamide moiety with in vivo efficacy in behavioral models of neuropathic pain.

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.

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