GlyT
GlyTs mediate the uptake of glycine from the extracellular space into the cytosol. They belong to a large family of NaC/ClK-dependent transporter proteins, which includes transporters for monoamines (serotonin, norepinephrine and dopamine) and the inhibitory neurotransmitter g-aminobutyric acid (GABA). These polytopic membrane proteins share a common transmembrane topology with 12 transmembrane domains (TMDs) connected by six extracellular and five intracellular loops. Both GlyTs exist in multiple splice variants: three GlyT2 isoforms (a, b, c) differ in the N-terminal region, whereas three N-terminal (a, b, c) and two C-terminal (d, e) exons have been reported to generate different variants of GlyT1. The transporters GLYTla, GLYTlb and GLYTlc have been isolated from the CNS of both rodents and humans. Two isoforms of the GLYT2 gene product have been reported and have been named GLYT2a and GLYT2b. The uptake of glycine mediated by GlyTs is energetically coupled to the transmembrane sodium gradient maintained by the NaC/KC-ATPase. Pharmacological evidence indicates that GLYT 1 transports glycine in the cerebral cortex, but that in the cerebellum, it shares this function with GLYT2.
References
1.Eulenburg V, et al. Trends Biochem Sci. 2005;30(6):325–333.
2.Tunnicliff G. J Biomed Sci. 2003;10(1):30–36.
References
1.Eulenburg V, et al. Trends Biochem Sci. 2005;30(6):325–333.
2.Tunnicliff G. J Biomed Sci. 2003;10(1):30–36.
Membrane Transporter/Ion Channel
AMPK(58)
ASBT Transporter(6)
BCRP(10)
Beta Amyloid(69)
Carbonic Anhydrase(40)
Chloride Channel(34)
CRAC Channel(0)
CRM1(5)
Exportin-1(5)
FABP(6)
GAT(63)
GLUT(5)
Glutamate Transporter(1)
GlyT(13)
HCN Channel(5)
iGluR(52)
Monoamine Transporter(26)
Monocarboxylate Transporter(12)
MTP(1)
nAChR(5)
NADPH(35)
Na-K-ATPase(2)
NKCC(4)
NMDAR(65)
OCT(4)
Other Targets(13)
P2X Receptor(23)
P-glycoprotein(14)
Proton Pump(38)
Sodium Channel(147)
TRP/TRPV Channel(115)
URAT1(1)
GlyT
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PF-03463275 B
catalog no : M35572
cas no: 1173239-39-8
PF-03463275 is an orally active and selective reversible inhibitor of competitive glycine transporter protein-1 (GlyT1) with a Ki of 11.6 nM. -
Iclepertin
catalog no : M34912
cas no: 1421936-85-7
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. -
ALX-1393
catalog no : M33260
cas no: 949164-09-4
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. -
Org 25543 hydrochloride
catalog no : M27512
cas no: 495076-64-7
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. -
LY2365109 hydrochloride
catalog no : M26285
cas no: 1779796-27-8
LY2365109 hydrochloride is a potent and selective GlyT1 inhibitor, with an IC50 of 15.8 nM for glycine uptake in cells over-expressing hGlyT1a.