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关于此项目
经验公式(希尔记法):
C19H19F3LiNO3
化学文摘社编号:
分子量:
373.30
UNSPSC Code:
12352202
PubChem Substance ID:
MDL number:
Assay:
≥98% (HPLC)
Form:
solid
Quality Segment
assay
≥98% (HPLC)
form
solid
color
white to off-white
solubility
H2O: >2 mg/mL
storage temp.
2-8°C
SMILES string
[Li+].CN(CC[C@@H](Oc1ccc(cc1)C(F)(F)F)c2ccccc2)CC([O-])=O
InChI
1S/C19H20F3NO3.Li/c1-23(13-18(24)25)12-11-17(14-5-3-2-4-6-14)26-16-9-7-15(8-10-16)19(20,21)22;/h2-10,17H,11-13H2,1H3,(H,24,25);/q;+1/p-1/t17-;/m1./s1
InChI key
VMQXVSNARQMSDL-UNTBIKODSA-M
Biochem/physiol Actions
Org 24598 is a selective, potent inhibitor of glial GlyT (GlyT1, glycine transporter type 1).
Org 24598 is a selective, potent inhibitor of glial GlyT (GlyT1, glycine transporter type 1). In rats (P12-P16) and in the presence of kynurenic acid, 6-cyano-7-nitroquinoxaline-2,3-dione (CNQX) and bicuculline, ORG 24598 at a concentration of 10 μM induced a mean inward current of -10/-50 pA at -60 mV and increased significantly the decay time constants of miniature (mIPSCs), spontaneous (sIPSCs) and electrically evoked glycinergic (eIPSCs) inhibitory postsynaptic currents. Replacing extracellular sodium with N-methyl-d-glucamine or superfusing the slice with micromolar concentrations of glycine also increased the decay time constant of glycinergic IPSCs. Glycine (1-5 μM and d-serine (10 μM) increased the amplitude of eEPSCs whereas l-serine had no effect. Org 24598 increased significantly the amplitude of NMDA receptor-mediated eEPSCs without affecting the amplitude of non-NMDA receptor-mediated eEPSCs. This brings conclusion that blocking glial glycine transporter by Org 24598 increased the level of glycine in spinal cord slices, which in turn prolonged the duration of glycinergic synaptic current and potentiated the NMDA-mediated synaptic response.
Features and Benefits
This compound is featured on the Glycine Transporters page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
存储类别
11 - Combustible Solids
怎么回事?
WGK 3
闪点 (F)
Not applicable
闪点 (°C)
Not applicable