Org 24598 lithium salt

• Catalog No.: O7639
• CAS Number: 722456-08-8
• M. F.: C19H19F3LiNO3
• M. W.: 373.2952696
• Purity: ≥98% (HPLC)

SYNONYMS

• IUPAC name: lithium(1+) ion 2-{methyl[(3R)-3-phenyl-3-[4-(trifluoromethyl)phenoxy]propyl]amino}acetate
• IUPAC Traditional name: lithium(1+) ion 2-{methyl[(3R)-3-phenyl-3-[4-(trifluoromethyl)phenoxy]propyl]amino}acetate
• Synonyms: R-(-)-N-Methyl-N-[3-[(4-trifluoromethyl)phenoxy]-3-phenyl-propyl]glycine lithium salt

DATABASE IDS

• MDL Number: MFCD08705419
• PubChem SID: 24898046
• CAS Number: 722456-08-8

PROPERTIES

• Empirical Formula (Hill Notation): C19H19F3LiNO3
• Purity: ≥98% (HPLC)
• Apperance: white to off-white solid
• Solubility: H2O: >2 mg/mL
• Storage Temperature: 2-8°C
• German water hazard class: 3

DETAILS

Description (English)

Biochem/physiol Actions
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.

Description (简体中文)

Biochem/physiol Actions
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.