O7639

Org 24598 lithium salt

≥98% (HPLC), solid

• Synonym(s): R-(−)-N-Methyl-N-[3-[(4-trifluoromethyl)phenoxy]-3-phenyl-propyl]glycine lithium salt
• Empirical Formula (Hill Notation): C₁₉H₁₉F₃LiNO₃
• CAS Number: 722456-08-8
• Molecular Weight: 373.30
• MDL number: MFCD08705419
• UNSPSC Code: 12352202
• PubChem Substance ID: 24898046

Properties

• 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

Description

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.

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.

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable