O7639

Org 24598 lithium salt

≥98% (HPLC), solid

• Synonyme(s) : R-(−)-N-Methyl-N-[3-[(4-trifluoromethyl)phenoxy]-3-phenyl-propyl]glycine lithium salt
• Formule empirique (notation de Hill): C₁₉H₁₉F₃LiNO₃
• Numéro CAS: 722456-08-8
• Poids moléculaire : 373.30
• Numéro MDL: MFCD08705419
• Code UNSPSC : 12352202
• ID de substance PubChem : 24898046

Propriétés

• Pureté: ≥98% (HPLC)
• Forme: solid
• Couleur: white to off-white
• Solubilité: H₂O: >2 mg/mL
• Température de stockage: 2-8°C
• Chaîne SMILES: [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
• Clé InChI: VMQXVSNARQMSDL-UNTBIKODSA-M

Description

Actions biochimiques/physiologiques

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.

Caractéristiques et avantages

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.

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable