ORG 24598 LITHIUM SALT 化学特性,用途語,生産方法
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Org 24598 Lithium Salt is a selective glycine transporter-1 (GlyT-1) inhibitor.
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.
ORG 24598 LITHIUM SALT 上流と下流の製品情報
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