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CAS No. : 138199-51-6
MCE 国际站:(RS)-(Tetrazol-5-yl)glycine
产品活性:(RS)-(Tetrazol-5-yl)glycine (D,L-(tetrazol-5-yl)glycine) 是一种高效且选择性的 N-甲基-D-天冬氨酸 (NMDA) 受体激动剂。(RS)-(Tetrazol-5-yl)glycine 对 GluN1/GluN2D 和 GluN1/GluN2A 的 EC50 分别为 99 nM,1.7 μM。(RS)-(Tetrazol-5-yl)glycine 诱导小鼠癫痫发作反应和 Fos。
研究领域:Membrane Transporter/Ion Channel | Neuronal Signaling
作用靶点:iGluR
In Vitro: (RS)-(Tetrazol-5-yl)glycine (D,L-(tetrazol-5-yl)glycine) is a agonist of N-methyl-D-aspartate (NMDA) subtype of excitatory amino acid receptor. (RS)-(Tetrazol-5-yl)glycine displaces NMDA receptor binding to rat brain membranes as measured using [3H]CGS19755 (IC50=98 nM) and [3H]glutamate (IC50=36 nM) as ligands.
(RS)-(Tetrazol-5-yl)glycine does not appreciably inhibit the binding of D,L-alpha-[5-methyl-3H] amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA), [3H]kainate, or [3H]glycine (IC50s>30 μM).
In Vivo: (RS)-(Tetrazol-5-yl)glycine can be used in animal modeling to construct epilepsy models.
(RS)-(Tetrazol-5-yl)glycine (D,L-(tetrazol-5-yl)glycine; 1.25, 1.5 mg/kg; IP) induces seizure responses and Fos in the NR1+/+ and NR1-/- mice.
(RS)-(Tetrazol-5-yl)glycine is a highly potent convulsant when given to neonatal rats (ED50=0.071 mg/kg; i.p.) .
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