化合物 Nelonemdaz T16286

Product Introduction
Bioactivity


英文名: Nelonemdaz

描述: Neu2000 is an uncompetitive antagonist of N-methyl-D-aspartate (NMDA) receptor.

体外活性: Neu2000 displays apparent neuroprotection against 300 μM N-methyl-D-aspartate (NMDA) at doses as low as 30 μM. Neu2000 inhibits the electrophysiologic response of cultured cortical neurons to 300 μM NMDA in a concentration-dependent manner, indicating that the effect is mediated by a specific action at NMDA receptors. Neu2000 does not protect cortical neurons against α-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid- or kainate-mediates excitotoxicity. Neu2000 (100 μM) obviously decreases the maximal NMDA response by 58.31±2.72% (n=5) and the EC50 values of NMDA from 18.88±1.85 to 9.92±0.17 μM (n=5, P<0.05). The Neu2000 dose-response has an IC50 of 35.38±5.94 μM and Hill's coefficient of 0.91 (n=8) [1].

体内活性: Pharmacokinetic analysis reveals that the half-life of Neu2000 is 1.42, 2.14, and 1.79?h following intraperitoneal administration of 10, 25, and 50?mg/kg, respectively. The results of the blood-brain barrier (BBB) test also reveals significant changes in open field locomotion in spinal cord-injured animals treated with Neu2000 compare to vehicle-treated animals. Single (p<0.05) or repeated (p<0.01) Neu2000 treatment causes a decreased swing to stance ratio to compare to vehicle-treated animals. Repeated treatment with Neu2000 induces a 45.6% decrease (p<0.01) in overall lesion volume compared to vehicle treatment, while a single administration of Neu2000 results in a 36.8% decrease (p<0.05) in overall lesion volume. Compare to sham controls, the levels of basal mitochondrial ROS are obviously elevated at 24?h post-surgery in both the vehicle-treated (4.1-fold, p<0.01) and Neu2000-treated (2.9-fold, p<0.01) groups. The Cmax (maximum plasma concentration) is calculated as 3.86, 18.73, and 52.83?μg/mL and the AUC (area under the curve) is determined to be 7.37, 55.15, and 96.77?μg/h/mL at the same respective doses [2].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 112.5 mg/mL (293.57 mM)


关键字: Nelonemdaz

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