生物活性

TCN-201 is a selective GluN2A-containing N-methyl-D-aspartate receptor (NMDAR) antagonist with IC50 of 0.326 μM. TCN-201 displays selectivity for GluN1/GluN2A NMDARs over GluN1/GluN2B containing NMDARs, in assays using two-electrode voltage-clamp (TEVC) recordings of NMDAR currents from Xenopus laevis oocytes expressing either GluN1/GluN2A or GluN1/GluN2B NMDARs. Similar to TCN 213, the degree of inhibition produced by TCN-201 is dependent on the concentration of the GluN1-site co-agonist, glycine (or D-serine), and is independent of the glutamate concentration. In regard to glycine at 3 μM, 10 μM, and 30 μM, the IC50 values of TCN-201 are 0.446 μM, 0.746 μM, and 3.89 μM, respectively, while with D-serine at 3 μM, 10 μM, and 30 μM, the IC50 values of TCN-201 are 0.326 μM, 0.816 μM, and 1.92 μM, respectively. TCN-201 acts in a non-competitive manner but its equilibrium constant at GluN1/GluN2A NMDARs indicates TCN-201 is around 30-times more potent than TCN 213. TCN-201 shows only modest antagonism of NMDAR-mediated currents recorded from young (DIV 9-10) neurones, but gives a strong block in older cultures (DIV 15-18) or in cultures where GluN2A subunits have been over-expressed. TCN-201 antagonism of NMDAR-mediated currents shows a negative correlation with their ifenprodil sensitivity and therefore, in combination with ifenprodil, can be used to monitor, pharmacologically, the expression levels of GluN2A and GluN2B NMDAR subunits in neuronal populations.

化学数据

不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

例如，依据体表面积折算法，将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量，需要将20 mg/kg 乘以小鼠的K_m系数（3），再除以大鼠的K_m系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。

储备液配制

以下数据基于产品分子量，对于特殊产品，请参照COA中的储备液配制条件和说明进行操作。