Gavestinel (sodium salt)

NMDA受体拮抗剂；选择性结合NMDA受体的甘氨酸位点，而非NMDA、AMPA或GluK受体的谷氨酸结合位点（Kis分别为0.003、10、7.94和3.98µM）；选择性结合70种受体中的NMDA受体（所有受体的IC50=>10µM）；以3mg/kg的剂量减少MCAO诱发的局灶性缺血大鼠模型中的梗塞体积。An NMDA receptor antagonist; selectively binds to the glycine site of the NMDA receptor over the glutamate binding site of NMDA, AMPA, or GluK receptors (Kis = 0.003, 10, 7.94, and 3.98 µM, respectively); selective for the NMDA receptor over a panel of 70 receptors (IC50s = >10 µM for all); reduces infarct volume in a rat model of MCAO-induced focal ischemia at 3 mg/kg.分子式C18H11Cl2N2O3 • Na分子量397.2O=C(NC1=CC=CC=C1)/C=C/C2=C(C([O-])=O)NC3=CC(Cl)=CC(Cl)=C23.[Na+]