非竞争性N-甲基-D-天冬氨酸（NMDA）拮抗剂FR115427和MK801可提高原代培养神经元的存活率。
Non-competitive NMDA antagonists, FR115427 and MK801, enhance neuronal survival in primary culture.
作者信息
Ueda Y, Katsuta K, Nakanishi H, Yoshida K
机构信息
New Drug Research Laboratories, Fujisawa Pharmaceutical Co., Ltd., Osaka, Japan.
出版信息
Neurosci Lett. 1995 Feb 9;185(2):107-10. doi: 10.1016/0304-3940(94)11236-c.
Primary culture of cerebral cortical neurons from mouse embryo was treated with non-competitive N-methyl-D-aspartate (NMDA) receptor antagonists, FR115427 and MK801. Both FR115427 and MK801 at 1-10 microM promoted neuronal survival after 7 days cultivation, determined by calorimetric assay for acid phosphatase (AP) activity. FR115426, the (-) isomer of FR115427 also promoted neuronal survival. However, competitive NMDA antagonists, APH and CGS19755 did not show promotive effect on neuronal survival at up to 100 microM. Anti-NMDA activity of these compounds was evaluated using an NMDA-induced convulsion assay. The relative potency of anti-NMDA activity was CGS19755 > MK801 > APH > FR115427 > FR115426. These data suggest that the effects on neuronal survival by FR115427 and MK801 are independent of anti-NMDA activity.
用非竞争性N-甲基-D-天冬氨酸（NMDA）受体拮抗剂FR115427和MK801处理小鼠胚胎大脑皮质神经元的原代培养物。通过酸性磷酸酶（AP）活性的比色测定法确定，在培养7天后，1-10 microM的FR115427和MK801均可促进神经元存活。FR115427的（-）异构体FR115426也可促进神经元存活。然而，竞争性NMDA拮抗剂APH和CGS19755在高达100 microM时对神经元存活未显示促进作用。使用NMDA诱导的惊厥试验评估这些化合物的抗NMDA活性。抗NMDA活性的相对效力为CGS19755>MK801>APH>FR115427>FR115426。这些数据表明，FR115427和MK801对神经元存活的影响与抗NMDA活性无关。
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