| Description | RPR104632 is a novel and potent antagonist located at the NMDA glycine site with neuroprotective activity. |
| In vitro | RPR104632以4.9 nM的Ki值拮抗[3H]5,7-二氯羟基喹啉酸与大鼠脑皮层的结合。在N-甲基-D-天冬氨酸(NMDA)存在下，RPR104632以55 nM的IC50抑制[3H]N-[1-(2-噻吩基)cyclohexyl]-3,4-哌啶 ([3H]TCP)的结合。以非竞争方式，RPR104632在890 nM的IC50下抑制新生大鼠小脑切片中NMDA诱导的鸟苷酸环化酶3',5'-单磷酸(cGMP)水平的增加，并且显著降低大鼠海马切片和皮质原代细胞培养中NMDA诱导的神经毒性。虽然MK-801 (1 μM)能完全保护CA1和CA3锥体神经元免受NMDA诱导的毒性损伤，但这些效应不受甘氨酸的阻碍。RPR104632一致地对所有NMDA诱导的毒性产生显著的神经保护作用，在高达10 μM的浓度单独添加时无任何效应。RPR104632的神经保护效力以4 μM的EC50表征。 |
| Target activity | Cerebral cortex:4.9 nM (Ki,rat), Neuroprotection:4 μM (EC50), Neuro:4 μM (EC50), Cerebellar slices:890 nM (rat), [3H]-TCP:55 nM |
| molecular weight | 466.13 |
| Molecular formula | C15H11BrCl2N2O4S |
| CAS | 154106-92-0 |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| References | 1. Boireau A, et al. Neuroprotective effects of RPR 104632, a novel antagonist at the glycine site of the NMDA receptor, in vitro. Eur J Pharmacol. 1996 Apr 11;300(3):237-46. |