Name | RPR104632 |
Synonyms | RPR104632 RPR 104632 154106-92-0 2H-1,2,4-Benzothiadiazine-3-carboxylic acid, 2-[(3-bromophenyl)methyl]-6,8-dichloro-3,4-dihydro-, 1,1-dioxide |
CAS | 154106-92-0 |
Molecular Formula | C15H11BrCl2N2O4S |
Molar Mass | 466.13384 |
Density | 1.788±0.06 g/cm3(Predicted) |
Boling Point | 658.6±65.0 °C(Predicted) |
pKa | 2.00±0.20(Predicted) |
Storage Condition | 2-8℃ |
Use | RPR104632 is a specific NMDA receptor antagonist with neuroprotective effects. |
In vitro study | RPR104632 antagonizes the binding of [ 3 H]5,7-dichlorokynurenic acid to the rat cerebral cortex, with a K i of 4.9 nM. RPR104632 inhibits [ 3 H]N-[1-(2-thienyl)cyclohexyl]-3,4-piperidine ([ 3 H]TCP) binding in the presence of N-methyl-D-aspartate (NMDA) (IC 50 = 55 nM). RPR104632 inhibits the NMDA-evoked increase in guanosine 3',5'-cyclic monophosphate (cGMP) levels of neonatal rat cerebellar slices (IC 50 = 890 nM) in a non-competitive manner and markedly reduces NMDA-induced neurotoxicity in rat hippocampal slices and in cortical primary cell cultures. MK-801 (1 μM) completely protects the CA1 and CA3 pyramidal neurones against NMDA-induced toxicity, but these effects are not blocked by glycine. RPR104632 produces a significant and consistent neuroprotective effect towards all the NMDA-induced toxicity and has no effect when it is added alone at concentrations up to 10 μM. RPR104632 has neuroprotective potencies, with EC 50 of 4 μM. |