245063-59-6
Chemical Structure
SPD-502
Synonym(s): NS-1209
- CAS No.: 245063-59-6
- Formula:C24H28N4O7S
- Molecular Weight:516.57
IUPAC Name: (Z)-2-(((5-(4-(N,N-dimethylsulfamoyl)phenyl)-8-methyl-2-oxo-1,2,6,7,8,9-hexahydro-3H-pyrrolo[3,2-h]isoquinolin-3-ylidene)amino)oxy)-4-hydroxybutanoic acid
InChIKey: CFJRSKULEDUDKL-UHFFFAOYSA-N
SMILES: O=C(N1)/C(C2=C1C3=C(C(C4=CC=C(S(N(C)C)(=O)=O)C=C4)=C2)CCN(C)C3)=N\OC(C(O)=O)CCO
Biological Activity: SPD-502 is a novel glutamate antagonist with potential neuroprotective properties, particularly in brain ischemia. It selectively targets the AMPA receptor, showing high affinity (IC50 = 0.043 μM) and competitive inhibition of AMPA-induced effects in rat cortical membranes and cultured mouse cortical neurons. In vivo, SPD-502 effectively blocks AMPA-evoked spike activity in the hippocampus after intravenous administration, significantly increasing the seizure threshold in mice and demonstrating robust protection against ischemia-induced damage to hippocampal neurons in gerbils. These findings suggest SPD-502 may be promising for studying neurodegenerative conditions associated with glutamate excitotoxicity[1].
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SPD-502 | SPD-502 is a novel glutamate antagonist with potential neuroprotective properties, particularly in brain ischemia. It selectively targets the AMPA receptor, showing high affinity (IC50 = 0.043 μM) and competitive inhibition of AMPA-induced effects in rat cortical membranes and cultured mouse cortical neurons. In vivo, SPD-502 effectively blocks AMPA-evoked spike activity in the hippocampus after intravenous administration, significantly increasing the seizure threshold in mice and demonstrating robust protection against ischemia-induced damage to hippocampal neurons in gerbils. These findings suggest SPD-502 may be promising for studying neurodegenerative conditions associated with glutamate excitotoxicity. | |||||||||||||||||||||
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Keywords
