Chemical Name:(2S*,3R*)-1-(Phenanthren-2-carbonyl)piperazine-2,3-dica
rboxylic acid
Biological Activity:
Subtype-selective
NMDA receptor antagonist that preferentially binds to NR2C/NR2D-containing
receptors (Ki values are 0.096, 0.125, 0.31 and 0.55 μM for NR2C, NR2D, NR2B and NR2A
subunits respectively).
Fenget al (2004)
Structure-activity analysis of a novel NR2C/NR2D-preferring NMDA receptor
antagonist: 1-(phenanthrene-2-carbonyl)piperazine-2,3-dicarboxylic acid.
Br.J.Pharmacol. 141 508. Morleyet al (2005)
Synthesis and pharmacology of N1-substituted
piperazine-2,3-dicarboxylic acid derivatives acting as NMDA receptor
antagonists. J.Med.Chem. 48 2627. Kinarskyet al
(2005) Identification of subunit- and antagonist-specific amino acid residues
in the N-methyl-D-aspartate receptor glutamate-binding
pocket. J.Pharmacol.Exp.Ther. 313 1066.