684283-16-7Relevant academic research and scientific papers
Piperazine-2,3-dicarboxylic acid derivatives as dual antagonists of NMDA and GluK1-containing kainate receptors
Irvine, Mark W.,Costa, Blaise M.,Dlaboga, Daniel,Culley, Georgia R.,Hulse, Richard,Scholefield, Caroline L.,Atlason, Palmi,Fang, Guangyu,Eaves, Richard,Morley, Richard,Mayo-Martin, Maria B.,Amici, Mascia,Bortolotto, Zuner A.,Donaldson, Lucy,Collingridge, Graham L.,Molnár, Elek,Monaghan, Daniel T.,Jane, David E.
experimental part, p. 327 - 341 (2012/03/11)
Competitive N-methyl-d-aspartate receptor (NMDAR) antagonists bind to the GluN2 subunit, of which there are four types (GluN2A-D). We report that some N1-substituted derivatives of cis-piperazine-2,3-dicarboxylic acid display improved relative
Synthesis and pharmacology of N1-substituted piperazine-2,3-dicarboxylic acid derivatives acting as NMDA receptor antagonists
Morley, Richard M.,Tse, Heong-Wai,Feng, Bihua,Miller, Jacqueline C.,Monaghan, Daniel T.,Jane, David E.
, p. 2627 - 2637 (2007/10/03)
The binding site for competitive NMDA receptor antagonists is on the NR2 subunit, of which there are four types (NR2A-D). Typical antagonists such as (R)-AP5 have a subunit selectivity of NR2A > NR2B > NR2C > NR2D. The competitive NMDA receptor antagonist
Phenanthryl piperazinyl dicarboxylic acids as selective nmda receptor modulating agents
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, (2008/06/13)
Disclosed are compounds of formula (I) wherein: L is (a) optionally substituted by replacement of one or more of the hydrogen atoms on the phenanthrene ring system by one or more groups other than hydrogen; A is CH2, SO2 or C=O; X is CO2H, PO3H2, PO2H2, PO2HR5, PO2HOR5, SO3H, SO2H, or tetrazole; and R1, R2, R3, R4 and R5 are independently selected from H, alkyl, alkenyl, alkynyl, aryl and aralkyl; or a pharmaceutically acceptable acid salt or base addition salt or an in vivo hydrolysable ester or amide thereof. Compounds of formula (I) are selective NMDA receptor modulating agents and, therefore, may be used to advantage in vitro in neuroassays and in vivo in the treatment of disorders of the CNS.
