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The Novel NMDA Receptor Antagonist, 2-hydroxy-5-(2,3,5,6-tetrafluoro-4-trifluoromethyl-benzylamino)-benzoic Acid, Is a Gating Modifier in Cultured Mouse Cortical Neurons

The Novel NMDA Receptor Antagonist, 2-hydroxy-5-(2,3,5,6-tetrafluoro-4-trifluoromethyl-benzylamino)-benzoic Acid, Is a Gating Modifier in Cultured Mouse Cortical Neurons

Jihyun Noh, Eun-sung Lee, Jun-mo Chung

J Neurochem. 2009 Jun;109(5):1261-71.

PMID: 19302475

Abstract:

Neu2000 [NEU, 2-hydroxy-5-(2,3,5,6-tetrafluoro-4-trifluoromethyl-benzylamino)-benzoic acid], a derivative of sulfasalazine, attenuates NMDA-induced neuronal toxicity. Here we investigated the effects of NEU on the NMDA receptor (NMDAR) using whole-cell patch clamp technique to determine the molecular mechanisms underlying its neuroprotective role. NEU reversibly suppressed NMDA responses in an uncompetitive manner with fast binding kinetics. Its inhibition of NMDAR activity depended on both the concentration and the use of agonist but not on the membrane potential. NEU accelerated NMDA desensitization without affecting the binding affinity of NMDAR for its agonists and stabilized the closed state of NMDAR. Therefore, NEU should effectively alleviate disorders that are a result of glutamate excitoxicity with fewer side effects because it is a low-affinity gating modifier that antagonizes NMDAR in an uncompetitive manner. Moreover, in the presence of ifenprodil (an NR2B antagonist) but not NVP-AAM077 [(R)-[(S)-1-(4-bromo-phenyl)-ethylamino]-(2,3-dioxo-1,2,3,4-tetrahydro-quinoxalin-5-yl)-methyl]-phosphonic acid, an NR2A antagonist], the extent of NEU block was decreased, suggesting that NEU is an NR2B-specific antagonist.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP146780098	{[3-(Trifluoromethyl)phenyl]methyl}phosphonic acid		146780-09-8	Price
AP146780167	{[2-(Trifluoromethyl)phenyl]methyl}phosphonic acid		146780-16-7	Price

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