Glutamate receptor competitive AMPA

Pyridinyl)-3//-l,2,3-triazolo[4,5-d]pyrimidin-7(6H)-one 313 has been shown to be a potent competitive antagonist of the AMPA subtype glutamate receptor. It may be useful as a neuroprotectant (95JMC587). 

Figure 10.4 Structures of some antagonists at the various receptors for glutamate. CNQX is an AMPA antagonist but NQQX has greater selectivity. AP-5 is an NMDA receptor antagonist while MK-801 blocks the NMDA receptor channel (non-competitive)...

A post-mortem study on the brains of alcohoUcs showed a modest increased binding for [3H]glutamate and [3H]CGP-39653—a competitive NMDA receptor antagonist (Freund and Anderson 1996). In humans with a history of alcohol abuse, an increase in immunoreactivity toward AMPA GluR2 and GluR3 subunits was also found (Breese et al. 1995). In rodents lacking functional... 

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