Non-competitive NMDA antagonists as drugs


in The NMDA Receptor

Second edition

Published in print February 1995 | ISBN: 9780192625021
Published online March 2012 | e-ISBN: 9780191724701 | DOI:
Non-competitive NMDA antagonists as drugs

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The ‘excitotoxic theory’ suggests that ischaemia-induced neuronal degeneration is caused, at least in part, by excessive release of glutamate and a subsequent overactivation of post-synaptic receptors. The N-methyl-d-aspartate (NMDA) receptor plays a key role in mediating this toxicity, probably due to its high permeability to calcium, a known mediator of cell damage. Much of the evidence supporting a role for NMDA receptors has come from studies with selective antagonists. Initially, these were performed with competitive antagonists of the glutamate recognition site, such as d-2-amino-5-phosphonopentanoate (d-AP5) and d-2-amino-5-phosphonoheptanoate (d-AP7), which were shown to be neuroprotective in animal studies. More recently, however, much work has concentrated on antagonists acting in a non-competitive manner with glutamate at the NMDA receptor complex.

Keywords: NMDA receptors; toxicity; cell damage; selective antagonists; competitive antagonists; glutamate recognition site

Chapter.  7363 words.  Illustrated.

Subjects: Neuroscience

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