Glutamic binding

The NRl family is composed of one subunit with nine different alternatively spliced variants. Block by NMDA channel blockers such as ketamine, MK-801 and phencyclidine is affected by which splice variant of the NRl subunit is involved, probably because the NRl splice variant affects the kinetics of channel activation (the effectiveness of any channel blocker being dependent on how much the channel is open). The glycine binding site is on the NRl subunit and the glutamate binding site is on the NR2 and NR3 subunits. 

Glutamate receptors belong to one of two main categories Ionotropic receptors are cation channels whose opening is enhanced when glutamate binds to the receptor. Metabotropic receptors do not conduct ion fluxes instead they activate intracellular enzymes through... 

What is the molecular underpinning for the coincidence-detector property of the NMDA receptor The NMDA receptor is a channel protein that sits in the postsynaptic membrane (Fig. 53-3). The electrical stimulation of a presynaptic cell releases glutamate which binds to the postsynaptic AMPA and NMDA receptors. Glutamate binding to the NMDA receptor alone is not sufficient to activate... 

Malherbe, P., Knoflach, F Broger, C., et al. (2001) Identification of essential residues involved in the glutamate binding pocket of the group II metabotropic glutamate receptor. Mol. Pharmacol. 60,944-954. 

However, the reactivity in vitro towards biological systems is not always in agreement with this role, because [ H]glutamate binding was more sensitive to diphenyl ditelluride than diphenyl diselenide, and other bindings were similarly affected by both compounds. ... 

S1 - glutamate binding site (e.g. glutamate 337) SZ - glutamate binding site (e.g. serine 664)... 

FIGURE 2.3 Glutamatergic synapse. Glutamate binds to ionotropic receptors (1) and metabotropic receptors (2). The glutamate transporter (3) pumps glutamate back into the glutamatergic neuron. 

Monaghan, D. T., McMills, M. C., Chamberlin, A. R., Cotman, C. W. Synthesis of [3H]2-amino-4-phosphonobutyric acid and characterization of its binding to rat brain membranes a selective ligand for the chloride/calcium-dependent class of L-glutamate binding sites, Brain Res. 1983, 278, 137-144. 

Laube, B., Hirai, H., Sturgess, M., Betz, H., Kuhse, J. Molecular determinants of agonist discrimination by NMDA receptor subunits Analysis of the glutamate binding site on the NR2B subunit. Neuron 1997, 18, 493-503. 

Managhan D. T., Holets V. R., Toy D. W., and Cotman C. W. (1983). Anatomical distribution of four pharmacologically distinct 3H-L-glutamate binding sites. Nature 306 176-179. 

NR2 is the glutamate binding subunit. This subunit also contains the polyaminebinding site. It is generated as the product of four distinct genes (Yamakura and Shimoji, 1999). The NR2 subunit is responsible for most of the structural... 

Kerwin R., Patel S., and Meldrum B. (1990). Quantitative autoradiographic analysis of glutamate binding sites in the hippocampal formation in normal and schizophrenic brain post mortem. Neuroscience 39 25-32. 

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