Mechanism of Partial Agonist Action at the NR1 Subunit of NMDA Receptors

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Mechanism of Partial Agonist Action at the NR1 Subunit of NMDA Receptors

Partial agonists produce submaximal activation of ligand-gated ion channels. To address the question of partial agonist action at the NR1 subunit of the NMDA receptor, we performed crystallographic and electrophysiological studies with 1-aminocyclopropane-1-carboxylic acid (ACPC), 1-aminocyclobutane-1-carboxylic acid (ACBC), and 1-aminocyclopentane-1-carboxylic acid (cycloleucine), three compou...

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Activation of recombinant NR1/NR2C NMDA receptors.

The N-methyl-d-aspartate (NMDA) subtype of ionotropic glutamate receptors comprises both NR1 and NR2 subunits, and plays numerous roles in both physiological and pathophysiological processes in the central nervous system (CNS). NR2C-containing NMDA receptors are most abundant in cerebellum, thalamus and olfactory bulb, and are also expressed in oligodendrocytes and hippocampal interneurons. We ...

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Inactivation of NMDA Receptors by Direct Interaction of Calmodulin with the NR1 Subunit

NMDA (N-methyl-D-aspartate) receptors are excitatory neurotransmitter receptors in the brain critical for synaptic plasticity and neuronal development. These receptors are Ca2+-permeable glutamate-gated ion channels whose physiological properties are regulated by intracellular Ca2+. We report here the purification of a 20 kDa protein identified as calmodulin that interacts with the NR1 subunit ...

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Control of voltage-independent zinc inhibition of NMDA receptors by the NR1 subunit.

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ژورنال

عنوان ژورنال: Neuron

سال: 2005

ISSN: 0896-6273

DOI: 10.1016/j.neuron.2005.05.022