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

@article{Inanobe2005MechanismOP,
  title={Mechanism of Partial Agonist Action at the NR1 Subunit of NMDA Receptors},
  author={Atsushi Inanobe and Hiroyasu Furukawa and Eric Gouaux},
  journal={Neuron},
  year={2005},
  volume={47},
  pages={71-84}
}
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 compounds with incrementally larger carbocyclic rings. Whereas ACPC and ACBC partially activate the NMDA… CONTINUE READING
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