Article
Mechanism of partial agonist action at the NR1 subunit of NMDA receptors.
Neuron - 7 Jul 2005
Inanobe Atsushi, Furukawa Hiroyasu, Gouaux Eric
Abstract excerpt
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...
Topics
- Amino Acids, Cyclic
- Animals
- Binding, Competitive
- Crystallography, X-Ray
- Cycloleucine
- Electrophysiology
- Excitatory Amino Acid Agonists
- Female
- Kinetics
- Ligands
- Models, Molecular
- Mutation
- Oocytes
- Patch-Clamp Techniques
- Protein Conformation
- Rats
- Receptors, AMPA
- Receptors, Glycine
