A novel NMDA receptor positive allosteric modulator that acts via the transmembrane domain

• Published in: Neuropharmacology Vol. 121; pp. 204 - 218
• Main Authors: Wang, Tzu-Ming, Brown, Brandon M., Deng, Lunbin, Sellers, Benjamin D., Lupardus, Patrick J., Wallweber, Heidi J.A., Gustafson, Amy, Wong, Evera, Volgraf, Matthew, Schwarz, Jacob B., Hackos, David H., Hanson, Jesse E.
• Format: Journal Article
• Language: English
• Published: England Elsevier Ltd 15.07.2017
• Subjects: Allosteric Regulation - drug effects; Allosteric Regulation - genetics; Binding Sites - drug effects; Binding Sites - genetics; Calcium - metabolism; Dose-Response Relationship, Drug; Doxycycline - pharmacology; Electric Stimulation; Excitatory Amino Acid Agents - chemistry; Excitatory Amino Acid Agents - pharmacology; Glutamic Acid - pharmacology; Glycine - metabolism; HEK293 Cells; Humans; Membrane Potentials - drug effects; Membrane Potentials - genetics; NMDA receptor; Patch-Clamp Techniques; Positive allosteric modulator; Protein Domains - drug effects; Protein Domains - genetics; Pyrimidinones - chemistry; Pyrimidinones - pharmacology; Receptors, N-Methyl-D-Aspartate - genetics; Receptors, N-Methyl-D-Aspartate - metabolism; Sulfonamides - chemistry; Sulfonamides - pharmacology; Synaptic Transmission - drug effects; Synaptic Transmission - genetics; Synaptic Transmission - physiology; Transfection; Transmembrane domain; Ifenprodil (PubChem CID; GNE-8016 (PubChem CID; iGluR; 118009479; 20938953; 4231127; Transmembrane domain; 22432385; TMD; GNE-3419 (PubChem CID; LBD; ATD; GNE-9278 (PubChem CID; Positive allosteric modulator; NAM; NMDA receptor; 3689; PAM; CIQ (PubChem CID

Ionotropic glutamate receptors (iGluRs) mediate fast excitatory neurotransmission and are key nervous system drug targets. While diverse pharmacological tools have yielded insight into iGluR extracellular domain function, less is known about molecular mechanisms underlying the ion conduction gating...