22753-30-6Relevant academic research and scientific papers
Studies on Aryl-Substituted Phenylalanines: Synthesis, Activity, and Different Binding Modes at AMPA Receptors
Szymanska, Ewa,Frydenvang, Karla,Pickering, Darryl S.,Krintel, Christian,Nielsen, Birgitte,Kooshki, Ayesheh,Zachariassen, Linda G.,Olsen, Lars,Kastrup, Jette S.,Johansen, Tommy N.
, p. 448 - 461 (2016)
A series of racemic aryl-substituted phenylalanines was synthesized and evaluated in vitro at recombinant rat GluA1-3, at GluK1-3, and at native AMPA receptors. The individual enantiomers of two target compounds, (RS)-2-amino-3-(3,4-dichloro-5-(5-hydroxyp
3-Substituted phenylalanines as selective AMPA- and kainate receptor ligands
Szymanska, Ewa,Pickering, Darryl S.,Nielsen, Birgitte,Johansen, Tommy N.
experimental part, p. 6390 - 6401 (2011/03/17)
On the basis of X-ray structures of ionotropic glutamate receptor constructs in complex with amino acid-based AMPA and kainate receptor antagonists, a series of rigid as well as flexible biaromatic alanine derivatives carrying selected hydrogen bond acceptors and donors have been synthesized in order to investigate the structural determinants for receptor selectivity between AMPA and the GluR5 subtype of kainate receptors. Compounds selective for either GluR5 or AMPA receptors were identified. One particular substituent position appeared to be of special importance for control of ligand selectivity. Using molecular modeling the observed structure-activity relationships at AMPA and GluR5 receptors were deduced.
