4,4-Dimethyl- and diastereomeric 4-hydroxy-4-methyl-(2S)-glutamate analogues display distinct pharmacological profiles at ionotropic glutamate receptors and excitatory amino acid transporters
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4,4-Dimethyl- and diastereomeric 4-hydroxy-4-methyl-(2S)-glutamate analogues display distinct pharmacological profiles at ionotropic glutamate receptors and excitatory amino acid transporters. / Bunch, Lennart; Pickering, Darryl S; Gefflaut, Thierry; Vinatier, Virginie; Helaine, Virgil; Amir, Ahmad; Nielsen, Birgitte; Jensen, Anders Asbjørn.
I: ChemMedChem, Bind 4, Nr. 11, 2009, s. 1925-1929.Publikation: Bidrag til tidsskrift › Tidsskriftartikel › Forskning › fagfællebedømt
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T1 - 4,4-Dimethyl- and diastereomeric 4-hydroxy-4-methyl-(2S)-glutamate analogues display distinct pharmacological profiles at ionotropic glutamate receptors and excitatory amino acid transporters
AU - Bunch, Lennart
AU - Pickering, Darryl S
AU - Gefflaut, Thierry
AU - Vinatier, Virginie
AU - Helaine, Virgil
AU - Amir, Ahmad
AU - Nielsen, Birgitte
AU - Jensen, Anders Asbjørn
PY - 2009
Y1 - 2009
N2 - Subtype-selective ligands are of great interest to the scientific community, as they provide a tool for investigating the function of one receptor or transporter subtype when functioning in its native environment. Several 4-substituted (S)-glutamate (Glu) analogues were synthesized, and altogether this approach has provided important insight into the structure-activity relationships (SAR) for ionotropic and metabotropic glutamate receptors (iGluRs and mGluRs), as well as the excitatory amino acid transporters (EAATs). In this work, three 4,4-disubstituted Glu analogues 1-3, which are hybrid structures of important 4-substituted Glu analogues 4-8, were investigated at iGluRs and EAATs. Collectively, their pharmacological profiles add new and valuable information to the SAR for the iGluRs and EAAT1-3.
AB - Subtype-selective ligands are of great interest to the scientific community, as they provide a tool for investigating the function of one receptor or transporter subtype when functioning in its native environment. Several 4-substituted (S)-glutamate (Glu) analogues were synthesized, and altogether this approach has provided important insight into the structure-activity relationships (SAR) for ionotropic and metabotropic glutamate receptors (iGluRs and mGluRs), as well as the excitatory amino acid transporters (EAATs). In this work, three 4,4-disubstituted Glu analogues 1-3, which are hybrid structures of important 4-substituted Glu analogues 4-8, were investigated at iGluRs and EAATs. Collectively, their pharmacological profiles add new and valuable information to the SAR for the iGluRs and EAAT1-3.
KW - Former Faculty of Pharmaceutical Sciences
U2 - 10.1002/cmdc.200900258
DO - 10.1002/cmdc.200900258
M3 - Journal article
C2 - 19731281
VL - 4
SP - 1925
EP - 1929
JO - Farmaco
JF - Farmaco
SN - 1860-7179
IS - 11
ER -
ID: 17007204