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

Lennart Bunch; Darryl S Pickering; Thierry Gefflaut; Virginie Vinatier; Virgil Helaine; Ahmad Amir; Birgitte Nielsen; Anders Asbjørn Jensen

doi:10.1002/cmdc.200900258

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

Lennart Bunch, Darryl S Pickering, Thierry Gefflaut, Virginie Vinatier, Virgil Helaine, Ahmad Amir, Birgitte Nielsen, Anders Asbjørn Jensen

5 Citations (Scopus)

Abstract

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.

Original language	English
Journal	ChemMedChem
Volume	4
Issue number	11
Pages (from-to)	1925-1929
ISSN	1860-7179
DOIs	https://doi.org/10.1002/cmdc.200900258
Publication status	Published - 2009

Keywords

Former Faculty of Pharmaceutical Sciences

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Bunch, L., Pickering, D. S., Gefflaut, T., Vinatier, V., Helaine, V., Amir, A., Nielsen, B., & Jensen, A. A. (2009). 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. ChemMedChem, 4(11), 1925-1929. https://doi.org/10.1002/cmdc.200900258

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 et al.

In: ChemMedChem, Vol. 4, No. 11, 2009, p. 1925-1929.

Research output: Contribution to journal › Journal article › Research › peer-review

Bunch, L , Pickering, DS, Gefflaut, T, Vinatier, V, Helaine, V, Amir, A, Nielsen, B & Jensen, AA 2009, '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', ChemMedChem, vol. 4, no. 11, pp. 1925-1929. https://doi.org/10.1002/cmdc.200900258

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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

Abstract

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