4-Alkylidenyl glutamic acids, potent and selective GluR5 agonists

Bioorganic & Medicinal Chemistry Letters
2000.0

Abstract

Twenty-four 4-alkylidene glutamic acids were synthesised and tested as potential subtype selective GluR5 and 6 ligands. It was found that a critical size of alkylidene group gave potent and selective GluR5 receptor agonists. LY339624 had Kis of 0.0326 and >100 microM on GluR5 and 6 receptors, respectively.

Knowledge Graph

Similar Paper

4-Alkylidenyl glutamic acids, potent and selective GluR5 agonists
Bioorganic & Medicinal Chemistry Letters 2000.0
4-Alkyl- and 4-Cinnamylglutamic Acid Analogues Are Potent GluR5 Kainate Receptor Agonists
Journal of Medicinal Chemistry 2000.0
The Glutamate Receptor GluR5 Agonist (S)-2-Amino-3-(3-hydroxy-7,8-dihydro-6H-cyclohepta[d]isoxazol-4-yl)propionic Acid and the 8-Methyl Analogue: Synthesis, Molecular Pharmacology, and Biostructural Characterization†PDB ID: 2WKY.
Journal of Medicinal Chemistry 2009.0
(S)-2-Amino-3-(3-hydroxy-7,8-dihydro-6H-cyclohepta[d]isoxazol-4-yl)propionic Acid, a Potent and Selective Agonist at the GluR5 Subtype of Ionotropic Glutamate Receptors. Synthesis, Modeling, and Molecular Pharmacology
Journal of Medicinal Chemistry 2003.0
New 4-Functionalized Glutamate Analogues Are Selective Agonists at Metabotropic Glutamate Receptor Subtype 2 or Selective Agonists at Metabotropic Glutamate Receptor Group III
Journal of Medicinal Chemistry 2016.0
(2S,1‘S,2‘S,3‘R)-2-(2‘-Carboxy-3‘-methylcyclopropyl) Glycine Is a Potent and Selective Metabotropic Group 2 Receptor Agonist with Anxiolytic Properties
Journal of Medicinal Chemistry 2002.0
Chemo-Enzymatic Synthesis of a Series of 2,4-Syn-Functionalized (S)-Glutamate Analogues: New Insight into the Structure−Activity Relation of Ionotropic Glutamate Receptor Subtypes 5, 6, and 7
Journal of Medicinal Chemistry 2008.0
1H-Cyclopentapyrimidine-2,4(1H,3H)-dione-Related Ionotropic Glutamate Receptors Ligands. Structure−Activity Relationships and Identification of Potent and Selective iGluR5 Modulators
Journal of Medicinal Chemistry 2008.0
Diastereoselective synthesis of (2S,4R)-4-Methylglutamic acid (sym 2081): A high affinity and selective ligand at the kainate subtype of glutamate receptors
Bioorganic & Medicinal Chemistry Letters 1995.0
Common and Selective Molecular Determinants Involved in Metabotopic Glutamate Receptor Agonist Activity
Journal of Medicinal Chemistry 2002.0