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- W2023475085 abstract "The kainic acid (KA) receptors belong to the class of glutamate (Glu) receptors in the brain and constitute a promising target for the treatment of neurological and/or psychiatric diseases such as schizophrenia, major depression, and epilepsy. Five KA subtypes have been identified and named GluK1-5. In this article, we present the discovery of (2S,3R)-3-(3-carboxyphenyl)-pyrrolidine-2-carboxylic acid (1) based on a rational design process. Target compound 1 was synthesized by a stereoselective strategy in 10 steps from commercially available starting materials. Binding affinities of 1 at native ionotropic Glu receptors were determined to be in the micromolar range (AMPA, 51 μM; KA, 22 μM; NMDA 6 μM), with the highest affinity for cloned homomeric KA receptor subtypes GluK1,3 (3.0 and 8.1 μM, respectively). Functional characterization of 1 by two electrode voltage clamp (TEVC) electrophysiology at a nondesensitizing mutant of GluK1 showed full competitive antagonistic behavior with a K(b) of 11.4 μM." @default.
- W2023475085 created "2016-06-24" @default.
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- W2023475085 date "2010-11-12" @default.
- W2023475085 modified "2023-10-01" @default.
- W2023475085 title "Discovery of a New Class of Ionotropic Glutamate Receptor Antagonists by the Rational Design of (2<i>S</i>,3<i>R</i>)-3-(3-Carboxyphenyl)-pyrrolidine-2-carboxylic Acid" @default.
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- W2023475085 doi "https://doi.org/10.1021/cn100093f" @default.
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