Diastereoselective synthesis of (2S,4R)-4-methylglutamic acid (SYM 2081): A high affinity and selective ligand at the kainate subtype of glutamate receptors

doi:10.1016/0960-894X(95)00335-Q

Paper

Diastereoselective synthesis of (2S,4R)-4-methylglutamic acid (SYM 2081): A high affinity and selective ligand at the kainate subtype of glutamate receptors

Published Sep 7, 1995 · Z. Gu, Xiao Lin, D. Hesson

Bioorganic & Medicinal Chemistry Letters

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Abstract

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Study Snapshot

Diastereoselective synthesis of (2S,4R)-4-methylglutamic acid (SYM 2081), a high affinity and selective ligand for the kainate receptor subtype, provides a 47% isolated yield.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

Diastereoselective synthesis of (2S,4R)-4-methylglutamic acid (SYM 2081): A high affinity and selective ligand at the kainate subtype of glutamate receptors

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References

Current Excitement about the Glutamate Receptor Family

The glutamate receptor family offers potential for therapeutic intervention by linking specific neuronal functions to specific receptors, potentially promoting neuronal plasticity or causing neurotoxic effects.

Enzymic synthesis of 4-methyl- and 4-ethyl-L-glutamic acids

GOT from pig heart and bacteria effectively synthesizes 4-methyl- and 4-ethyl-L-glutamic acids, enabling the synthesis of both diastereoisomers of 4-substituted L-glutamic acids.

Specific binding of [3H]kainic acid to receptor sites in rat brain.

[3H]kainic acid binding to receptor sites in rat brain is saturable, with high and low affinity sites representing independent entities, and differences in regional distribution.

The excitatory amino acid receptors: their classes, pharmacology, and distinct properties in the function of the central nervous system.

The excitatory amino acid receptors (EAA) play a crucial role in the central nervous system, with their distinct classes and properties influencing their function.

Citations

SYM-2081 a kainate receptor antagonist reduces allodynia and hyperalgesia in a freeze injury model of neuropathic pain

SYM-2081, a kainate receptor antagonist, reduces mechanical allodynia and thermal hyperalgesia in a cold injury model of neuropathic pain.

The kainate receptor antagonist 2S,4R-4-methylglutamate attenuates mechanical allodynia and thermal hyperalgesia in a rat model of nerve injury

The kainate receptor antagonist 2S,4R-4-methylglutamate effectively reduces mechanical allodynia and thermal hyperalgesia in rats with peripheral nerve injury, suggesting its potential as a treatment for neuropathic pain.

Excitatory amino acids.

Recent synthetic developments of excitatory amino acid analogues have significantly improved our understanding of memory and CNS-mediated processes.