The Preclinical Properties of a Novel Group II Metabotropic Glutamate Receptor Agonist LY379268

ABSTRACT Activation of group II metabotropic glutamate (mGlu2/3) receptors reduces excessive glutamate release that is often associated with neurodegenerative and psychiatric disorders. This finding encouraged the search for potent and selective agonists as potential therapeutic agents. The search l...

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Bibliographic Details
Published in:CNS drug reviews 2007, Vol.13 (4), p.444-464
Main Author: Imre, Gabor
Format: Article
Language:English
Subjects:
Amino Acids - pharmacology
Amino Acids - therapeutic use
Analgesics
Animals
Antipsychotics
Anxiety - drug therapy
Anxiolytics
Brain Chemistry - drug effects
Brain Diseases - drug therapy
Bridged Bicyclo Compounds, Heterocyclic - pharmacology
Bridged Bicyclo Compounds, Heterocyclic - therapeutic use
Drug abuse
Drug Evaluation, Preclinical
Excitatory Amino Acid Agonists - pharmacology
Excitatory Amino Acid Agonists - therapeutic use
Glutamate
Humans
LY379268
mGlu 2/3 receptors
Neuroprotection
Receptors, Metabotropic Glutamate - antagonists & inhibitors
Receptors, Metabotropic Glutamate - physiology
Reviews
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Summary:ABSTRACT Activation of group II metabotropic glutamate (mGlu2/3) receptors reduces excessive glutamate release that is often associated with neurodegenerative and psychiatric disorders. This finding encouraged the search for potent and selective agonists as potential therapeutic agents. The search led to the discovery of LY379268 {(‐)‐2‐oxa‐4‐aminobicyclo[3.1.0]hexane‐4,6‐dicarboxylic acid}, which is a highly potent and systemically available mGlu2/3 receptor agonist. LY379268 was effective in several animal models of stroke, epilepsy, drug abuse, schizophrenia, and pain. Suppression of motor activity is the major side effect of LY379268. Upon repeated administration tolerance develops to this side effect, while the therapeutic effects of LY379268 remain. To date, no clinical data with LY379268 are available. This review article summarizes the preclinical pharmacology of LY379268.
ISSN:1080-563X
1527-3458
DOI:10.1111/j.1527-3458.2007.00024.x