Abstract:
:(+)-2-Methyl-4-carboxyphenylglycine (LY367385), a potent and selective antagonist of mGlu1a metabotropic glutamate receptors, was neuroprotective in the following in vitro and in vivo models of excitotoxic death: (i) mixed cultures of murine cortical cells transiently exposed to N-methyl-D-aspartate (NMDA); (ii) rats monolaterally infused with NMDA into the caudate nucleus; and (iii) gerbils subjected to transient global ischemia. We have compared the activity of LY367385 with that of the novel compound (+/-)-alpha-thioxantylmethyl-4-carboxyphenylglycine (LY367366), which antagonizes both mGlu1a and -5 receptors at low micromolar concentrations, but also recruits other subtypes at higher concentrations. Although LY367366 was neuroprotective, it was in general less efficacious than LY357385, suggesting that inhibition of mGlu1 receptors is sufficient to confer significant neuroprotection. We conclude that endogenous activation of mGlu1a receptors (or perhaps other mGlu1 receptor splice variants) contributes to the development of neuronal degeneration of excitotoxic origin.
journal_name
Neuropharmacologyjournal_title
Neuropharmacologyauthors
Bruno V,Battaglia G,Kingston A,O'Neill MJ,Catania MV,Di Grezia R,Nicoletti Fdoi
10.1016/s0028-3908(98)00159-2subject
Has Abstractpub_date
1999-02-01 00:00:00pages
199-207issue
2eissn
0028-3908issn
1873-7064pii
S0028390898001592journal_volume
38pub_type
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