title: A derivative of a rigid glutamate analog protects the retina from excitotoxicity.
abstract: In the retina, the activation of metabotropic glutamate receptors (mGluRs) reduces the toxic effect of N-methyl-D-aspartate (NMDA). We have induced NMDA-mediated excitotoxicity in the adult rat retina by a single intraocular injection of NMDA. The damage that resulted was estimated by assessing the NMDA-induced loss of retinal choline acetyltransferase (ChAT) activity. The new rigid glutamate analog, dimethyl ester of (+/-)-trans-azetidine-2,4-dicarboxylic acid (t-DMADA), with a putative mGluR-agonistic activity, protected the retina from NMDA-induced loss of ChAT activity. This study demonstrated that t-DMADA can be considered a prototype of new retino-protective agents.
authors.affiliation: Fldia Research Laboratories, Abano Terme, Italy.
authors.forename: R
authors.initials: R
authors.lastname: Siliprandi
authors.forename: M
authors.initials: M
authors.lastname: Lipartiti
authors.forename: E
authors.initials: E
authors.lastname: Fadda
authors.forename: R
authors.initials: R
authors.lastname: Arban
authors.forename: A P
authors.initials: AP
authors.lastname: Kozikowski
authors.forename: H
authors.initials: H
authors.lastname: Manev
mesh_terms: D000818:Animals; D001383:Azetidinecarboxylic Acid / Q000008:administration & dosage / Q000009:adverse effects / Q000031:analogs & derivatives* / Q000627:therapeutic use; D002795:Choline O-Acetyltransferase / Q000378:metabolism; D005123:Eye; D005971:Glutamates / Q000494:pharmacology*; D007267:Injections; D008297:Male; D051381:Rats; D017207:Rats, Sprague-Dawley; D018094:Receptors, Metabotropic Glutamate / Q000819:agonists* / Q000187:drug effects; D012164:Retinal Diseases / Q000201:enzymology / Q000473:pathology / Q000517:prevention & control*
chemical_list: D005971:Glutamates; D018094:Receptors, Metabotropic Glutamate; C083095:azetidine-2,4-dicarboxylic acid; D001383:Azetidinecarboxylic Acid; D002795:Choline O-Acetyltransferase