Synthesis and biological activity of glutamic acid derivatives.
In order to develop new specific glutamate analogues at metabotropic glutamate receptors, Diels-Alder, 1-4 ionic and radical reactions were performed starting from (2S)-4-methyleneglutamic acid. Preliminary pharmacological evaluation by measuring IP accumulation using rat forebrain synaptoneurosomes has shown that (2S)-4-(2-phthalimidoethyl)glutamic acid (3a), (2S)-4-(4-phthalimidobutyl)glutamic acid (3b) and 1-[(S)-2-amino-2-carboxyethyl]-3,4-dimethylcyclohex-3-ene-1-carbox ylic acid (8) presented moderate antagonist activities.
Receveur
J M
JM
Laboratoire des Aminoacides, Peptides et Protéines ESA CNRS 5075, Université Montpellier I & II, France.
Guiramand
J
J
Récasens
M
M
Roumestant
M L
ML
Viallefont
P
P
Martinez
J
J
D000818:Animals; D018691:Excitatory Amino Acid Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology; D018698:Glutamic Acid / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D016548:Prosencephalon / Q000166:cytology / Q000187:drug effects; D051381:Rats; D018094:Receptors, Metabotropic Glutamate / Q000037:antagonists & inhibitors*; D013574:Synaptosomes / Q000187:drug effects
D018691:Excitatory Amino Acid Antagonists; D018094:Receptors, Metabotropic Glutamate; D018698:Glutamic Acid