Protection by pyroglutamic acid and some of its newly synthesized derivatives against glutamate-induced seizures in mice.
The protection by pyroglutamic acid (CAS 98-79-3) and derivatives Ia-i (injected i.p.) against glutamate- and NMDA (N-methyl-D-aspartate) (i.c.v.) induced seizures in mice has been studied in comparison with known antiepileptics and antagonists of excitatory aminoacids. The potency of pyroglutamic acid and some derivatives (Id,f,g,h) against glutamate-induced convulsions was similar to that shown by glutamic acid diethylester and by valproic acid. Interestingly, pyroglutamic acid did not affect NMDA-induced convulsions which were well antagonized by both 2-amino-5-phosphono valeric acid and by diazepam. Thus, pyroglutamic acid may represent the starting for synthesis of excitatory aminoacid antagonists acting at non NMDA receptors.
Beani
L
L
Dipartimento di Farmacologia, Università di Ferrara, Italy.
Bianchi
C
C
Baraldi
P G
PG
Manfredini
S
S
Pollini
G P
GP
D000818:Animals; D000927:Anticonvulsants; D001522:Behavior, Animal / Q000187:drug effects; D005971:Glutamates; D018698:Glutamic Acid; D007202:Indicators and Reagents; D007274:Injections, Intraperitoneal; D007276:Injections, Intraventricular; D008297:Male; D051379:Mice; D009043:Motor Activity / Q000187:drug effects; D016202:N-Methylaspartate; D011761:Pyrrolidonecarboxylic Acid / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology*; D012640:Seizures / Q000139:chemically induced / Q000517:prevention & control*
D000927:Anticonvulsants; D005971:Glutamates; D007202:Indicators and Reagents; D018698:Glutamic Acid; D016202:N-Methylaspartate; D011761:Pyrrolidonecarboxylic Acid