The protection of pyroglutamic acid and derivs. (I, R = CH2C≡CH, CH2CH:CH2, CH2Ph, CH2C6H4Cl-p, CH2C6H4CN-p, as Me) (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 amino acids. The potency of pyroglutamic acid and some derivs. (Id,f,g,h) against glutamate-induced convulsions was similar to that shown by di-Et glutamate and by valproic acid. Interestingly, pyroglutamic acid did not affect NMDA-induced convulsions which were well antagonized by both 2-amino-5-phosphonoaleric acid and by diazepam. Thus, pyroglutamic acid may represent the starting material for synthesis of excitatory amino acid antagonists acting at non NMDA receptors.
Protection by pyroglutamic acid and some of its newly synthesized derivatives against glutamate-induced seizures in mice
BEANI, LorenzoPrimo
;BIANCHI, ClementinaSecondo
;BARALDI, Pier Giovanni
;MANFREDINI, StefanoPenultimo
;POLLINI, Gian PieroUltimo
1990
Abstract
The protection of pyroglutamic acid and derivs. (I, R = CH2C≡CH, CH2CH:CH2, CH2Ph, CH2C6H4Cl-p, CH2C6H4CN-p, as Me) (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 amino acids. The potency of pyroglutamic acid and some derivs. (Id,f,g,h) against glutamate-induced convulsions was similar to that shown by di-Et glutamate and by valproic acid. Interestingly, pyroglutamic acid did not affect NMDA-induced convulsions which were well antagonized by both 2-amino-5-phosphonoaleric acid and by diazepam. Thus, pyroglutamic acid may represent the starting material for synthesis of excitatory amino acid antagonists acting at non NMDA receptors.File | Dimensione | Formato | |
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Arzemittel-Forschung 1990, 40(11),1187-1191.pdf
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