Kovács G L, Szabó G, Telegdy G, Baláspiri L, Pálos E, Szpornyi L
Institute of Pathophysiology, University Medical School, Szeged, Hungary.
Pharmacol Biochem Behav. 1988 Dec;31(4):833-7. doi: 10.1016/0091-3057(88)90392-9.
The antiamnesic effects of prolyl-leucyl-glycinamide (PLG) and analogues of this tripeptide were investigated in rats. Retrograde amnesia was induced by electroconvulsive shock treatment and the degree of amnesia was characterized by the attenuation of one-trial learning passive avoidance response. PLG resulted in dose-dependent attenuation of retrograde amnesia. Structural modifications included N-terminal protection, substitution of the C-terminal NH2 group, replacement of the N-terminal amino acid, and replacement of the second amino acid of the tripeptide. Some tripeptides, all of them containing D-pipecolic acid instead of the N-terminal proline, were more effective than PLG. Therefore, D-pipecolic acid, D-pipecolamide and their N-terminally protected analogues were also investigated, and were found to have powerful antiamnesic effects.
在大鼠中研究了脯氨酰 - 亮氨酰 - 甘氨酰胺（PLG）及其三肽类似物的抗遗忘作用。通过电惊厥休克治疗诱导逆行性遗忘，遗忘程度以一次性学习被动回避反应的减弱来表征。PLG导致逆行性遗忘呈剂量依赖性减弱。结构修饰包括N端保护、C端NH2基团的取代、N端氨基酸的替换以及三肽第二个氨基酸的替换。一些三肽，所有这些都含有D - 哌啶酸而非N端脯氨酸，比PLG更有效。因此，还研究了D - 哌啶酸、D - 哌啶酰胺及其N端保护类似物，发现它们具有强大的抗遗忘作用。
