Institute of Pharmaceutical Chemistry and Research Group for Stereochemistry, Hungarian Academy of Sciences, University of Szeged, Eotvos u. 6, 6720, Szeged, Hungary.
J Neural Transm (Vienna). 2012 Feb;119(2):109-14. doi: 10.1007/s00702-011-0721-7. Epub 2011 Oct 14.
Pharmacological and histological studies of ten new amides of kynurenic acid revealed that N-(2-N,N-dimethylaminoethyl)-4-oxo-1H-quinoline-2-carboxamide hydrochloride has effective neuroprotective properties. Namely, this molecule is: (1) proved to be an effective inhibitor of excitatory synaptic transmission in the CA1 region of the hippocampus both in in vitro and ex vivo studies, (2) in four vessel occlusion model of transient global forebrain ischaemia, measuring the rate of hippocampal CA1 pyramidal cell loss and preservation of long-term potentiation at Schaffer collateral-CA1 synapses, the neuroprotective potential was represented. N-(2-N,N-dimethylaminoethyl)-4-oxo-1H-quinoline-2-carboxamide hydrochloride administration significantly diminished hippocampal CA1 cell loss and preserved LTP expression.
对 10 种新的色氨酸酸酰胺的药理学和组织学研究表明，N-(2-N,N-二甲基氨基乙基)-4-氧代-1H-喹啉-2-甲酰胺盐酸盐具有有效的神经保护特性。也就是说，这种分子：（1）在体外和离体研究中均被证明是 CA1 区兴奋性突触传递的有效抑制剂；（2）在 4 血管闭塞短暂性全脑缺血模型中，通过测量海马 CA1 锥体神经元丧失率和沙斐尔侧枝-CA1 突触长时程增强的保留率，来表示神经保护潜能。N-(2-N,N-二甲基氨基乙基)-4-氧代-1H-喹啉-2-甲酰胺盐酸盐的给药显著减少了海马 CA1 细胞的丢失并保存了 LTP 的表达。
