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Article

Structural Evaluation and Electrophysiological Effects of Some Kynurenic Acid Analogs

1
Department of Neurology, Interdisciplinary Excellence Centre, Albert Szent-Györgyi Clinical Center, Faculty of Medicine, University of Szeged, Semmelweis u. 6, H-6725 Szeged, Hungary
2
Department of Physiology, Anatomy and Neuroscience, University of Szeged, Közép fasor 52, H-6726 Szeged, Hungary
3
Institute of Pharmaceutical Chemistry, University of Szeged, Eötvös u. 6, H-6720 Szeged, Hungary
4
Stereochemistry Research Group of the Hungarian Academy of Sciences, Eötvös utca 6, H-6720 Szeged, Hungary
5
Institute of Pharmaceutical Chemistry, Interdisciplinary Excellence Centre, University of Szeged, Eötvös u. 6, H-6720 Szeged, Hungary
6
MTA-SZTE Neuroscience Research Group, Semmelweis u. 6, H-6725 Szeged, Hungary
*
Author to whom correspondence should be addressed.
These authors contributed equally to this work.
Academic Editor: Tomasz Tuzimski
Received: 12 September 2019 / Revised: 23 September 2019 / Accepted: 24 September 2019 / Published: 26 September 2019
Kynurenic acid (KYNA), a metabolite of tryptophan, as an excitatory amino acid receptor antagonist is an effective neuroprotective agent in case of excitotoxicity, which is the hallmark of brain ischemia and several neurodegenerative processes. Therefore, kynurenine pathway, KYNA itself, and its derivatives came into the focus of research. During the past fifteen years, our research group has developed several neuroactive KYNA derivatives, some of which proved to be neuroprotective in preclinical studies. In this study, the synthesis of these KYNA derivatives and their evaluation with divergent molecular characteristics are presented together with their most typical effects on the monosynaptic transmission in CA1 region of the hippocampus of the rat. Their effects on the basic neuronal activity (on the field excitatory postsynaptic potentials: fEPSP) were studied in in vitro hippocampal slices in 1 and 200 μM concentrations. KYNA and its derivative 4 in both 1 and 200 μM concentrations proved to be inhibitory, while derivative 8 only in 200 μM decreased the amplitudes of fEPSPs. Derivative 5 facilitated the fEPSPs in 200 μM concentration. This is the first comparative study which evaluates the structural and functional differences of formerly and newly developed KYNA analogs. Considerations on possible relations between molecular structures and their physiological effects are presented. View Full-Text
Keywords: kynurenic acid; Mannich reaction; neuroprotection; excitatory amino acid receptors kynurenic acid; Mannich reaction; neuroprotection; excitatory amino acid receptors
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MDPI and ACS Style

Fehér, E.; Szatmári, I.; Dudás, T.; Zalatnai, A.; Farkas, T.; Lőrinczi, B.; Fülöp, F.; Vécsei, L.; Toldi, J. Structural Evaluation and Electrophysiological Effects of Some Kynurenic Acid Analogs. Molecules 2019, 24, 3502. https://0-doi-org.brum.beds.ac.uk/10.3390/molecules24193502

AMA Style

Fehér E, Szatmári I, Dudás T, Zalatnai A, Farkas T, Lőrinczi B, Fülöp F, Vécsei L, Toldi J. Structural Evaluation and Electrophysiological Effects of Some Kynurenic Acid Analogs. Molecules. 2019; 24(19):3502. https://0-doi-org.brum.beds.ac.uk/10.3390/molecules24193502

Chicago/Turabian Style

Fehér, Evelin, István Szatmári, Tamás Dudás, Anna Zalatnai, Tamás Farkas, Bálint Lőrinczi, Ferenc Fülöp, László Vécsei, and József Toldi. 2019. "Structural Evaluation and Electrophysiological Effects of Some Kynurenic Acid Analogs" Molecules 24, no. 19: 3502. https://0-doi-org.brum.beds.ac.uk/10.3390/molecules24193502

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