A new class of agonists and antagonists of N-methyl-D-aspartic acid receptors: Derivatives of imidazole-4,5- and pyrazole-3,4-dicarboxylic acids
| Autor: | L. B. Piotrovskii, I. Ya. Aleksandrova, A. P. Maksimyuk, O. A. Kryshtal, P. V. Lishko |
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| Rok vydání: | 2000 |
| Předmět: |
Male
Agonist Patch-Clamp Techniques medicine.drug_class Stereochemistry N-Methyl-D-aspartic acid In Vitro Techniques Pyrazole Hippocampus Receptors N-Methyl-D-Aspartate Membrane Potentials Structure-Activity Relationship chemistry.chemical_compound medicine Animals Imidazole Dicarboxylic Acids Rats Wistar Receptor Pyramidal Cells General Neuroscience Imidazoles Rats nervous system Biochemistry chemistry Lipophilicity Pyrazoles NMDA receptor Antagonism |
| Zdroj: | Neuroscience and Behavioral Physiology. 30:553-558 |
| ISSN: | 1573-899X 0097-0549 |
| DOI: | 10.1007/bf02462614 |
| Popis: | Studies of imidazole-4,5- and pyrazole-3,4-dicarboxylic acid derivatives revealed a number of new agonists and antagonists of N-methyl-D-aspartic acid (NMDA) receptors. Studies were based on whole-cell patch-clamp methods applied to rat hippocampus pyramidal cells. Increases in the lipophilicity of the environment of the nitrogen atom, keeping the distance between the terminal acid functions constant, led to a weakening of NMDA antagonism and increases in NMDA antagonism. Increases in the lipophilicity around the nitrogen atom could also lead to less of selectivity in the interaction with NMDA receptors and the appearance of non-NMDA antagonist properties. |
| Databáze: | OpenAIRE |
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