P.0439 Antiparkinsonian activity of new glutamate N-methyl-D-aspartate receptor ligands - imidazole-4, 5-dicarboxylic acid derivatives in the arecoline hyperkinesis test

2021 ◽  
Vol 53 ◽  
pp. S319-S320
Author(s):  
V. Dergachev ◽  
E. Iakovleva ◽  
M. Brusina ◽  
E. Bychkov ◽  
L. Piotrovskij ◽  
...  
Keyword(s):  
Dicarboxylic Acid ◽  
Receptor Ligands ◽  
Aspartate Receptor

Effects of intraseptal infusions of N-methyl-d-aspartate receptor ligands on memory in an object recognition task in rats

1998 ◽  
Vol 244 (2) ◽  
pp. 97-100 ◽  
Author(s):  
Carole Puma ◽  
Claude Baudoin ◽  
Jean-Charles Bizot
Keyword(s):  
Object Recognition ◽  
Recognition Task ◽  
Receptor Ligands ◽  
Object Recognition Task ◽  
Aspartate Receptor

Solubilization of Rat Brain Phencyclidine Receptors in an Active Binding Form That Is Sensitive to N-Methyl-d-Aspartate Receptor Ligands

1988 ◽  
Vol 51 (1) ◽  
pp. 133-140 ◽  
Author(s):  
Ifat Ambar ◽  
Yoel Kloog ◽  
Mordechai Sokolovsky
Keyword(s):  
Rat Brain ◽  
Receptor Ligands ◽  
Aspartate Receptor

scholarly journals Effects of N-methyl-D-aspartate receptor ligands on sensitivity to reinforcer magnitude and delayed reinforcement in a delay-discounting procedure

2016 ◽  
Vol 234 (3) ◽  
pp. 461-473 ◽  
Author(s):  
Justin R Yates ◽  
Benjamin T Gunkel ◽  
Katherine K Rogers ◽  
Mallory N Hughes ◽  
Nicholas A Prior
Keyword(s):  
Delay Discounting ◽  
Delayed Reinforcement ◽  
Receptor Ligands ◽  
Reinforcer Magnitude ◽  
Aspartate Receptor

Effects of N-methyl-D-aspartate receptor ligands on yeast sporulation

1990 ◽  
Vol 4 (10) ◽  
pp. 1765-1769 ◽  
Author(s):  
R. Piñón
Keyword(s):  
Receptor Ligands ◽  
Aspartate Receptor

ChemInform Abstract: Synthesis and Structure-Activity Relationships of Diiodotyrosine- Derived Glycine-Site N-Methyl-D-aspartate Receptor Ligands.

ChemInform ◽  
2010 ◽  
Vol 27 (37) ◽  
pp. no-no
Author(s):  
N. R. CURTIS ◽  
J. J. KULAGOWSKI ◽  
P. D. LEESON ◽  
I. M. MAWER ◽  
M. P. RIDGILL ◽  
...  
Keyword(s):  
Glycine Site ◽  
Receptor Ligands ◽  
Structure Activity Relationships ◽  
Aspartate Receptor ◽  
Structure Activity

Effects of CNQX, APB, PDA, and kynurenate on horizontal cells of the tiger salamander retina

1989 ◽  
Vol 3 (3) ◽  
pp. 207-212 ◽  
Author(s):  
Xiong-Li Yang ◽  
Samuel M. Wu
Keyword(s):  
Dicarboxylic Acid ◽  
Nmda Receptors ◽  
Receptor Antagonist ◽  
Horizontal Cells ◽  
Tiger Salamander ◽  
Light Responses ◽  
Aspartate Receptor ◽  
Synaptic Receptors

AbstractEffects of 6-cyano-7-nitroquinoxaline-2,3-dione (CNQX), 2-amino-4-phosphonobutyrate (APB), cis-2,3-piperidine dicarboxylic acid (PDA), and kynurenate (KYN) on the depolarizing actions of glutamate and kainate on horizontal cells (HCs) were studied in the larval tiger salamander retina. APB, PDA, and KYN hyperpolarized the HCs, but they failed to block either the actions of glutamate and kainate, or the HC light responses. APB and PDA did not cause membrane polarizations in either rods or cones, suggesting that the HC hyperpolarizations were not mediated by presynaptic actions of these compounds. CNQX, the newly synthesized non-NMDA (N-Methyl-D-Aspartate) receptor antagonist, blocked the HC light responses and the action of kainate, but not that of glutamate. These results suggest that the synaptic receptors in the tiger salamander HCs are probably non-NMDA although extra-synaptic NMDA receptors may exist in these cells.

Synthesis and SAR of diiodotyrosine-derived glycine-site N-methyl-D-aspartate receptor ligands

1996 ◽  
Vol 6 (10) ◽  
pp. 1145-1150 ◽  
Author(s):  
Neil R. Curtis ◽  
Janusz J. Kulagowski ◽  
Paul D. Leeson ◽  
Ian M. Mawer ◽  
Mark P. Ridgill ◽  
...  
Keyword(s):  
Glycine Site ◽  
Receptor Ligands ◽  
Aspartate Receptor

scholarly journals Antiparkinsonian activity of new N-methyl-D-aspartate receptor ligands in the arecoline hyperkinesis test

2021 ◽  
pp. 406-412
Author(s):  
V. D. Dergachev ◽  
E. E. Yakovleva ◽  
M. A. Brusina ◽  
E. R. Bychkov ◽  
L. B. Piotrovskiy ◽  
...  
Keyword(s):  
Nmda Receptor ◽  
Dicarboxylic Acid ◽  
Latent Period ◽  
High Efficiency ◽  
Dicarboxylic Acids ◽  
Channel Blockers ◽  
Receptor Ligands ◽  
Urgent Task ◽  
Nmda Receptor Complex ◽  
Preliminary Administration

Introduction. Parkinson’s disease (PD) is one of the most common neurodegenerative diseases in the population of older patients. Even though long-term combination therapy helps to cope with the main manifestations of PD. It inevitably leads to the appearance of  such side effects as drowsiness, hallucinations, dyskinesia, and many others.  [12]. Therefore, the  search for  effective antiparkinsonian drugs devoid of the above-mentioned adverse reactions remains an urgent task of modern neuropharmacology.The explored substances are derivatives of imidazole-4,5-dicarboxylic acid. These compounds belong to a fundamentally new class of N-methyl-D-aspartate ligands (NMDA) that are not channel blockers. Their pharmacological effect is realized due to interaction with the NMDA receptor recognition site, which, along with high efficiency, allows us to assume their higher safety, compared to previously existing channel blockers from the NMDA ligand group.Objective. Studing of  the  antiparkinsonian activity of  new ligands of  the  glutamate NMDA-receptor complex-1,2-substituted imidazole-4,5-dicarboxylic acids on an experimental model of arecoline hyperkinesis.Materials and methods. Imidazole-dicarboxylic acid derivatives (IEM2258, IEM2248, IEM2247, and IEM1574) were injected into the lateral ventricles of the mouse brain 10 minutes before arecoline in a volume of 5 µl at doses of 0.1-0.5 µmol, then the latent period, intensity, and duration of tremor were recorded. Amantadine was used as a comparison drug.Results. Preliminary administration of the studied examined substances led to a significant decrease in the intensity and duration of arecoline tremor. The highest inhibitory activity with respect to the intensity and duration of the experimental tremor was demonstrated with the introduction of the compound IEM-2247 (at a dose of 0.1-0.5 mmol, the duration of the latent period of the tremor was 1.7-2.3 times longer than the control one, respectively, the duration of the tremor decreased by 1.5 - 2.5 times).Conclusions. The  dose-dependent antiparkinsonian activity of  imidazole-dicarboxylic acid derivatives is shown, indicating the prospects for the development of these substances and the further search for effective and safe antiparkinsonian agents among the compounds of this class. 

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