(Z)-MDL 105519 - CAS 179105-67-0
Category: Inhibitor
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Molecular Formula:
C18H11Cl2NO4
Molecular Weight:
376.19
COA:
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Targets:
Others
Description:
(Z)-MDL 105519 is the inactive isoform of MDL 105519 which is a high affinity NMDA glutamate receptor antagonist at the glycine site.
Storage:
Store in a cool and dry place (or refer to the Certificate of Analysis).
MSDS:
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Boiling Point:
601.3±55.0 ℃ at 760 Torr
Density:
1.594±0.06 g/cm3
InChIKey:
LPWVUDLZUVBQGP-FLIBITNWSA-N
InChI:
InChI=1S/C18H11Cl2NO4/c19-10-6-13(20)15-12(16(18(24)25)21-14(15)7-10)8-11(17(22)23)9-4-2-1-3-5-9/h1-8,21H,(H,22,23)(H,24,25)/b11-8-
Canonical SMILES:
C1=CC=C(C=C1)C(=CC2=C(NC3=CC(=CC(=C32)Cl)Cl)C(=O)O)C(=O)O
1.Abnormal glutamate receptor expression in the medial temporal lobe in schizophrenia and mood disorders.
Beneyto M;Kristiansen LV;Oni-Orisan A;McCullumsmith RE;Meador-Woodruff JH Neuropsychopharmacology. 2007 Sep;32(9):1888-902. Epub 2007 Feb 14.
Pharmacological and anatomical evidence suggests that abnormal glutamate neurotransmission may be associated with the pathophysiology of schizophrenia and mood disorders. Medial temporal lobe structural alterations have been implicated in schizophrenia and to a lesser extent in mood disorders. To comprehensively examine the ionotropic glutamate receptors in these illnesses, we used in situ hybridization to determine transcript expression of N-methyl-D-aspartate (NMDA), alpha-amino-3-hydroxy-5-methyl-4-isoxazole propionate (AMPA), and kainate receptor subunits in the medial temporal lobe of subjects with schizophrenia, bipolar disorder (BD), or major depression (MDD). We used receptor autoradiography to assess changes in glutamate receptor binding in the same subjects. Our results indicate that there are region- and disorder-specific abnormalities in the expression of ionotropic glutamate receptor subunits in schizophrenia and mood disorders. We did not find any changes in transcript expression in the hippocampus. In the entorhinal cortex, most changes in glutamate receptor expression were associated with BD, with decreased GluR2, GluR3, and GluR6 mRNA expression. In the perirhinal cortex we detected decreased expression of GluR5 in all three diagnoses, of GluR1, GluR3, NR2B in both BD and MDD, and decreased NR1 and NR2A in BD and MDD, respectively.
2.Functional expression of recombinant N-methyl-D-aspartate receptors in the yeast Saccharomyces cerevisiae--localization and pharmacological characterization.
Li Z;Becker J;Noe CR Eur J Biochem. 1998 Mar 15;252(3):391-9.
The yeast Saccharomyces cerevisiae was used for expressing the genes encoding the ionotropic N-methyl-D-aspartate (NMDA) receptor subunits from rats (NR1a, NR2A, NR2C) and mice (NR2B). Four plasmids were constructed by cloning the different NMDA receptor genes in the two multi-copy yeast-Escherichia coli shuttle vectors pMB01 (--> NR1a gene) and pMB02 (--> NR2A-2C genes). The protease-deficient S. cerevisiae strain cI3-ABYS-86 (leu-, ura-) was transformed or co-transformed with the resulting plasmids pMBNR1a (leu+) or pMBNR1a/pMBNR2A-C (ura+) respectively. Western blotting analysis with antibodies raised against amino acid sequences at the C-termini of the respective subunits revealed that the recombinant receptor proteins were differently expressed and only partially glycosylated in the cell membranes of the recombinant yeast strains. The expression and localization of the recombinant NMDA receptor proteins were also proved by immunofluorescence microscopy which indicated a distinct expression of the different NMDA receptor subunits in the plasma membrane of the transformed yeast cells. Pharmacological characterization of crude membrane preparations of the recombinant yeast cells showed saturable binding of the glycine antagonist [3H]MDL105,519 with Kd values of 56.
3.Expression and initial characterization of a soluble glycine binding domain of the N-methyl-D-aspartate receptor NR1 subunit.
Ivanovic A;Reiländer H;Laube B;Kuhse J J Biol Chem. 1998 Aug 7;273(32):19933-7.
Glycine is an essential co-agonist of the excitatory N-methyl-D-aspartate (NMDA) receptor, a subtype of the ionotropic glutamate receptor family. The glycine binding site of this hetero-oligomeric ion channel protein is formed by two distinct extracellular regions, S1 and S2, of the NR1 subunit, whereas the homologous domains of the NR2 subunit mediate glutamate binding. Here, segments S1 and S2 of the NR1 polypeptide were fused via a linker peptide followed by N- and C-terminally tagging with Flag and His6 epitopes, respectively. Infection of High Five insect cells with a recombinant baculovirus containing this glycine binding site construct resulted in efficient secretion of a soluble fusion protein of about 53 kDa. After affinity purification to near-homogeneity, the fusion protein bound the competitive glycine site antagonist [3H]MDL105,519 with high affinity (Kd = 5.22 +/- 0. 13 nM) similar to that determined with rat brain membrane fractions. This high affinity binding could be competed by the glycine site antagonist 7-chlorokynurenic acid as well as the agonists glycine and D-serine but not by L-glutamate. This indicates that the S1 and S2 domains of the NR1 subunit are sufficient for the formation of a glycine binding site that displays pharmacological properties similar to those of the NMDA receptor in vivo.
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CAS 179105-67-0 (Z)-MDL 105519

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