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ZD-9379

From Wikipedia, the free encyclopedia
Antagonist of the NMDA receptor at the glycine site
ZD-9379
Names
IUPAC name
7-Chloro-2-(4-methoxy-2-methylphenyl)-3,5-dihydropyridazino[4,5-b]quinoline-1,4,10-trione
Identifiers
3D model (JSmol)
ChEMBL
ChemSpider
  • InChI=1S/C19H14ClN3O4/c1-9-7-11(27-2)4-6-14(9)23-19(26)15-16(18(25)22-23)21-13-8-10(20)3-5-12(13)17(15)24/h3-8H,1-2H3,(H,21,24)(H,22,25)
    Key: PSTDMIAVUUYOOQ-UHFFFAOYSA-N
  • CC1=C(C=CC(=C1)OC)N2C(=O)C3=C(C(=O)N2)NC4=C(C3=O)C=CC(=C4)Cl
Properties
C19H14ClN3O4
Molar mass383.79 g·mol−1
Except where otherwise noted, data are given for materials in theirstandard state (at 25 °C [77 °F], 100 kPa).
Chemical compound

ZD-9379 is an antagonist of theN-methyl-D-aspartate receptor. It possesses neuroprotective properties and could potentially be used for the treatment of certain strokes.

Mechanism of action

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ZD-9379 works by antagonizing (blocking) theglycine site on theNMDA receptor,[1][2] because bothglycine (co-agonist) and anagonist at the main site are needed to activate the NMDA receptor, blocking the glycine binding site prevents the receptor from activating.

Potential use

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In rats, ZD-9379 has been tested to helpspreading depression andbrain infarction, results have shown that treatment with ZD-9379 reduced the amount of spreading depressions and the volume of infarcts.[3] Another study was also able to produce similar results.[4]

References

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  1. ^"ZD 9379 | CAS 170142-20-8 | ZD9379 | Tocris Bioscience".
  2. ^Danysz, Wojciech; Parsons, Chris G. (March 2002). "Neuroprotective potential of ionotropic glutamate receptor antagonists".Neurotoxicity Research.4 (2):119–126.doi:10.1080/10298420290015872.ISSN 1476-3524.PMID 12829411.
  3. ^Tatlisumak, T.; Takano, K.; Meiler, M. R.; Fisher, M. (2000)."A Glycine Site Antagonist ZD9379 Reduces Number of Spreading Depressions and Infarct Size in Rats with Permanent Middle Cerebral Artery Occlusion".Brain Edema XI. Vol. 76. pp. 331–333.doi:10.1007/978-3-7091-6346-7_68.ISBN 978-3-7091-7257-5.ISSN 0065-1419.PMID 11450037.{{cite book}}:|journal= ignored (help)
  4. ^Qiu, H.; Hedlund, L. W.; Gewalt, S. L.; Benveniste, H.; Bare, T. M.; Johnson, G. A. (1997). "Progression of a focal ischemic lesion in rat brain during treatment with a novel glycine/NMDA antagonist: an in vivo three-dimensional diffusion-weighted MR microscopy study".Journal of Magnetic Resonance Imaging.7 (4):739–744.doi:10.1002/jmri.1880070421.ISSN 1053-1807.PMID 9243396.
AMPARTooltip α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor
KARTooltip Kainate receptor
NMDARTooltip N-Methyl-D-aspartate receptor
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