2840581-38-4

Name	1H-Naphtho[1,2-b][1,4]diazepine-2,4(3H,5H)-dione, 5-[3-(2,5-dihydro-5-thioxo-1,2,4-oxadiazol-3-yl)phenyl]-9-methyl-, sodium salt, ion(1-) (1:1)
CAS	2840581-38-4
Molecular Formula	C22H15N4O3S.Na
Molecular Weight	438.44
MOL File	2840581-38-4.mol

Synonyms

1H-Naphtho[1,2-b][1,4]diazepine-2,4(3H,5H)-dione, 5-[3-(2,5-dihydro-5-thioxo-1,2,4-oxadiazol-3-yl)phenyl]-9-methyl-, sodium salt, ion(1-) (1:1)

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Hazard Information

Uses

MRS4596 is a potent and selective P2X4 receptor antagonist with an IC50 value of 1.38 μM for human P2X4 receptor. MRS4596 has neuroprotective and neuro-rehabilitative activities in ischemic stroke model. MRS4596 can be used in research of ischemic stroke [1].

in vivo

MRS4719 (compound 22c; 5 mg/kg; 3 days continuous infusion with an Alzet minipump) has neuroprotective and learning- and memory-enhancing activities in a mouse middle cerebral artery occlusion (MCAO) model of ischemic stroke^[1].

Animal Model:	Male and female young C57B/6 mice (8-12 weeks; induced transient focal cerebral ischemia by a 60 min right middle cerebral artery occlusion)^[1]
Dosage:	5 mg/kg
Administration:	3 days continuous infusion with an Alzet minipump
Result:	Decreased in total hemispheric infarct volume while effects were not significant on cortical or striatal infarct volume alone.

References

[1] Toti KS, et al. Structure-Activity Relationship and Neuroprotective Activity of 1,5-Dihydro-2H-naphtho[1,2-b][1,4]diazepine-2,4(3H)-diones as P2X4 Receptor Antagonists. J Med Chem. 2022 Sep 23. DOI:10.1021/acs.jmedchem.2c01197

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