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5,7-Dichlorokynurenic acid

Cat. No. M28153
5,7-Dichlorokynurenic acid Structure
Synonym:

5,7-DCKA

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Biological Activity

5,7-Dichlorokynurenic acid (5,7-DCKA) is a selective and competitive antagonist of the glycine site on NMDA receptor with a KB of 65 nM. 5,7-Dichlorokynurenic acid, a derivative of kynurenic acid, reduced NMDA-induced neuron injury in rat cortical cell cultures.

Chemical Information
Molecular Weight 258.06
Formula C10H5Cl2NO3
CAS Number 131123-76-7
Form Solid
Storage 4°C, dry, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] M Mugnaini, et al. J Recept Signal Transduct Res. [3H]5,7-dichlorokynurenic acid recognizes two binding sites in rat cerebral cortex membranes

[2] B M Baron, et al. Mol Pharmacol. Activity of 5,7-dichlorokynurenic acid, a potent antagonist at the N-methyl-D-aspartate receptor-associated glycine binding site

[3] D McNamara, et al. Neurosci Lett. 5,7-Dichlorokynurenic acid, a potent and selective competitive antagonist of the glycine site on NMDA receptors

[4] S D Hurt, et al. J Recept Res. [3H] 5,7-dichlorokynurenic acid, a high affinity ligand for the NMDA receptor glycine regulatory site

[5] B M Baron, et al. Eur J Pharmacol. [3H]5,7-dichlorokynurenic acid, a novel radioligand labels NMDA receptor-associated glycine binding sites

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Keywords: 5,7-Dichlorokynurenic acid, 5,7-DCKA supplier, GluR, inhibitors, activators


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