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Ro 25-6981 

Cat. No. M28813
Ro 25-6981  Structure
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Biological Activity

Ro 25-6981 is a potent, selective and activity-dependent NR2B subunit specific NMDA receptor antagonist. Ro 25-6981 shows anticonvulsant and anti-parkinsonian activity. Ro 25-6981 has the potential for the research of parkinson's disease (PD).

Chemical Information
Molecular Weight 339.47
Formula C22H29NO2
CAS Number 169274-78-6
Solubility (25°C) DMSO 100 mg/mL (ultrasonic)
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
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] Pavel Mareš, et al. Pharmaceutics. The GluN2B-Selective Antagonist Ro 25-6981 Is Effective against PTZ-Induced Seizures and Safe for Further Development in Infantile Rats

[2] Bartłomiej Pochwat, et al. Int J Mol Sci. Ketamine and Ro 25-6981 Reverse Behavioral Abnormalities in Rats Subjected to Dietary Zinc Restriction

[3] Emma Clark, et al. Behav Brain Res. Effects of the GluN2B-NMDA receptor antagonist Ro 25-6981 on two types of behavioral flexibility in rats

[4] D R Lynch, et al. Eur J Pharmacol. Pharmacological characterization of interactions of RO 25-6981 with the NR2B (epsilon2) subunit

[5] G Fischer, et al. J Pharmacol Exp Ther. Ro 25-6981, a highly potent and selective blocker of N-methyl-D-aspartate receptors containing the NR2B subunit. Characterization in vitro

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