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NMDA receptor antagonist 8

Cat. No. M42200
NMDA receptor antagonist 8 Structure
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Biological Activity

NMDA receptor antagonist 8 is GluN2B subunit-selective NMDA Receptor antagonist, with an Ki of 265 nM and an IC50 of 62 nM.

Chemical Information
Molecular Weight 349.47
Formula C22H27N3O
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
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] Ayodeji O Egunlusi et al. Molecules. 4-Oxatricyclo[5.2.1.02,6]dec-8-ene-3,5-dione Derivatives as NMDA Receptor- and VGCC Blockers with Neuroprotective Potential

[2] Tetsuro Kikuchi. Biomolecules. Is Memantine Effective as an NMDA-Receptor Antagonist in Adjunctive Therapy for Schizophrenia?

[3] Irena Smaga et al. Curr Neuropharmacol. Cocaine-induced Changes in the Expression of NMDA Receptor Subunits

[4] Daniela Catarzi et al. Curr Top Med Chem. Competitive Gly/NMDA receptor antagonists

[5] J N Kew et al. Br J Pharmacol. State-dependent NMDA receptor antagonism by Ro 8-4304, a novel NR2B selective, non-competitive, voltage-independent antagonist

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