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CP-101,606

Cat. No. M8215
CP-101,606 Structure
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Biological Activity

Traxoprodil (CP-101,606) is a potent noncompetitive antagonist of N-methyl-D-aspartate (NMDA) receptors, selective for the NR2B subunit. It has been shown to be neuroprotective in animal models of brain injury and stroke.

Chemical Information
Molecular Weight 327.42
Formula C20H25NO3
CAS Number 134234-12-1
Solubility (25°C) DMSO: ≥35 mg/mL
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] Ewa Bromek, et al. The Selective NMDA Receptor GluN2B Subunit Antagonist CP-101,606 with Antidepressant Properties Modulates Cytochrome P450 Expression in the Liver

[2] Ioline D Henter, et al. Novel Glutamatergic Modulators for the Treatment of Mood Disorders: Current Status

[3] Samuel T Wilkinson, et al. A new generation of antidepressants: an update on the pharmaceutical pipeline for novel and rapid-acting therapeutics in mood disorders based on glutamate/GABA neurotransmitter systems

[4] Ioline D Henter, et al. Glutamatergic Modulators in Depression

[5] F Menniti, et al. CP-101,606, a potent neuroprotectant selective for forebrain neurons

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