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Dizocilpine

Cat. No. M2646
Dizocilpine Structure
Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mg USD 50  USD50 In stock
50mg USD 180  USD180 In stock
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Quality Control & Documentation
Biological Activity

Dizocilpine (MK-801) is a potent N-methyl-D-aspartate (NMDA) receptor antagonist with Ki of 30.5 nM.

Chemical Information
Molecular Weight 221.3
Formula C16H15N
CAS Number 77086-21-6
Solubility (25°C) DMSO 23 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] K Harsha Vardhan Reddy, et al. Convergent Strategy to Dizocilpine MK-801 and Derivatives

[2] Peter Kovacic, et al. Clinical physiology and mechanism of dizocilpine (MK-801): electron transfer, radicals, redox metabolites and bioactivity

[3] T M Tzschentke, et al. Does the noncompetitive NMDA receptor antagonist dizocilpine (MK801) really block behavioural sensitization associated with repeated drug administration?

[4] L J Vanderschuren, et al. Dizocilpine (MK801): use or abuse?

[5] B Geter-Douglass, et al. Dizocilpine-like discriminative stimulus effects of competitive NMDA receptor antagonists in mice

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