Biological Activity

Dizocilpine (MK-801) is a potent N-methyl-D-aspartate (NMDA) receptor antagonist with K_i 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 K_m factor for a mouse and then divide by the K_m 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