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Halopemide

Cat. No. M7830
Halopemide Structure
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Biological Activity

Halopemide is a dopamine receptor antagonist and a phospholipase D2 inhibitor. Halopemide may be used as a screen to identify inhibitors of human PLD2 using an in vitro biochemical assay. It is also inhibitory at benzodiazepine binding sites.

Chemical Information
Molecular Weight 416.88
Formula C21H22ClFN4O2
CAS Number 59831-65-1
Solubility (25°C) DMSO: ≥10 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] Lauren Monovich, et al. Optimization of halopemide for phospholipase D2 inhibition

[2] H De Cuyper, et al. The clinical significance of halopemide, a dopamine-blocker related to the butyrophenones

[3] A J Loonen, et al. Halopemide, a new psychotropic agent. Cerebral distribution and receptor interactions

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