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Dipraglurant

Cat. No. M22211
Dipraglurant Structure
Synonym:

ADX48621

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Biological Activity

Dipraglurant

Chemical Information
Molecular Weight 265.29
Formula C16H12FN3
CAS Number 872363-17-2
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] O Abu-Hadid, et al. Expert Opin Pharmacother. An overview of the pharmacotherapeutics for dystonia: advances over the past decade

[2] Shayan Pourmirbabaei, et al. Eur J Pharmacol. Pathophysiological clues to therapeutic applications of glutamate mGlu5 receptor antagonists in levodopa-induced dyskinesia

[3] Franois Tison, et al. Mov Disord. A Phase 2A Trial of the Novel mGluR5-Negative Allosteric Modulator Dipraglurant for Levodopa-Induced Dyskinesia in Parkinson's Disease

[4] Olivier Rascol, et al. Parkinsonism Relat Disord. Use of metabotropic glutamate 5-receptor antagonists for treatment of levodopa-induced dyskinesias

[5] Erwan Bezard, et al. Mov Disord. The mGluR5 negative allosteric modulator dipraglurant reduces dyskinesia in the MPTP macaque model

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