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Mesdopetam

Cat. No. M28345
Mesdopetam Structure
Synonym:

IRL790

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Biological Activity

Mesdopetam (IRL790) is a dopamine D3 receptor antagonist (Ki=90 nM; IC50=9.8 μM for human recombinant D3 receptor) with psychomotor stabilizing properties. Mesdopetam is used for the research of motor and psychiatric complications in Parkinson disease.

Chemical Information
Molecular Weight 275.34
Formula C12H18FNO3S
CAS Number 1403894-72-3
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
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] M Angela Cenci, et al. Neuropharmacology. Non-dopaminergic approaches to the treatment of motor complications in Parkinson's disease

[2] Philippe Huot, et al. Neurodegener Dis Manag. Levodopa-induced dyskinesia: a brief review of the ongoing clinical trials

[3] Folke Sjöberg, et al. Pharmacol Res Perspect. A first-in-human oral dose study of mesdopetam (IRL790) to assess its safety, tolerability, and pharmacokinetics in healthy male volunteers

[4] Susanna Waters, et al. J Pharmacol Exp Ther. Preclinical Pharmacology of [2-(3-Fluoro-5-Methanesulfonyl-phenoxy)Ethyl](Propyl)amine (IRL790), a Novel Dopamine Transmission Modulator for the Treatment of Motor and Psychiatric Complications in Parkinson Disease

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