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Metopimazine

Cat. No. M28333
Metopimazine Structure
Synonym:

EXP999; RP9965

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Biological Activity

Metopimazine (EXP999) is a phenothiazine derivative used to prevent emesis during chemotherapy. Metopimazine belongs to the anti-dopaminergic anti-emetics (ADA) class. Metopimazine can be used for the research of gastroenteritis (GE) .

Chemical Information
Molecular Weight 445.6
Formula C22H27N3O3S2
CAS Number 14008-44-7
Form Solid
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] Robert W Busby, et al. Pharmacol Res Perspect. Metopimazine is primarily metabolized by a liver amidase in humans

[2] Clémentine Vabre, et al. Therapie. Initial data on the safety of metopimazine during pregnancy and the risk of major birth defects and pregnancy loss - An observational study using the EFEMERIS database

[3] Michaël Rochoy, et al. Therapie. From domperidone to metopimazine: Anticipating the media impact of pharmacovigilance announcements

[4] T Sigsgaard, et al. Br J Cancer. Granisetron compared with prednisolone plus metopimazine as anti-emetic prophylaxis during multiple cycles of moderately emetogenic chemotherapy

[5] J Herrstedt. Dan Med Bull. Chemotherapy-induced nausea and vomiting with special emphasis on metopimazine

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Keywords: Metopimazine, EXP999; RP9965 supplier, inhibitors, activators


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