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Maropitant (Cerenia) is a novel, selective neurokinin type-1 (NK1) receptor antagonist developed to treat and prevent emesis in dogs; it is administered by subcutaneous (s.c.) injection at 1 mg/kg, or orally (p.o.), in tablet form, at either 2 or 8 mg/kg depending on indication. The absolute bioavailability of maropitant was markedly higher (90.7%) following s.c. injection than after oral administration (23.7% at the 2 mg/kg dose and 37.0% at the 8 mg/kg dose). First-pass metabolism contributes to the low bioavailability of maropitant following oral administration. The difference in bioavailability between the two oral doses reflects the nonlinear kinetics characterizing the disposition of maropitant within the 2-8 mg/kg dose range. Systemic clearance of maropitant following intravenous (i.v.) administration was 970, 995 and 533 mL/h.kg at doses of 1, 2 and 8 mg/kg, respectively. Nonproportional kinetics were observed for p.o. administered maropitant at doses ranging from 2 to 16 mg/kg but dose proportionality was demonstrated at higher doses (20-50 mg/kg).
| Molecular Weight | 468.67 |
| Formula | C32H40N2O |
| CAS Number | 147116-67-4 |
| Solubility (25°C) | DMSO 10 mM |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Neurokinin Receptor Products |
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| Monohydroxy Netupitant
Monohydroxy Netupitant is the metabolite of Netupitant, which is a highly selective NK1 receptor antagonist. |
| Aprepitant
Aprepitant (Emend) is an antiemetic chemical compound that belongs to a class of compounds called substance P antagonists (SPA). |
| Eprazinone dihydrochloride
Eprazinone is a mucolytic. |
| Fosaprepitant dimeglumine salt
Fosaprepitant is a water-soluble phosphoryl procompound for Aprepitant which is a NK1 antagonist.*The compound is unstable in solutions, freshly prepared is recommended |
| Netupitant
Netupitant is a selective neurokinin 1 (NK1) receptor antagonist with potential antiemetic activity with Ki of 0.95 nM. |
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