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CAS NO.147116-67-4
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Maropitant is a neurokinin type 1 (NK-1) receptor antagonist. Recent studies show that Maropitant decreased the anesthetic requirements during visceral stimulation of the ovary and ovarian ligament in dogs.
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).
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Maropitant is a selective and orally active neurokinin (NK1) receptor antagonist. Maropitant acts by blocking the binding of substance P within the emetic center and the chemoreceptor trigger zone (CRTZ). Maropitant is highly effective in preventing vomiting.
Name | Maropitant |
---|---|
Iupac Chemical Name | (1R,2S,3S,4R)-2-benzhydryl-N-(5-(tert-butyl)-2-methoxybenzyl)quinuclidin-3-amine |
Synonyms | CJ-11,972; CJ 11,972; CJ11,972; CJ-11972; CJ 11972; CJ11972; Maropitant; |
Molecular Formula | C32H40N2O |
Molecular Weight | 468.6728 |
Smile | COC1=CC=C(C(C)(C)C)C=C1CN[C@@H]2[C@H](C(C3=CC=CC=C3)C4=CC=CC=C4)[N@]5CC[C@]2([H])CC5 |
InChiKey | OMPCVMLFFSQFIX-CONSDPRKSA-N |
InChi | InChI=1S/C32H40N2O/c1-32(2,3)27-15-16-28(35-4)26(21-27)22-33-30-25-17-19-34(20-18-25)31(30)29(23-11-7-5-8-12-23)24-13-9-6-10-14-24/h5-16,21,25,29-31,33H,17-20,22H2,1-4H3/t30-,31-/m0/s1 |
CAS Number | 147116-67-4 |