Morinidazole is an orally active and 5-nitroimidazole antimicrobial agent that undergoes extensive metabolism in humans via N + -glucuronidation and sulfation. Morinidazole can be used for bacterial infections research including appendicitis and pelvic inflammatory disease (PID) caused by anaerobic bacteria
In Vitro
Morinidazole can be metabolized to N + -glucuronide of S-morinidazole [M8-1] and N + -glucuronide of R-morinidazole [M8-2] via N + -glucuronidation, and sulfate conjugate of morinidazole [M7] via sulfation. M7 is a substrate for organic anion transporter 1 (OAT1) and OAT3 (K m =28.6 and 54.0 μM, respectively), M8-1 and M8-2 are the substrates for OAT3. Morinidazole shows activity against Trichomonas vaginalis and Entamoeba histolytica in vitro, with MIC values of 2 μg/mL and 3 μg/mL, respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Morinidazole (20 mg/kg or 25 mg/kg; p.o.; single dose) inhibits Trichomonas vaginalis and Entamoeba histolytica in vivo in rats with EC 50 s of 20 mg/kg and 25 mg/kg, respectively. Morinidazole (50 mg/kg; i.v.; 0.25, 0.75, 1.5 h) shows a different concentration in tissues after intravenous injection, with a higher concentration in liver, kidney, plasma than lung, heart, and spleen in mice. Pharmacokinetic parameters of Morinidazole in control and 5/6 nephrectomized (Nx) ratsGroup C max (μg/mL) T max (h) T 1/2 (h) AUC 0-t (μg·h/mL) AUC 0-∞ (μg·h/mL) CL (mL/h/kg) V ss (mL/kg) MRT (h) Control rats 48.2 0.08 1.16 87.2 87.3 582 805 1.39 5/6 Nx rats 53.2 0.08 1.32 91.2 91.3 552 891 1.62 Intravenous injection; 50 mg/kg Morinidazole; Blood samples were collected from retro-orbital venous plexus before the dose (0 hours), at 5, 15, and 30 minutes, and at 1, 2, 4, 6, 8, and 12 hours after the dose. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Renal failure model in SD rats (180-220 g)Dosage: 50 mg/kg Administration: Intravenous injection; sacrificed rats at 0.25, 0.75, and 1.50 hours after dose administration Result: Increased plasma exposures slightly compared with control.
Form:Solid
IC50& Target:organic anion transporter
