(R)-Morinidazole

(R)-Morinidazole is an orally active and 5-nitroimidazole antimicrobial agent that undergoes extensive metabolism in humans via N⁺-glucuronidation and sulfation. (R)-Morinidazole can be used for bacterial infections research including appendicitis and pelvic inflammatory disease (PID) caused by anaerobic bacteria^[1]. IC50 & Target:organic anion transporter^[1] In Vitro:(R)-Morinidazole can be metabolized to N⁺-glucuronide of S-Morinidazole R enantiomer [M8-1] and N⁺-glucuronide of (R)-Morinidazole [M8-2] via N⁺-glucuronidation, and sulfate conjugate of (R)-Morinidazole [M7] via sulfation^[1].
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^[1].
(R)-Morinidazole shows activity against Trichomonas vaginalis and Entamoeba histolytica in vitro, with MIC values of 2 μg/mL and 3 μg/mL, respectively^[2].
In Vivo:(R)-Morinidazole (20 mg/kg or 25 mg/kg; p.o.; single dose) inhibits Trichomonas vaginalis and Entamoeba histolytica in vivo in rats with EC₅₀s of 20 mg/kg and 25 mg/kg, respectively^[2].
(R)-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^[3].
Pharmacokinetic parameters of (R)-Morinidazole in control and 5/6 nephrectomized (Nx) rats^[3]

Group	Cmax (μg/mL)	Tmax (h)	T1/2 (h)	AUC0-t (μg·h/mL)	AUC0-∞ (μg·h/mL)	CL (mL/h/kg)	Vss (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 (R)-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.