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(R)-Morinidazole

CAS No. : 898230-59-6

MCE 站：(R)-Morinidazole

产品活性：(R)-Morinidazole 是一种口服有效的 5-硝基咪唑抗菌剂，在人体中通过 N⁺-葡萄糖醛酸化和磺化进行代谢。(R)-Morinidazole 可用于用于研究细菌感染，包括厌氧菌引起的阑尾炎、盆腔炎 (PID) 等。

研究领域：Anti-infection

作用靶点：Bacterial

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.
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.
(R)-Morinidazole shows activity against Trichomonas vaginalis ａnd Entamoeba histolytica in vitro, with MIC values of 2 μg/mL ａnd 3 μg/mL, respectively.

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.
(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.
Pharmacokinetic parameters of (R)-Morinidazole in control ａnd 5/6 nephrectomized (Nx) rats

Group	Cmax (μg/mL)	Tmax (h)	T1/2 (h)	AUC0-t (μgh/mL)	AUC0-∞ (μgh/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.

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