| Identification | Back Directory | [Name]
Lerisetron | [CAS]
143257-98-1 | [Synonyms]
F-0930-RS
CID 65997
Lerisetron
1-benzyl-2-piperazin-1-ylbenzimidazole
1-BENZYL-2-PIPERAZIN-1-YL-1H-BENZIMIDAZOLE
1H-Benzimidazole, 1-(phenylmethyl)-2-(1-piperazinyl)-
1-benzyl-2-piperazin-1-yl-1H-benzimidazole dihydrochloride | [Molecular Formula]
C18H20N4 | [MDL Number]
MFCD22587621 | [MOL File]
143257-98-1.mol | [Molecular Weight]
292.38 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: 58 mg/mL (198.37 mM);Ethanol: 58 mg/mL (198.37 mM) | [form ]
Solid | [color ]
White to off-white | [Water Solubility ]
Water: Insoluble |
| Hazard Information | Back Directory | [Uses]
Lerisetron is a potent 5-HT3 antagonists and possess high-affinity binding for the 5-HT3 receptors with pKi value of 9.2. Lerisetron has a potent ability to inhibit the 5-HT-evoked reflex bradycardia in urethane-anesthetized rats[1]. | [in vivo]
Lerisetron (50-200 μg/kg; IV; single) exhibits CL of 0.004-0.005 L/min, Vds of 0.88-0.96 L, MRT0-LAST of 224-337.1 min and AUC∞ of 57.7-66.1 μg·min/L in rats[2].
Lerisetron (2-10 μg/kg; IV; single) causes rapid recovery from bradycardia[2].
Pharmacokinetic Parameters of Lerisetron in Sprague-Dawley rats[2].
| IV (50 μg/kg) | IV (100 μg/kg) | IV (200 μg/kg) | | CL (L/min) | 0.005 | 0.004 | 0.004 | | Vds (L) | 0.9 | 0.88 | 0.96 | | MRT0-LAST (min) | 224 | 337.1 | 226.3 | | AUC∞ (μg·min/L) | 66.1 | 57.7 | 58.1 |
| [References]
[1] Orjales A, Mosquera R, Labeaga L, Rodes R. New 2-piperazinylbenzimidazole derivatives as 5-HT3 antagonists. Synthesis and pharmacological evaluation. J Med Chem. 1997;40(4):586-593.
[2] Jauregizar N, Calvo R, Suarez E, Quintana A, Raczka E, Lukas JC. Pharmacokinetics and pharmacological effect of lerisetron, a new 5-HT3 antagonist, in rats. J Pharm Sci. 2002;91(1):41-52. DOI:10.1002/jps.1169 |
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