Introduction：Basic information about Lerisetron CAS 143257-98-1, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
Lerisetron Basic information
| Product Name: | Lerisetron |
| Synonyms: | 1-benzyl-2-piperazin-1-ylbenzimidazole;F-0930-RS;Lerisetron;1-benzyl-2-piperazin-1-yl-1H-benzimidazole dihydrochloride;1-BENZYL-2-PIPERAZIN-1-YL-1H-BENZIMIDAZOLE;CID 65997;1H-Benzimidazole, 1-(phenylmethyl)-2-(1-piperazinyl)-;5-HT Receptor,Serotonin Receptor,Serotonin,Lerisetron,Bradycardia,Inhibitor,5-hydroxytryptamine Receptor,Pharmacokinetics,inhibit,SD rats |
| CAS: | 143257-98-1 |
| MF: | C18H20N4 |
| MW: | 292.38 |
| EINECS: | |
| Product Categories: | |
| Mol File: | 143257-98-1.mol |
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Lerisetron Chemical Properties
| 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 |
Safety Information
Lerisetron Usage And Synthesis
| 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 |
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| 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 |
Lerisetron Preparation Products And Raw materials
| Raw materials | 2-CHLORO-1-(PHENYLMETHYL)-BENZIMIDAZOLE-->2-Chlorobenzimidazole-->Piperazine-->Benzyl bromide |
