Introduction：Basic information about CAS 143257-98-1|Lerisetron, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| Common Name | Lerisetron |
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| CAS Number | 143257-98-1 | Molecular Weight | 292.37800 |
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| Density | 1.22g/cm3 | Boiling Point | 502ºC at 760mmHg |
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| Molecular Formula | C18H20N4 | Melting Point | / |
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| MSDS | / | Flash Point | 257.4ºC |
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Names
| Name | 1-benzyl-2-piperazin-1-ylbenzimidazole |
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| Synonym | More Synonyms |
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Lerisetron BiologicalActivity
| Description | 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]. |
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| Related Catalog | Research Areas >>Cardiovascular DiseaseResearch Areas >>Neurological DiseaseSignaling Pathways >>GPCR/G Protein >>5-HT ReceptorSignaling Pathways >>Neuronal Signaling >>5-HT Receptor |
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| Target | pKi: 9.2 (5-HT3)[1] |
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| 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. |
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Chemical & Physical Properties
| Density | 1.22g/cm3 |
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| Boiling Point | 502ºC at 760mmHg |
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| Molecular Formula | C18H20N4 |
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| Molecular Weight | 292.37800 |
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| Flash Point | 257.4ºC |
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| Exact Mass | 292.16900 |
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| PSA | 33.09000 |
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| LogP | 2.88800 |
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| Vapour Pressure | 3.31E-10mmHg at 25°C |
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| Index of Refraction | 1.669 |
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| InChIKey | PWWDCRQZITYKDV-UHFFFAOYSA-N |
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| SMILES | c1ccc(Cn2c(N3CCNCC3)nc3ccccc32)cc1 |
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| Storage condition | -20°C |
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Synonyms
| Lerisetron |
| lerisetron[inn] |
| UNII-Q36R82SXRG |
| 1-Benzyl-2-piperazin-1-yl-1H-benzoimidazole |
| 1-benzyl-2-(piperazin-1-yl)-1H-benzimidazole |
| 1-phenylmethyl-2-(1-piperazinyl)-1H-benzimidazole |
