Lerisetron
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
- Mol File:
- 143257-98-1.mol
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
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 |
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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Lerisetron(143257-98-1)Related Product Information
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- Palonosetron
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- Palonosetron Hydrochloride
- Palonosetron
- 1-(4-FLUORO-BENZYL)-2-PIPERAZIN-1-YL-1H-BENZOIMIDAZOLE
- 1-BENZYL-2-(4-BENZYLPIPERAZIN-1-YL)-1H-BENZIMIDAZOLE
- Lerisetron
- 1-BENZYL-2-(4-METHYL-PIPERAZIN-1-YL)-1H-BENZOIMIDAZOLE
- ZERENEX EZX001545
- 1-BENZYL-2-(4-PHENYL-PIPERAZIN-1-YL)-1H-BENZOIMIDAZOLE