
Lerisetron
CAS No. 143257-98-1
Lerisetron( —— )
Catalog No. M21941 CAS No. 143257-98-1
Lerisetron is an antagonist of serotonin type 3 (5-HT3) receptor, with antiemetic activity.
Purity : >98% (HPLC)






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Biological Information
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Product NameLerisetron
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NoteResearch use only, not for human use.
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Brief DescriptionLerisetron is an antagonist of serotonin type 3 (5-HT3) receptor, with antiemetic activity.
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DescriptionLerisetron is an antagonist of serotonin type 3 (5-HT3) receptor, with antiemetic activity.showed a decrease in total clearance and distribution volume of the central compartment in old rats. The lerisetron free (unbound) fraction remained unchanged among the groups, and there were no significant differences in alpha(1)-acid glycoprotein levels. The concentration-effect relationship was best described by a sigmoid E(max) model. Since the drug concentration in plasma at half-maximal effect (EC(50)) decreased in old rats, an increased sensitivity to the effect of lerisetron in old animals could be expected.
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In Vitro——
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In VivoLerisetron (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.Lerisetron (2-10 μg/kg; IV; single) causes rapid recovery from bradycardia.Pharmacokinetic Parameters of Lerisetron in Sprague-Dawley rats.
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Synonyms——
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PathwayEndocrinology/Hormones
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Target5-HT Receptor
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Recptor5-HT3
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Research Area——
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Indication——
Chemical Information
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CAS Number143257-98-1
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Formula Weight292.38
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Molecular FormulaC18H20N4
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Purity>98% (HPLC)
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SolubilityDMSO:53 mg/ml(181.27 mM)
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SMILESC(c1ccccc1)n1c(nc2ccccc12)N1CCNCC1
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Nerea, Jauregizar, Antonio, et al. Age-Related Changes in Pharmacokinetics and Pharmacodynamics of Lerisetron in the Rat: A Population Pharmacokinetic Model[J]. Gerontology, 2003
2. Strenge H , Goebel S , Kowalski J , et al. Effects of Lerisetron, a New 5-HT3 Receptor Antagonist, on Ipecacuanha- induced Emesis in Healthy Volunteers[J]. Arzneimittelforschung, 2002, 52(09):689-694.
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