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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)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
1 mL x 10 mM in DMSO 120 In Stock
5MG 123 In Stock
10MG 188 In Stock
25MG 332 In Stock
50MG 477 In Stock
100MG 685 In Stock
200MG Get Quote In Stock
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Biological Information

  • Product Name
    Lerisetron
  • Note
    Research use only, not for human use.
  • Brief Description
    Lerisetron is an antagonist of serotonin type 3 (5-HT3) receptor, with antiemetic activity.
  • Description
    Lerisetron 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.
  • In Vitro
    ——
  • 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.Lerisetron (2-10 μg/kg; IV; single) causes rapid recovery from bradycardia.Pharmacokinetic Parameters of Lerisetron in Sprague-Dawley rats.
  • Synonyms
    ——
  • Pathway
    Endocrinology/Hormones
  • Target
    5-HT Receptor
  • Recptor
    5-HT3
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    143257-98-1
  • Formula Weight
    292.38
  • Molecular Formula
    C18H20N4
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO:53 mg/ml(181.27 mM)
  • SMILES
    C(c1ccccc1)n1c(nc2ccccc12)N1CCNCC1
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • 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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