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Lerisetron

SKU: orb1298932

Description

Lerisetron is a selective 5-HT3 receptor antagonist used as an antiemetic in research. It is applied in pharmacological studies to investigate emesis pathways and serotonin receptor function in both in vitro binding assays and in vivo animal models.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Images & Validation

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Lerisetron

Key Properties

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CAS Number143257-98-1
MW292.38
Purity99.82% (May vary between batches)
FormulaC18H20N4
SMILESC(N1C(=NC=2C1=CC=CC2)N3CCNCC3)C4=CC=CC=C4
Target5-HT Receptor
SolubilityDMSO:53 mg/mL (181.27 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (6.84 mM)

Bioactivity

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Target IC50
5-HT3 receptor (cell-free assay):0.81 μM
In Vivo
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.
Animal Research
Fischer 344 rats (n = 44) were divided into three groups, depending on their age: 5, 13, and 25 months. Blood samples were collected before administration of 200 micro g/kg of lerisetron for measurements of albumin, alpha(1)-acid glycoprotein, and unbound fraction of lerisetron. The lerisetron plasma concentrations were measured by high-performance liquid chromatography. A two-compartment model was fitted to the data using the nonlinear mixed-effects computer program WinNonMix. The population analysis was performed with the complete set of the collected data, and the potential sources of variability in the population parameters were investigated. Additionally, a pharmacodynamic study was performed. The effect of lerisetron (inhibition of the von Bezold-Jarisch reflex) was evaluated in young, adult, and senescent Fischer 344 rats.

Storage & Handling

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Storage-20°C
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

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5HTReceptor, 5-hydroxytryptamine Receptor, 5-HT3, 5HT Receptor, 5-HT Receptor, Bradycardia, inhibit, Inhibitor, Lerisetron, SD rats, Serotonin Receptor, Serotonin, Pharmacokinetics

Similar Products

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  • Lerisetron

    Lerisetron [orb1220146]

    >98% (HPLC)

    143257-98-1

    292.38

    C18H20N4

    5 mg, 10 mg, 25 mg, 50 mg, 1 g, 2 mg, 100 mg, 200 mg, 500 mg
Quality Guarantee

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Compound Identifiers

PubChem CID
65997 ↗

Key Properties

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No computed properties available.

Protocol Information

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Available Sizes

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1 mg
$ 100.00
5 mg
$ 170.00
1 ml x 10 mM (in DMSO)
$ 170.00
10 mg
$ 240.00
25 mg
$ 390.00
50 mg
$ 560.00
100 mg
$ 780.00
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