Details
Stereochemistry | ACHIRAL |
Molecular Formula | C18H20N4 |
Molecular Weight | 292.3782 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
C(N1C(=NC2=C1C=CC=C2)N3CCNCC3)C4=CC=CC=C4
InChI
InChIKey=PWWDCRQZITYKDV-UHFFFAOYSA-N
InChI=1S/C18H20N4/c1-2-6-15(7-3-1)14-22-17-9-5-4-8-16(17)20-18(22)21-12-10-19-11-13-21/h1-9,19H,10-14H2
Lerisetron is a 5-hydroxytryptamine3 receptor antagonist. It was under development by FAES Farma for the potential treatment of emesis resulting from chemotherapy. Lerisetron specifically binds to 5-HT3 receptors, located peripherally on vagus nerve terminals and centrally in the chemoreceptor trigger zone (CTZ) of the area postrema, which may result in suppression of chemotherapy-induced nausea and vomiting. Lerisetron had been in phase III clinical trials for the treatment of emesis. However, this study was discontinued.
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
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Target ID: CHEMBL2094116 |
9.2 null [pKi] | ||
Target ID: CHEMBL1899 Sources: https://www.ncbi.nlm.nih.gov/pubmed/11514154 |
0.36 nM [Ki] |
PubMed
Title | Date | PubMed |
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5-HT(3)R binding of lerisetron: an interdisciplinary approach to drug-Receptor interactions. | 2001 Aug 20 |
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Effects of lerisetron, a new 5-HT3 receptor antagonist, on ipecacuanha-induced emesis in healthy volunteers. | 2002 |
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Pharmacokinetics and pharmacological effect of lerisetron, a new 5-HT3 antagonist, in rats. | 2002 Jan |
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Lerisetron. FAES. | 2003 Jul |
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Age-related changes in pharmacokinetics and pharmacodynamics of lerisetron in the rat: a population pharmacokinetic model. | 2003 Jul-Aug |
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Subunit rotation models activation of serotonin 5-HT3AB receptors by agonists. | 2004 Oct |
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Pharmacokinetic-pharmacodynamic modeling of the hydroxy lerisetron metabolite L6-OH in rats: an integrated parent-metabolite model. | 2005 Nov |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/12404884
Single dose
intravenous - 18 mg
oral - 20 mg
Route of Administration:
Other
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NCI_THESAURUS |
C267
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NCI_THESAURUS |
C94726
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100000082572
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LERISETRON
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65997
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143257-98-1
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7059
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SUB08439MIG
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DTXSID90162368
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Q36R82SXRG
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C115094
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CHEMBL56900
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C30143
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DB12964
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ACTIVE MOIETY