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
| Molecular Formula | C18H20N4 |
| Molecular Weight | 292.3782 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
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
PubMed
| Title | Date | PubMed |
|---|---|---|
| 5-HT(3)R binding of lerisetron: an interdisciplinary approach to drug-Receptor interactions. | 2001 Aug 20 |
|
| 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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| Subunit rotation models activation of serotonin 5-HT3AB receptors by agonists. | 2004 Oct |
|
| Pharmacokinetic-pharmacodynamic modeling of the hydroxy lerisetron metabolite L6-OH in rats: an integrated parent-metabolite model. | 2005 Nov |
Patents
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sun Dec 18 17:56:52 UTC 2022
by
admin
on
Sun Dec 18 17:56:52 UTC 2022
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| Record UNII |
Q36R82SXRG
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| Record Status |
Validated (UNII)
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| Record Version |
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| Name | Type | Language | ||
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Official Name | English | ||
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Common Name | English | ||
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Systematic Name | English | ||
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Common Name | English |
| Classification Tree | Code System | Code | ||
|---|---|---|---|---|
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NCI_THESAURUS |
C267
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admin on Sun Dec 18 17:56:53 UTC 2022 , Edited by admin on Sun Dec 18 17:56:53 UTC 2022
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NCI_THESAURUS |
C94726
Created by
admin on Sun Dec 18 17:56:53 UTC 2022 , Edited by admin on Sun Dec 18 17:56:53 UTC 2022
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| Code System | Code | Type | Description | ||
|---|---|---|---|---|---|
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LERISETRON
Created by
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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
Created by
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CHEMBL56900
Created by
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C30143
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DB12964
Created by
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PRIMARY |
| Related Record | Type | Details | ||
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ACTIVE MOIETY |
