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
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL2094116 |
9.2 null [pKi] | ||
Target ID: CHEMBL1899 Sources: https://www.ncbi.nlm.nih.gov/pubmed/11514154 |
0.36 nM [Ki] |
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
Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 16:04:26 UTC 2023
by
admin
on
Sat Dec 16 16:04:26 UTC 2023
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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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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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NCI_THESAURUS |
C94726
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admin on Sat Dec 16 16:04:26 UTC 2023 , Edited by admin on Sat Dec 16 16:04:26 UTC 2023
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Code System | Code | Type | Description | ||
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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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Related Record | Type | Details | ||
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ACTIVE MOIETY |