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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
Structure of LERISETRON

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

HIDE SMILES / InChI

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

Targets

PubMed

PubMed

TitleDatePubMed
Functional group interactions of a 5-HT3R antagonist.
2002 Jun 13
Age-related changes in pharmacokinetics and pharmacodynamics of lerisetron in the rat: a population pharmacokinetic model.
2003 Jul-Aug
Patents

Patents

Sample Use Guides

Single dose intravenous - 18 mg oral - 20 mg
Route of Administration: Other
Substance Class Chemical
Created
by admin
on Sat Dec 16 16:04:26 UTC 2023
Edited
by admin
on Sat Dec 16 16:04:26 UTC 2023
Record UNII
Q36R82SXRG
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
LERISETRON
INN   WHO-DD  
INN  
Official Name English
Lerisetron [WHO-DD]
Common Name English
1-BENZYL-2-(1-PIPERAZINYL)BENZIMIDAZOLE
Systematic Name English
lerisetron [INN]
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C267
Created by admin on Sat Dec 16 16:04:26 UTC 2023 , Edited by admin on Sat Dec 16 16:04:26 UTC 2023
NCI_THESAURUS C94726
Created by admin on Sat Dec 16 16:04:26 UTC 2023 , Edited by admin on Sat Dec 16 16:04:26 UTC 2023
Code System Code Type Description
SMS_ID
100000082572
Created by admin on Sat Dec 16 16:04:26 UTC 2023 , Edited by admin on Sat Dec 16 16:04:26 UTC 2023
PRIMARY
WIKIPEDIA
LERISETRON
Created by admin on Sat Dec 16 16:04:26 UTC 2023 , Edited by admin on Sat Dec 16 16:04:26 UTC 2023
PRIMARY
PUBCHEM
65997
Created by admin on Sat Dec 16 16:04:26 UTC 2023 , Edited by admin on Sat Dec 16 16:04:26 UTC 2023
PRIMARY
CAS
143257-98-1
Created by admin on Sat Dec 16 16:04:26 UTC 2023 , Edited by admin on Sat Dec 16 16:04:26 UTC 2023
PRIMARY
INN
7059
Created by admin on Sat Dec 16 16:04:26 UTC 2023 , Edited by admin on Sat Dec 16 16:04:26 UTC 2023
PRIMARY
EVMPD
SUB08439MIG
Created by admin on Sat Dec 16 16:04:26 UTC 2023 , Edited by admin on Sat Dec 16 16:04:26 UTC 2023
PRIMARY
EPA CompTox
DTXSID90162368
Created by admin on Sat Dec 16 16:04:26 UTC 2023 , Edited by admin on Sat Dec 16 16:04:26 UTC 2023
PRIMARY
FDA UNII
Q36R82SXRG
Created by admin on Sat Dec 16 16:04:26 UTC 2023 , Edited by admin on Sat Dec 16 16:04:26 UTC 2023
PRIMARY
MESH
C115094
Created by admin on Sat Dec 16 16:04:26 UTC 2023 , Edited by admin on Sat Dec 16 16:04:26 UTC 2023
PRIMARY
ChEMBL
CHEMBL56900
Created by admin on Sat Dec 16 16:04:26 UTC 2023 , Edited by admin on Sat Dec 16 16:04:26 UTC 2023
PRIMARY
NCI_THESAURUS
C30143
Created by admin on Sat Dec 16 16:04:26 UTC 2023 , Edited by admin on Sat Dec 16 16:04:26 UTC 2023
PRIMARY
DRUG BANK
DB12964
Created by admin on Sat Dec 16 16:04:26 UTC 2023 , Edited by admin on Sat Dec 16 16:04:26 UTC 2023
PRIMARY
Related Record Type Details
ACTIVE MOIETY