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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
Age-related changes in pharmacokinetics and pharmacodynamics of lerisetron in the rat: a population pharmacokinetic model.
2003 Jul-Aug
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

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