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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
MOL RATIO 1 MOL RATIO (average)
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description

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 TargetPharmacologyConditionPotency
9.2 null [pKi]
0.36 nM [Ki]

PubMed

Patents

Sample Use Guides

In Vivo Use Guide
Single dose intravenous - 18 mg oral - 20 mg
Route of Administration: Other
Substance Class Chemical
Record UNII
Q36R82SXRG
Record Status Validated (UNII)
Record Version