General
Preferred name
Troriluzole
Synonyms
BHV4157 ()
BHV-4157 ()
BHV-4157a ()
FC 4157 ()
BHV 4157 ()
TRORILUZOLE HYDROCHLORIDE ()
Trigriluzole ()
BHV-4157A ()
BHV-4157 HYDROCHLORIDE ()
P&D ID
PD122247
CAS
1926203-09-9
Tags
available
prodrug
drug candidate
Drug Status
investigational
Max Phase
3.0
Drug indication
obsessive-compulsive disorder
Probe control
Probe control not defined
Orthogonal probes
0
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION
Troriluzole (BHV-4157) is a prodrug of the voltage-dependent calcium channel blocker riluzole. Chemically it is riluzole conjugated to a tripeptide carrier (IUPAC sequence H-Gly-Gly-Sar-Unk, where Unk = the riluzole component), and the active moiety is released by peptidases in vivo. The prodrug is more stable than riluzole and is suitable for once-daily dosing.
(GtoPdb)
DESCRIPTION
Troriluzole, a third-generation, tripeptide proagent of Riluzole (HY-B0211), is an orally active glutamate modulator. Troriluzole reduces synaptic glutamate level and increases the synaptic glutamate absorption. Troriluzole has the potential for Alzheimer disease and generalized anxiety disorder (GAD)[1][2].
DESCRIPTION
Troriluzole is an orally active glutamate modulator with anticancer activity.Troriluzole enhances the expression of excitatory amino acid transporters located in glial cells and is used in the study of spinocerebellar ataxia, Alzheimer's disease, and generalized anxiety disorder (GAD).
(TargetMol Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Compound Sets
5
ChEMBL Drugs
DrugBank
Guide to Pharmacology
MedChem Express Bioactive Compound Library
TargetMol Bioactive Compound Library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
17
Molecular Weight
419.09
Hydrogen Bond Acceptors
7
Hydrogen Bond Donors
3
Rotatable Bonds
7
Ring Count
2
Aromatic Ring Count
2
cLogP
0.67
TPSA
126.65
Fraction CSP3
0.33
Chiral centers
0.0
Largest ring
6.0
QED
0.61
Structural alerts
0
No structural alerts detected
Custom attributes
(extracted from source data)
Target
mGluR
GLU
Pathway
GPCR/G protein
Neuronal Signaling
Metabolism
Source data

