General
Preferred name
BENSERAZIDE
Synonyms
BENSERAZIDE HYDROCHLORIDE ()
Ro 8-0576-12 ()
Benserazide hydrochloride (Synonyms: Serazide ()
Ro 4-4602) ()
Ro 4-4602 ()
Serazide ()
Benserazide HCl ()
Benserazide (hydrochloride) ()
RO-4-4602 ()
Benserazide (as hydrochloride) ()
NSC-755907 ()
Benserazida ()
Benserazide-d3 (hydrochloride) ()
P&D ID
PD013354
CAS
322-35-0
14919-77-8
14046-64-1
Tags
available
drug
First approval
1990
Drug Status
approved
investigational
Max Phase
4.0
Drug indication
Inhibitor (decarboxylase)
Probe control
Probe control not defined
Orthogonal probes
0
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure
P&D probe-likeness score
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
INDICATION
The primary therapeutic use for which benserazide is currently indicated for is as a combination therapy with levadopa for the treatment of Parkinson's disease in adults > 25 years of age, with the exception of drug-induced parkinsonism [F2, L2553].; ; At certain doses, the combination product of levodopa and benserazide may also be used to treat restless legs syndrome, which is sometimes associated with Parkinson's disease [L2553, T181].; ; There have also been some studies that have prompted the European Medicines Agency to confer orphan designation upon benserazide hydrochloride as a potential therapy for beta thalassaemia [F3]. Although studies are ongoing, no evidence has been formally elucidated as of yet [F3].
ROE
Benserazide is rapidly excreted in the urine in the form of metabolites, mostly within the first 6 hours of administration, 85% of urinary excretion occurs within 12 hours [T181].; ; Elimination of radiolabelled 14C-benserazide was primarily by urinary excretion with 86% to 90% of an intravenous dose recovered in the urine while 53% to 64% of an oral dose was detected in the urine [F2, L2553]. The majority of the 14C-benserazide was ultimately accounted for in the urine within 48 hours after administration [F2, L2553]. Fecal recovery studies conducted over five to eight days accounted for the majority (about 30%) of the remainder of the administered 14C-benserazide [F2, L2553].; ; Ultimately, benserazide is almost entirely eliminated by metabolism [F2, L2553]. These metabolites are mainly excreted in the urine (64%) and to a smaller extent in the feces (24%) [F2, L2553].
TOXICITY
Overdosage may lead to cardiovascular side effects like cardiac arrhythmias, psychiatric disturbances like confusion and insomnia, gastrointestinal effects like nausea and vomiting, and abnormal involuntary movements [F2, L2553].; ; Various LD50 values have been established for the rat model, including an oral LD50 of 5300 mg/kg in rats [MSDS].
DESCRIPTION
Marketed formulations may contain benserazide hydrochloride (PubChem CID 26964).
(GtoPdb)
DESCRIPTION
Peripheral decarboxylase inhibitor
(LOPAC library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
0
Organisms
1
Compound Sets
24
AdooQ Bioactive Compound Library
ChEMBL Approved Drugs
ChEMBL Drugs
Concise Guide to Pharmacology 2017/18
Concise Guide to Pharmacology 2019/20
Concise Guide to Pharmacology 2021/22
Concise Guide to Pharmacology 2023/24
Drug Repurposing Hub
DrugBank
DrugBank Approved Drugs
DrugCentral
DrugCentral Approved Drugs
DrugMAP
DrugMatrix
EU-OPENSCREEN Bioactive Compound Library
Guide to Pharmacology
LOPAC library
MedChem Express Bioactive Compound Library
NPC Screening Collection
Prestwick Chemical Library
ReFrame library
TargetMol Bioactive Compound Library
The Spectrum Collection
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
63
Molecular Weight
257.1
Hydrogen Bond Acceptors
7
Hydrogen Bond Donors
7
Rotatable Bonds
5
Ring Count
1
Aromatic Ring Count
1
cLogP
-1.76
TPSA
148.07
Fraction CSP3
0.3
Chiral centers
1.0
Largest ring
6.0
QED
0.24
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Selectivity
Decarboxylase
Pathway
GPCR/G protein
Neuroscience
Target
Dopa decarboxylase
dopamine
DDC
Indication
Parkinson's Disease
MOA
Dopa decarboxylase inhibitor
Source data
