benserazide indications/contra

Stem definitionDrug idCAS RN
314 322-35-0

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • benserazide hydrochloride
  • benserazide
  • serazide
  • benserazide HCl
An inhibitor of DOPA DECARBOXYLASE that does not enter the central nervous system. It is often given with LEVODOPA in the treatment of parkinsonism to prevent the conversion of levodopa to dopamine in the periphery, thereby increasing the amount that reaches the central nervous system and reducing the required dose. It has no antiparkinson actions when given alone.
  • Molecular weight: 257.25
  • Formula: C10H15N3O5
  • CLOGP: -2.90
  • LIPINSKI: 1
  • HAC: 8
  • HDO: 7
  • TPSA: 148.07
  • ALOGS: -1.70
  • ROTB: 5

Drug dosage:

None

Approvals:

DateAgencyCompanyOrphan
Jan. 1, 1990 YEAR INTRODUCED

FDA Adverse Event Reporting System

None

Pharmacologic Action:

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SourceCodeDescription
CHEBI has role CHEBI:48407 antiparkinson drug
CHEBI has role CHEBI:48560 dopaminergic agent
MeSH PA D018726 Anti-Dyskinesia Agents
MeSH PA D000978 Antiparkinson Agents
MeSH PA D002491 Central Nervous System Agents
MeSH PA D015259 Dopamine Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D018377 Neurotransmitter Agents

Drug Use (View source of the data)

None

Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation levelDissociation constantType (acidic/basic)
pKa1 3.67 acidic
pKa2 11.55 acidic
pKa3 12.19 acidic
pKa4 13.97 acidic
pKa5 6.88 Basic
pKa6 3.1 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Aromatic-L-amino-acid decarboxylase Enzyme WOMBAT-PK
Estrogen receptor beta Nuclear hormone receptor IC50 5.52 CHEMBL
SUMO-activating enzyme Enzyme IC50 4.63 CHEMBL
Cytoplasmic zinc-finger protein Unclassified EC50 4.43 CHEMBL
Zinc finger protein mex-5 Cytosolic other EC50 6.95 CHEMBL

External reference:

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IDSource
5150 IUPHAR_LIGAND_ID
C0770932 UMLSCUI
D01653 KEGG_DRUG
762OS3ZEJU UNII
3026 INN_ID
2327 PUBCHEM_CID
420240007 SNOMEDCT_US
391821005 SNOMEDCT_US
N0000166563 NDFRT
003682 NDDF
1374 RXNORM
14919-77-8 SECONDARY_CAS_RN
CHEBI:64187 CHEBI
CHEMBL1096979 ChEMBL_ID
CHEMBL1255778 ChEMBL_ID
DB12783 DRUGBANK_ID
D001545 MESH_DESCRIPTOR_UI

Pharmaceutical products:

None