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Details

Stereochemistry RACEMIC
Molecular Formula C10H15N3O5
Molecular Weight 257.2432
Optical Activity ( + / - )
Defined Stereocenters 0 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of BENSERAZIDE

SMILES

NC(CO)C(=O)NNCC1=CC=C(O)C(O)=C1O

InChI

InChIKey=BNQDCRGUHNALGH-UHFFFAOYSA-N
InChI=1S/C10H15N3O5/c11-6(4-14)10(18)13-12-3-5-1-2-7(15)9(17)8(5)16/h1-2,6,12,14-17H,3-4,11H2,(H,13,18)

HIDE SMILES / InChI

Molecular Formula C10H15N3O5
Molecular Weight 257.2432
Charge 0
Count
MOL RATIO 1 MOL RATIO (average)
Stereochemistry RACEMIC
Additional Stereochemistry No
Defined Stereocenters 0 / 1
E/Z Centers 0
Optical Activity ( + / - )

Description

Benserazide is a peripherally-acting aromatic L-amino acid decarboxylase (AADC) or DOPA decarboxylase inhibitor. Benserazide is only used in conjunction with L-dopa for the treatment of Parkinson's disease under the brand name Madopar in the UK. Madopar HBS (125 mg) is a controlled-release dosage form with 100 mg L-dopa and 25 mg benserazide.

CNS Activity

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency
550.0 nM [IC50]
30.0 µM [IC50]

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
MADOPAR

PubMed

Sample Use Guides

In Vivo Use Guide
Patients NOT already treated with levodopa: The usual starting dose is one 50 mg/12.5 mg tablet (50 mg levodopa), three or four times a day. Your doctor will then increase your dose every 2 to 3 days until they find the right dose for you. Patients already treated with levodopa: Your starting dose of Madopar will be one less 100 mg/25 mg tablet than the number of levodopa 500 mg capsules or tablets you take each day. For example if you take four levodopa tablets (2000 mg levodopa) each day, your doctor will start by giving you three Madopar 100 mg/25 mg tablets daily. After one week your doctor may then start to increase your dose every 2 to 3 days until they find the right dose for you. Patients already treated with a combined levodopa/decarboxylase inhibitor: The usual starting dose is one 50 mg/12.5 mg tablet (50 mg levodopa), three or four times a day. Your doctor will then increase your dose every 2 to 3 days until they find the right dose for you.
Route of Administration: Oral
In Vitro Use Guide
Benserazide inhibited AADC with IC50 550 and 530 nM in the presence and absence of 1 mM pargyline, respectively.
Substance Class Chemical
Record UNII
762OS3ZEJU
Record Status Validated (UNII)
Record Version