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
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)
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.
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL1843 |
550.0 nM [IC50] | ||
Target ID: CHEMBL3399911 |
30.0 µM [IC50] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | MADOPAR Approved UseMADOPAR is indicated for the treatment of all forms of Parkinson's syndrome with the exception of
medicine-induced parkinsonism. |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Selegiline: a second look. Six years later: too risky in Parkinson's disease. | 2002 Aug |
|
| Dopamine and human information processing: a reaction-time analysis of the effect of levodopa in healthy subjects. | 2002 Aug |
|
| Striatal metabotropic glutamate receptor function following experimental parkinsonism and chronic levodopa treatment. | 2002 Dec |
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| Adenosine A2A antagonism reverses levodopa-induced motor alterations in hemiparkinsonian rats. | 2002 Dec 15 |
|
| Gateways to Clinical Trials. June 2002. | 2002 Jun |
|
| [The effect of shourong compound formula on levels of dopamine and its metabolites in brain of Parkinson's disease mice induced by reserpine]. | 2002 May |
|
| Stimulation of cannabinoid receptors reduces levodopa-induced dyskinesia in the MPTP-lesioned nonhuman primate model of Parkinson's disease. | 2002 Nov |
|
| Naloxone reduces levodopa-induced dyskinesias and apomorphine-induced rotations in primate models of parkinsonism. | 2002 Oct |
|
| Pramipexole in Parkinson's disease. A short-term study using the combined levodopa-dopamine agonist test. | 2002 Oct-Dec |
|
| Growth-hormone release to clonidine and the clinical response to levodopa in parkinsonism. | 2002 Sep |
|
| Comparative single- and multiple-dose pharmacokinetics of levodopa and 3-O-methyldopa following a new dual-release and a conventional slow-release formulation of levodopa and benserazide in healthy volunteers. | 2003 |
|
| Time course of striatal DeltaFosB-like immunoreactivity and prodynorphin mRNA levels after discontinuation of chronic dopaminomimetic treatment. | 2003 Feb |
|
| Benserazide-induced gynaecomastia. | 2003 Jan-Feb |
|
| Catechol-O-methyltransferase inhibition in erythrocytes and liver by BIA 3-202 (1-[3,4-dibydroxy-5-nitrophenyl]-2-phenyl-ethanone). | 2003 Jun |
|
| Acute double-blind, placebo-controlled sleep laboratory and clinical follow-up studies with a combination treatment of rr-L-dopa and sr-L-dopa in restless legs syndrome. | 2003 Jun |
|
| Effects of benserazide on L-DOPA-derived extracellular dopamine levels and aromatic L-amino acid decarboxylase activity in the striatum of 6-hydroxydopamine-lesioned rats. | 2003 Mar |
|
| BIA 3-202, a novel catechol-O-methyltransferase inhibitor, reduces the peripheral O-methylation of L-DOPA and enhances its availability to the brain. | 2003 May |
|
| Improvement of sleep hypopnea by antiparkinsonian drugs in a patient with Parkinson's disease: a polysomnographic study. | 2003 Nov |
|
| Levodopa pharmacokinetics and dyskinesias: are there sex-related differences? | 2003 Oct |
|
| Hyperleptinemia elicited by the 5-HT precursor, 5-hydroxytryptophan in mice: involvement of insulin. | 2003 Sep 19 |
|
| [Influence of L-DOPA on rat brain depending on individual behavioral features]. | 2004 |
|
| Depletion and restoration of endogenous monoamines affects beta-CIT binding to serotonin but not dopamine transporters in non-human primates. | 2004 |
|
| Gas chromatography/mass spectrometric identification of dopaminergic metabolites in striata of rats treated with L-DOPA. | 2004 |
|
| Parkinsonism following anterior choroidal artery stroke. | 2004 Apr |
|
| Comparison between dopaminergic agents and physical exercise as treatment for periodic limb movements in patients with spinal cord injury. | 2004 Apr |
|
| Static mechanical hyperalgesia without dynamic tactile allodynia in patients with restless legs syndrome. | 2004 Apr |
|
| L-DOPA reverses the hypokinetic behaviour and rigidity in rotenone-treated rats. | 2004 Aug 31 |
|
| Effect of the adenosine A2A receptor antagonist 8-(3-chlorostyryl)caffeine on L-DOPA biotransformation in rat striatum. | 2004 Feb 20 |
|
| Phenotypic heterogeneity of dopa-responsive dystonia in monozygotic twins. | 2004 Feb 24 |
|
| Chronic levodopa intake increases levodopa plasma bioavailability in patients with Parkinson's disease. | 2004 Jun 17 |
|
| Augmentation of endogenous dopamine production increases lung liquid clearance. | 2004 Mar 15 |
|
| The neurobehavioral changes induced by bilateral rotenone lesion in medial forebrain bundle of rats are reversed by L-DOPA. | 2004 May 5 |
|
| [What helps in the treatment of restless legs?]. | 2004 Nov 11 |
|
| Cross talk between the intrarenal dopaminergic and cyclooxygenase-2 systems. | 2005 Apr |
|
| Enhanced cortical dopamine output and antipsychotic-like effect of raclopride with adjunctive low-dose L-dopa. | 2005 Aug 15 |
|
| 3,4-dihydroxyphenylalanine reverses the motor deficits in Pitx3-deficient aphakia mice: behavioral characterization of a novel genetic model of Parkinson's disease. | 2005 Feb 23 |
|
| [Madopar in the complex therapy of ischemic insult]. | 2005 Jan |
|
| Pharmacological validation of a mouse model of l-DOPA-induced dyskinesia. | 2005 Jul |
|
| [Idiopathic Parkinson's disease: practical hints for the treatment]. | 2005 Jul 27 |
|
| Genetic polymorphism of catechol-O-methyltransferase and levodopa pharmacokinetic-pharmacodynamic pattern in patients with Parkinson's disease. | 2005 Jun |
|
| Cholinopositive effect of dilept (neurotensin peptidomimetic) as the basis of its mnemotropic effect. | 2005 Mar |
|
| DOPA-sensitive dystonia-plus syndrome. | 2005 Mar |
|
| Early administration of entacapone prevents levodopa-induced motor fluctuations in hemiparkinsonian rats. | 2005 Mar |
|
| A spectroscopic study on applicability of spectral analysis for simultaneous quantification of l-dopa, benserazide and ascorbic acid in batch and flow systems. | 2005 Nov |
|
| Impact of levodopa on reduced nerve growth factor levels in patients with Parkinson disease. | 2005 Sep-Oct |
|
| Effect of L-dopa decarboxylase inhibitor benserazide on renal function in streptozotocin-diabetic rats. | 2006 |
|
| Paraphilic behaviours in a parkinsonian patient with hedonistic homeostatic dysregulation. | 2006 Dec |
|
| Prevention of levodopa-induced dyskinesias by a selective NR1A/2B N-methyl-D-aspartate receptor antagonist in parkinsonian monkeys: implication of preproenkephalin. | 2006 Jan |
|
| L-3,4-dihydroxyphenylalanine-induced c-Fos expression in the CNS under inhibition of central aromatic L-amino acid decarboxylase. | 2006 Jun |
|
| Levodopa availability improves with progression of Parkinson's disease. | 2006 Sep |
Patents
Sample Use Guides
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
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NCI_THESAURUS |
C38149
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NCI_THESAURUS |
C471
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3026
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100000086357
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314
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322-35-0
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DB12783
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CHEMBL1096979
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5150
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64187
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C81109
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BENSERAZIDE
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m2322
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1374
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SUB05731MIG
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D001545
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762OS3ZEJU
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ACTIVE MOIETY
SALT/SOLVATE (PARENT)
