Compounds > nebicapone
Page last updated: 2024-12-11

nebicapone

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Description

nebicapone: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9838389
CHEMBL ID160038
SCHEMBL ID132167
MeSH IDM0555257

Synonyms (22)

Synonym
bia 3-202
1-(3,4-dihydroxy-5-nitrophenyl)-2-phenylethanone
1-(3,4-dihydroxy-5-nitro-phenyl)-2-phenyl-ethanone
bdbm50108878
nebicapone
CHEMBL160038 ,
nebicapone [inn]
ethanone, 1-(3,4-dihydroxy-5-nitrophenyl)-2-phenyl-
1-(3,4-dihydroxy-5-nitrophenyl)-2-phenylethan-1-one
unii-nm2kxj990t
nm2kxj990t ,
274925-86-9
SCHEMBL132167
DTXSID30181912
FT-0703128
HY-106405
DB14849
Q21547145
CS-0025737
3-nitro-5-phenylacetyl catechol
MS-23873
AKOS040742276

Research Excerpts

Overview

Nebicapone is a reversible catechol-O-methyltransferase (COMT) inhibitor. It is being developed for use as an adjunct to levodopa/dopa decarboxylase inhibitor.

ExcerptReferenceRelevance
"Nebicapone is a new COMT inhibitor currently being developed for use as an adjunct to levodopa/dopa decarboxylase inhibitor in the treatment of PD."( Pharmacokinetic-pharmacodynamic interaction between nebicapone, a novel catechol-o-methyltransferase inhibitor, and controlled-release levodopa/carbidopa 200 mg/50 mg : randomized, double-blind, placebo-controlled, crossover study in healthy subjects.
Almeida, L; Costa, R; Falcão, A; Lopes, C; Loureiro, AI; Machado, R; Nunes, T; Rocha, J; Soares-da-Silva, P; Torrão, L; Vaz-da-Silva, M; Wright, L, 2008)		1.32
"Nebicapone is a reversible catechol-O-methyltransferase (COMT) inhibitor. "( Pharmacokinetic-pharmacodynamic interaction between nebicapone and controlled-release levodopa/benserazide: a single-center, Phase I, double-blind, randomized, placebo-controlled, four-way crossover study in healthy subjects.
Almeida, L; Costa, R; Falcão, A; Fernandes-Lopes, C; Loureiro, AI; Machado, R; Nunes, T; Rocha, JF; Soares-da-Silva, P; Torrão, L; Vaz-da-Silva, M; Wright, L, 2009)		2.05

Treatment

ExcerptReferenceRelevance
"Both nebicapone treatment regimens were subjectively well-tolerated, but a clinically relevant elevation in aspartate transaminase was observed in one subject of each nebicapone group."( Chronopharmacology of nebicapone, a new catechol-O-methyltransferase inhibitor.
Almeida, L; Falcão, A; Fernandes-Lopes, C; Igreja, B; Loureiro, AI; Maia, J; Soares-da-Silva, P; Torrão, L; Vaz-da-Silva, M; Wright, L, 2010)		1.13

Toxicity

ExcerptReferenceRelevance
"The objectives of this study were to analyze the clinical efficacy in reducing motor complications and to evaluate their use in clinical practice and the adverse events reported in the literature."( A systematic review of catechol-0-methyltransferase inhibitors: efficacy and safety in clinical practice.
Ceravolo, R; Gioulis, M; Marsala, SZ; Tinazzi, M, )		0.13
" Entacapone is generally well tolerated, and no significant adverse events are reported."( A systematic review of catechol-0-methyltransferase inhibitors: efficacy and safety in clinical practice.
Ceravolo, R; Gioulis, M; Marsala, SZ; Tinazzi, M, )		0.13

Pharmacokinetics

ExcerptReferenceRelevance
"This study investigated the tolerability and the pharmacokinetic and pharmacodynamic interactions between single oral administration of BIA 3-202 (50 mg, 100 mg, 200 mg, and 400 mg), a novel catechol-O-methyltransferase (COMT) inhibitor, and standard carbidopa/levodopa 25 mg/100 mg (Sinemet 25/100) in healthy adult volunteers."( Pharmacokinetic-pharmacodynamic interaction between BIA 3-202, a novel COMT inhibitor, and levodopa/carbidopa.
Almeida, L; Falcão, A; Loureiro, A; Machado, R; Maia, J; Silveira, P; Soares-da-Silva, P; Torrão, L; Vaz-da-Silva, M; Wright, L, )		0.13
"The present study was designed to characterize pharmacodynamic and pharmacokinetic properties of nebicapone in rats and mice."( Species differences in pharmacokinetic and pharmacodynamic properties of nebicapone.
Bonifácio, MJ; Fernandes-Lopes, C; Loureiro, AI; Pinho, MJ; Soares-da-Silva, P; Torrão, L; Wright, L, 2009)		0.8
"0] kg/m2) completed the 4 treatment periods and had data available for pharmacokinetic and pharmacodynamic analyses."( Pharmacokinetic-pharmacodynamic interaction between nebicapone and controlled-release levodopa/benserazide: a single-center, Phase I, double-blind, randomized, placebo-controlled, four-way crossover study in healthy subjects.
Almeida, L; Costa, R; Falcão, A; Fernandes-Lopes, C; Loureiro, AI; Machado, R; Nunes, T; Rocha, JF; Soares-da-Silva, P; Torrão, L; Vaz-da-Silva, M; Wright, L, 2009)		0.6
" In longer terminal half-life phases low concentrations of BIA 3-270 predominate."( Pharmacokinetics, disposition, and metabolism of [14C]-nebicapone in humans.
Almeida, L; Loureiro, AI; Maia, J; Soares-Da-Silva, P; Wright, LC, 2010)		0.61

Bioavailability

ExcerptReferenceRelevance
" In conclusion, the novel COMT inhibitor BIA 3-202 was well tolerated and significantly increased the bioavailability of levodopa and reduced the formation of 3-OMD when administered with standard release levodopa/benserazide."( Pharmacokinetic-pharmacodynamic interaction between BIA 3-202, a novel COMT inhibitor, and levodopa/benserazide.
Almeida, L; Falcão, A; Loureiro, A; Machado, R; Maia, J; Silveira, P; Soares-da-Silva, P; Torrão, L; Vaz-da-Silva, M; Wright, L, 2003)		0.32
" In conclusion, the novel COMT inhibitor BIA 3-202 increased the bioavailability of levodopa and reduced the formation of 3-OMD when administered with standard levodopa/carbidopa."( Pharmacokinetic-pharmacodynamic interaction between BIA 3-202, a novel COMT inhibitor, and levodopa/carbidopa.
Almeida, L; Falcão, A; Loureiro, A; Machado, R; Maia, J; Silveira, P; Soares-da-Silva, P; Torrão, L; Vaz-da-Silva, M; Wright, L, )		0.13
" These results show that nebicapone exhibited marked species differences in bioavailability and metabolic profile."( Species differences in pharmacokinetic and pharmacodynamic properties of nebicapone.
Bonifácio, MJ; Fernandes-Lopes, C; Loureiro, AI; Pinho, MJ; Soares-da-Silva, P; Torrão, L; Wright, L, 2009)		0.89

Dosage Studied

ExcerptRelevanceReference
"Patients with Parkinson's disease can benefit from controlled released levodopa dosage forms since there is a clear clinical advantage in obtaining sustained plasma concentrations."( In-vivo evaluation of prolonged release bilayer tablets of anti-Parkinson drugs in Göttingen minipigs.
Bonifácio, MJ; Falcão, A; Lobo, JS; Machado, R; Soares-da-Silva, P; Sousa e Silva, JP, 2011)		0.37
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (2)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Catechol O-methyltransferaseRattus norvegicus (Norway rat)IC50 (µMol)0.69000.00222.81277.0795AID256793
Adenosine receptor A2aHomo sapiens (human)IC50 (µMol)0.69000.00071.559410.0000AID256793
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (50)

Processvia Protein(s)Taxonomy
synaptic transmission, dopaminergicAdenosine receptor A2aHomo sapiens (human)
response to amphetamineAdenosine receptor A2aHomo sapiens (human)
regulation of DNA-templated transcriptionAdenosine receptor A2aHomo sapiens (human)
phagocytosisAdenosine receptor A2aHomo sapiens (human)
apoptotic processAdenosine receptor A2aHomo sapiens (human)
inflammatory responseAdenosine receptor A2aHomo sapiens (human)
cellular defense responseAdenosine receptor A2aHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayAdenosine receptor A2aHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayAdenosine receptor A2aHomo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathwayAdenosine receptor A2aHomo sapiens (human)
cell-cell signalingAdenosine receptor A2aHomo sapiens (human)
synaptic transmission, cholinergicAdenosine receptor A2aHomo sapiens (human)
central nervous system developmentAdenosine receptor A2aHomo sapiens (human)
blood coagulationAdenosine receptor A2aHomo sapiens (human)
sensory perceptionAdenosine receptor A2aHomo sapiens (human)
locomotory behaviorAdenosine receptor A2aHomo sapiens (human)
blood circulationAdenosine receptor A2aHomo sapiens (human)
negative regulation of cell population proliferationAdenosine receptor A2aHomo sapiens (human)
response to xenobiotic stimulusAdenosine receptor A2aHomo sapiens (human)
response to inorganic substanceAdenosine receptor A2aHomo sapiens (human)
positive regulation of glutamate secretionAdenosine receptor A2aHomo sapiens (human)
positive regulation of acetylcholine secretion, neurotransmissionAdenosine receptor A2aHomo sapiens (human)
regulation of norepinephrine secretionAdenosine receptor A2aHomo sapiens (human)
response to purine-containing compoundAdenosine receptor A2aHomo sapiens (human)
response to caffeineAdenosine receptor A2aHomo sapiens (human)
positive regulation of synaptic transmission, GABAergicAdenosine receptor A2aHomo sapiens (human)
synaptic transmission, glutamatergicAdenosine receptor A2aHomo sapiens (human)
positive regulation of urine volumeAdenosine receptor A2aHomo sapiens (human)
vasodilationAdenosine receptor A2aHomo sapiens (human)
eating behaviorAdenosine receptor A2aHomo sapiens (human)
negative regulation of vascular permeabilityAdenosine receptor A2aHomo sapiens (human)
negative regulation of neuron apoptotic processAdenosine receptor A2aHomo sapiens (human)
positive regulation of circadian sleep/wake cycle, sleepAdenosine receptor A2aHomo sapiens (human)
negative regulation of alpha-beta T cell activationAdenosine receptor A2aHomo sapiens (human)
astrocyte activationAdenosine receptor A2aHomo sapiens (human)
neuron projection morphogenesisAdenosine receptor A2aHomo sapiens (human)
positive regulation of protein secretionAdenosine receptor A2aHomo sapiens (human)
negative regulation of inflammatory responseAdenosine receptor A2aHomo sapiens (human)
regulation of mitochondrial membrane potentialAdenosine receptor A2aHomo sapiens (human)
membrane depolarizationAdenosine receptor A2aHomo sapiens (human)
regulation of calcium ion transportAdenosine receptor A2aHomo sapiens (human)
positive regulation of synaptic transmission, glutamatergicAdenosine receptor A2aHomo sapiens (human)
excitatory postsynaptic potentialAdenosine receptor A2aHomo sapiens (human)
inhibitory postsynaptic potentialAdenosine receptor A2aHomo sapiens (human)
prepulse inhibitionAdenosine receptor A2aHomo sapiens (human)
apoptotic signaling pathwayAdenosine receptor A2aHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionAdenosine receptor A2aHomo sapiens (human)
positive regulation of long-term synaptic potentiationAdenosine receptor A2aHomo sapiens (human)
positive regulation of apoptotic signaling pathwayAdenosine receptor A2aHomo sapiens (human)
G protein-coupled adenosine receptor signaling pathwayAdenosine receptor A2aHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (9)

Processvia Protein(s)Taxonomy
G protein-coupled adenosine receptor activityAdenosine receptor A2aHomo sapiens (human)
protein bindingAdenosine receptor A2aHomo sapiens (human)
calmodulin bindingAdenosine receptor A2aHomo sapiens (human)
lipid bindingAdenosine receptor A2aHomo sapiens (human)
enzyme bindingAdenosine receptor A2aHomo sapiens (human)
type 5 metabotropic glutamate receptor bindingAdenosine receptor A2aHomo sapiens (human)
identical protein bindingAdenosine receptor A2aHomo sapiens (human)
protein-containing complex bindingAdenosine receptor A2aHomo sapiens (human)
alpha-actinin bindingAdenosine receptor A2aHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (11)

Processvia Protein(s)Taxonomy
plasma membraneAdenosine receptor A2aHomo sapiens (human)
intermediate filamentAdenosine receptor A2aHomo sapiens (human)
plasma membraneAdenosine receptor A2aHomo sapiens (human)
membraneAdenosine receptor A2aHomo sapiens (human)
dendriteAdenosine receptor A2aHomo sapiens (human)
axolemmaAdenosine receptor A2aHomo sapiens (human)
asymmetric synapseAdenosine receptor A2aHomo sapiens (human)
presynaptic membraneAdenosine receptor A2aHomo sapiens (human)
neuronal cell bodyAdenosine receptor A2aHomo sapiens (human)
postsynaptic membraneAdenosine receptor A2aHomo sapiens (human)
presynaptic active zoneAdenosine receptor A2aHomo sapiens (human)
glutamatergic synapseAdenosine receptor A2aHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (27)

Assay IDTitleYearJournalArticle
AID256800Percentage inhibitory activity against COMT for 1h in homogenates of rat liver administered with 30 mg/kg by Gastric tube2005Journal of medicinal chemistry, Dec-15, Volume: 48, Issue:25
Synthesis and biological evaluation of a novel series of "ortho-nitrated" inhibitors of catechol-O-methyltransferase.
AID50091Percent inhibition of Catechol O-methyltransferase activity in rat brain at dose of 30 mg/kg determined at 3 hr after its administration2002Journal of medicinal chemistry, Jan-31, Volume: 45, Issue:3
Synthesis of 1-(3,4-dihydroxy-5-nitrophenyl)-2-phenyl-ethanone and derivatives as potent and long-acting peripheral inhibitors of catechol-O-methyltransferase.
AID49923Inhibition of Catechol O-methyltransferase activity in rat liver2002Journal of medicinal chemistry, Jan-31, Volume: 45, Issue:3
Synthesis of 1-(3,4-dihydroxy-5-nitrophenyl)-2-phenyl-ethanone and derivatives as potent and long-acting peripheral inhibitors of catechol-O-methyltransferase.
AID473638Inhibition of COMT in NMRI mouse liver homogenates assessed as metanephrine formation at 30 mg/kg, po measured after 6 hrs relative to control2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Discovery of a long-acting, peripherally selective inhibitor of catechol-O-methyltransferase.
AID256792Percentage inhibitory activity against COMT at 100 nM in human neuroblastoma SK-N-SH cells2005Journal of medicinal chemistry, Dec-15, Volume: 48, Issue:25
Synthesis and biological evaluation of a novel series of "ortho-nitrated" inhibitors of catechol-O-methyltransferase.
AID50085Percent inhibition of Catechol O-methyltransferase activity in rat liver at dose of 30 mg/kg determined at 3 hr after its administration2002Journal of medicinal chemistry, Jan-31, Volume: 45, Issue:3
Synthesis of 1-(3,4-dihydroxy-5-nitrophenyl)-2-phenyl-ethanone and derivatives as potent and long-acting peripheral inhibitors of catechol-O-methyltransferase.
AID256794Inhibitory activity against COMT in rat brain2005Journal of medicinal chemistry, Dec-15, Volume: 48, Issue:25
Synthesis and biological evaluation of a novel series of "ortho-nitrated" inhibitors of catechol-O-methyltransferase.
AID50079Percent inhibition of Catechol O-methyltransferase activity in rat brain at dose of 30 mg/kg determined at 1 hr after its administration2002Journal of medicinal chemistry, Jan-31, Volume: 45, Issue:3
Synthesis of 1-(3,4-dihydroxy-5-nitrophenyl)-2-phenyl-ethanone and derivatives as potent and long-acting peripheral inhibitors of catechol-O-methyltransferase.
AID50084Percent inhibition of Catechol O-methyltransferase activity in rat liver at dose of 30 mg/kg determined at 1 hr after its administration2002Journal of medicinal chemistry, Jan-31, Volume: 45, Issue:3
Synthesis of 1-(3,4-dihydroxy-5-nitrophenyl)-2-phenyl-ethanone and derivatives as potent and long-acting peripheral inhibitors of catechol-O-methyltransferase.
AID50088Percent inhibition of Catechol O-methyltransferase activity in rat liver at dose of 30 mg/kg determined at 9 hr after its administration2002Journal of medicinal chemistry, Jan-31, Volume: 45, Issue:3
Synthesis of 1-(3,4-dihydroxy-5-nitrophenyl)-2-phenyl-ethanone and derivatives as potent and long-acting peripheral inhibitors of catechol-O-methyltransferase.
AID256796Percentage inhibitory activity against COMT for 1h in homogenates of rat brain administered with 30mg/kg by Gastric tube2005Journal of medicinal chemistry, Dec-15, Volume: 48, Issue:25
Synthesis and biological evaluation of a novel series of "ortho-nitrated" inhibitors of catechol-O-methyltransferase.
AID50093percent inhibition of Catechol O-methyltransferase activity in rat brain at dose of 30 mg/kg determined at 6 hr after its administration2002Journal of medicinal chemistry, Jan-31, Volume: 45, Issue:3
Synthesis of 1-(3,4-dihydroxy-5-nitrophenyl)-2-phenyl-ethanone and derivatives as potent and long-acting peripheral inhibitors of catechol-O-methyltransferase.
AID50082Percent inhibition of Catechol O-methyltransferase activity in rat brain at dose of 30 mg/kg determined at 9 hr after its administration2002Journal of medicinal chemistry, Jan-31, Volume: 45, Issue:3
Synthesis of 1-(3,4-dihydroxy-5-nitrophenyl)-2-phenyl-ethanone and derivatives as potent and long-acting peripheral inhibitors of catechol-O-methyltransferase.
AID256799Percentage inhibitory activity against COMT for 9h in homogenates of rat brain administered with 30 mg/kg by Gastric tube2005Journal of medicinal chemistry, Dec-15, Volume: 48, Issue:25
Synthesis and biological evaluation of a novel series of "ortho-nitrated" inhibitors of catechol-O-methyltransferase.
AID256803Percentage inhibitory activity against COMT for 3h in homogenates of rat liver administered with 30 mg/kg by Gastric tube2005Journal of medicinal chemistry, Dec-15, Volume: 48, Issue:25
Synthesis and biological evaluation of a novel series of "ortho-nitrated" inhibitors of catechol-O-methyltransferase.
AID256798Percentage inhibitory activity against COMT for 6h in homogenates of rat brain administered with 30 mg/kg by Gastric tube2005Journal of medicinal chemistry, Dec-15, Volume: 48, Issue:25
Synthesis and biological evaluation of a novel series of "ortho-nitrated" inhibitors of catechol-O-methyltransferase.
AID256795Percentage inhibitory activity against COMT for 0.5h in homogenates of rat brain administered with 30mg/kg by Gastric tube2005Journal of medicinal chemistry, Dec-15, Volume: 48, Issue:25
Synthesis and biological evaluation of a novel series of "ortho-nitrated" inhibitors of catechol-O-methyltransferase.
AID49922Inhibition of Catechol O-methyltransferase activity in rat brain2002Journal of medicinal chemistry, Jan-31, Volume: 45, Issue:3
Synthesis of 1-(3,4-dihydroxy-5-nitrophenyl)-2-phenyl-ethanone and derivatives as potent and long-acting peripheral inhibitors of catechol-O-methyltransferase.
AID49912Inhibition of Catechol O-methyltransferase activity in SK-N-SH cells at a concentration of 100 nM2002Journal of medicinal chemistry, Jan-31, Volume: 45, Issue:3
Synthesis of 1-(3,4-dihydroxy-5-nitrophenyl)-2-phenyl-ethanone and derivatives as potent and long-acting peripheral inhibitors of catechol-O-methyltransferase.
AID50083Percent inhibition of Catechol O-methyltransferase activity in rat liver at dose of 30 mg/kg determined at 0.5 hr after its administration2002Journal of medicinal chemistry, Jan-31, Volume: 45, Issue:3
Synthesis of 1-(3,4-dihydroxy-5-nitrophenyl)-2-phenyl-ethanone and derivatives as potent and long-acting peripheral inhibitors of catechol-O-methyltransferase.
AID256801Percentage inhibitory activity against COMT for 6h in homogenates of rat liver administered with 30 mg/kg by Gastric tube2005Journal of medicinal chemistry, Dec-15, Volume: 48, Issue:25
Synthesis and biological evaluation of a novel series of "ortho-nitrated" inhibitors of catechol-O-methyltransferase.
AID256797Percentage inhibitory activity against COMT for 3h in homogenates of rat brain administered with 30mg/kg by Gastric tube2005Journal of medicinal chemistry, Dec-15, Volume: 48, Issue:25
Synthesis and biological evaluation of a novel series of "ortho-nitrated" inhibitors of catechol-O-methyltransferase.
AID256804Percentage inhibitory activity against COMT for 9h in homogenates of rat liver administered with 30mg/kg by Gastric tube2005Journal of medicinal chemistry, Dec-15, Volume: 48, Issue:25
Synthesis and biological evaluation of a novel series of "ortho-nitrated" inhibitors of catechol-O-methyltransferase.
AID256802Percentage inhibitory activity against COMT for 0.5h in homogenates of rat liver administered with 30mg/kg by Gastric tube2005Journal of medicinal chemistry, Dec-15, Volume: 48, Issue:25
Synthesis and biological evaluation of a novel series of "ortho-nitrated" inhibitors of catechol-O-methyltransferase.
AID256793Inhibitory activity against COMT in rat liver2005Journal of medicinal chemistry, Dec-15, Volume: 48, Issue:25
Synthesis and biological evaluation of a novel series of "ortho-nitrated" inhibitors of catechol-O-methyltransferase.
AID50086Percent inhibition of Catechol O-methyltransferase activity in rat liver at dose of 30 mg/kg determined at 6 hr after its administration2002Journal of medicinal chemistry, Jan-31, Volume: 45, Issue:3
Synthesis of 1-(3,4-dihydroxy-5-nitrophenyl)-2-phenyl-ethanone and derivatives as potent and long-acting peripheral inhibitors of catechol-O-methyltransferase.
AID50078Percent inhibition of Catechol O-methyltransferase activity in rat brain at dose of 30 mg/kg determined at 0.5 hr after its administration2002Journal of medicinal chemistry, Jan-31, Volume: 45, Issue:3
Synthesis of 1-(3,4-dihydroxy-5-nitrophenyl)-2-phenyl-ethanone and derivatives as potent and long-acting peripheral inhibitors of catechol-O-methyltransferase.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (20)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's14 (70.00)29.6817
2010's6 (30.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 18.30

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index18.30 (24.57)
Research Supply Index3.58 (2.92)
Research Growth Index4.25 (4.65)
Search Engine Demand Index15.26 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (18.30)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials11 (45.83%)5.53%
Reviews1 (4.17%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other12 (50.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
catechol
[no description available]		2.0110catecholsallelochemical;
genotoxin;
plant metabolite
3,4-dihydroxyphenylacetic acid
3,4-Dihydroxyphenylacetic Acid: A deaminated metabolite of LEVODOPA.. (3,4-dihydroxyphenyl)acetic acid : A dihydroxyphenylacetic acid having the two hydroxy substituents located at the 3- and 4-positions. It is a metabolite of dopamine.. dihydroxyphenylacetic acid : A dihydroxy monocarboxylic acid consisting of phenylacetic acid having two phenolic hydroxy substituents.		210catechols;
dihydroxyphenylacetic acid		human metabolite
dihydroxyphenylalanine
Dihydroxyphenylalanine: A beta-hydroxylated derivative of phenylalanine. The D-form of dihydroxyphenylalanine has less physiologic activity than the L-form and is commonly used experimentally to determine whether the pharmacological effects of LEVODOPA are stereospecific.. dopa : A hydroxyphenylalanine carrying hydroxy substituents at positions 3 and 4 of the benzene ring.		4.0931hydroxyphenylalanine;
non-proteinogenic alpha-amino acid;
tyrosine derivative		human metabolite
3-methoxytyrosine
[no description available]		5.2443tyrosine derivative
homovanillic acid
Homovanillic Acid: A 3-O-methyl ETHER of (3,4-dihydroxyphenyl)acetic acid.. homovanillate : A hydroxy monocarboxylic acid anion which is obtained by deprotonation of the carboxy group of homovanillic acid.. homovanillic acid : A monocarboxylic acid that is the 3-O-methyl ether of (3,4-dihydroxyphenyl)acetic acid. It is a catecholamine metabolite.		210guaiacols;
monocarboxylic acid		human metabolite;
mouse metabolite
benserazide
Benserazide: 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.. benserazide : A carbohydrazide that results from the formal condensation of the carboxy group of DL-serine with the primary amino group of 4-(hydrazinylmethyl)benzene-1,2,3-triol. An aromatic-L-amino-acid decarboxylase inhibitor (DOPA decarboxylase inhibitor) that does not enter the central nervous system, it is used as its hydrochloride salt as an adjunct to levodopa in the treatment of parkinsonism. By preventing the conversion of levodopa to dopamine in the periphery, it causes an increase in the amount of levodopa reaching the central nervous system and so reduces the required dose. Benserazide has no antiparkinson actions when given alone.		10.2543carbohydrazide;
catechols;
primary alcohol;
primary amino compound		antiparkinson drug;
dopaminergic agent;
EC 4.1.1.28 (aromatic-L-amino-acid decarboxylase) inhibitor
levodopa
Levodopa: The naturally occurring form of DIHYDROXYPHENYLALANINE and the immediate precursor of DOPAMINE. Unlike dopamine itself, it can be taken orally and crosses the blood-brain barrier. It is rapidly taken up by dopaminergic neurons and converted to DOPAMINE. It is used for the treatment of PARKINSONIAN DISORDERS and is usually given with agents that inhibit its conversion to dopamine outside of the central nervous system.. L-dopa : An optically active form of dopa having L-configuration. Used to treat the stiffness, tremors, spasms, and poor muscle control of Parkinson's disease		6.2194amino acid zwitterion;
dopa;
L-tyrosine derivative;
non-proteinogenic L-alpha-amino acid		allelochemical;
antidyskinesia agent;
antiparkinson drug;
dopaminergic agent;
hapten;
human metabolite;
mouse metabolite;
neurotoxin;
plant growth retardant;
plant metabolite;
prodrug
tyrosine
Tyrosine: A non-essential amino acid. In animals it is synthesized from PHENYLALANINE. It is also the precursor of EPINEPHRINE; THYROID HORMONES; and melanin.. tyrosine : An alpha-amino acid that is phenylalanine bearing a hydroxy substituent at position 4 on the phenyl ring.		5.2443amino acid zwitterion;
erythrose 4-phosphate/phosphoenolpyruvate family amino acid;
L-alpha-amino acid;
proteinogenic amino acid;
tyrosine		EC 1.3.1.43 (arogenate dehydrogenase) inhibitor;
fundamental metabolite;
micronutrient;
nutraceutical
methyldopa
Methyldopa: An alpha-2 adrenergic agonist that has both central and peripheral nervous system effects. Its primary clinical use is as an antihypertensive agent.. alpha-methyl-L-dopa : A derivative of L-tyrosine having a methyl group at the alpha-position and an additional hydroxy group at the 3-position on the phenyl ring.		2.0110L-tyrosine derivative;
non-proteinogenic L-alpha-amino acid		alpha-adrenergic agonist;
antihypertensive agent;
hapten;
peripheral nervous system drug;
sympatholytic agent
tolcapone
Tolcapone: A benzophenone and nitrophenol compound that acts as an inhibitor of CATECHOL O-METHYLTRANSFERASE, an enzyme involved in the metabolism of DOPAMINE and LEVODOPA. It is used in the treatment of PARKINSON DISEASE in patients for whom levodopa is ineffective or contraindicated.. tolcapone : Benzophenone substituted on one of the phenyl rings at C-3 and C-4 by hydroxy groups and at C-5 by a nitro group, and on the other phenyl ring by a methyl group at C-4. It is an inhibitor of catechol O-methyltransferase.		2.72302-nitrophenols;
benzophenones;
catechols		antiparkinson drug;
EC 2.1.1.6 (catechol O-methyltransferase) inhibitor
entacapone
entacapone: structure given in first source. entacapone : A monocarboxylic acid amide that is N,N-diethylprop-2-enamide in which the hydrogen at position 2 is substituted by a cyano group and the hydrogen at the 3E position is substituted by a 3,4-dihydroxy-5-nitrophenyl group.		4.53512-nitrophenols;
catechols;
monocarboxylic acid amide;
nitrile		antidyskinesia agent;
antiparkinson drug;
central nervous system drug;
EC 2.1.1.6 (catechol O-methyltransferase) inhibitor
oxadiazoles
Oxadiazoles: Compounds containing five-membered heteroaromatic rings containing two carbons, two nitrogens, and one oxygen atom which exist in various regioisomeric forms.		2.110
s-adenosylmethionine
(R)-S-adenosyl-L-methionine : An S-adenosyl-L-methionine that has R-configuration.. S-adenosyl-L-methionine zwitterion : A zwitterionic tautomer of S-adenosyl-L-methionine arising from shift of the proton from the carboxy group to the amino group.. (R)-S-adenosyl-L-methionine zwitterion : An S-adenosyl-L-methionine zwitterion that has R-configuration; major species at pH 7.3.. (S)-S-adenosyl-L-methionine zwitterion : An S-adenosyl-L-methionine zwitterion that has S-configuration; major species at pH 7.3.. S-adenosyl-L-methionine : A sulfonium compound that is the S-adenosyl derivative of L-methionine. It is an intermediate in the metabolic pathway of methionine.		2.0110organic cation;
sulfonium compound		coenzyme;
cofactor;
human metabolite;
micronutrient;
Mycoplasma genitalium metabolite;
nutraceutical;
Saccharomyces cerevisiae metabolite
opicapone
opicapone: structure in first source		2.4820oxadiazole;
ring assembly
carbidopa
Carbidopa: An inhibitor of DOPA DECARBOXYLASE that prevents conversion of LEVODOPA to dopamine. It is used in PARKINSON DISEASE to reduce peripheral adverse effects of LEVODOPA. It has no anti-parkinson activity by itself.. carbidopa : The hydrate of 3-(3,4-dihydroxyphenyl)propanoic acid in which the hydrogens alpha- to the carboxyl group are substituted by hydrazinyl and methyl groups (S-configuration). Carbidopa is a dopa decarboxylase inhibitor, so prevents conversion of levodopa to dopamine. It has no antiparkinson activity by itself, but is used in the management of Parkinson's disease to reduce peripheral adverse effects of levodopa.		9.6932
ConditionIndicatedRelationship StrengthStudiesTrials
Idiopathic Parkinson Disease
[description not available]		03.8621
Parkinson Disease
A progressive, degenerative neurologic disease characterized by a TREMOR that is maximal at rest, retropulsion (i.e. a tendency to fall backwards), rigidity, stooped posture, slowness of voluntary movements, and a masklike facial expression. Pathologic features include loss of melanin containing neurons in the substantia nigra and other pigmented nuclei of the brainstem. LEWY BODIES are present in the substantia nigra and locus coeruleus but may also be found in a related condition (LEWY BODY DISEASE, DIFFUSE) characterized by dementia in combination with varying degrees of parkinsonism. (Adams et al., Principles of Neurology, 6th ed, p1059, pp1067-75)		15.8621