Page last updated: 2024-09-25

rasagiline

Cross-References

ID SourceID
PubMed CID3052776
CHEMBL ID887
CHEBI ID63620
SCHEMBL ID74699
SCHEMBL ID2029054
MeSH IDM0100095

Synonyms (73)

Synonym
AC-723
unii-003n66ts6t
hsdb 7699
003n66ts6t ,
nsc 759639
tv 1030
rasagiline [usan:inn]
AKOS015837675
tv-1030
RAS ,
rasagiline ,
chembl887 ,
bdbm10989
(1r)-n-(prop-2-yn-1-yl)-2,3-dihydro-1h-inden-1-amine
DB01367
(r)-n-2-propynyl-1-indanamine
(r)-indan-1-yl-prop-2-ynyl-amine
(1r)-n-propargylindan-1-amine
1-indanamine, n-2-propynyl-, (r)-
1h-inden-1-amine, 2,3-dihydro-n-2-propynyl-, (1r)
rasagiline [inn]
136236-51-6
nsc-759639
chebi:63620 ,
D08469
rasagiline (usan/inn)
(1r)-n-prop-2-ynyl-2,3-dihydro-1h-inden-1-amine
A2916
(r)-n-(prop-2-ynyl)-2,3-dihydro-1h-inden-1-amine;(r)-n-(2-propynyl)-2,3-dihydroinden-1-amine
HMS3264K12
AKOS006271452
(r)-2,3-dihydro-n-2-propynyl-1h-inden-1-amine
nsc759639
pharmakon1600-01502333
(r)-n-(2-propynyl)-2,3-dihydroinden-1-amine
FS-3130
(1r)-n-(prop-2-yn-1-yl)indan-1-amine
rasagiline [hsdb]
rasagiline [who-dd]
1h-inden-1-amine, 2,3-dihydro-n-2-propyn-1-yl-, (1r)-
(r)-(+)-rasagiline
rasagiline [mi]
rasagiline [vandf]
(1r)-2,3-dihydro-n-2-propyn-1-yl-1h-inden-1-amine
rasagiline [usan]
rasagiline [ema epar]
1h-inden-1-amine, 2,3-dihydro-n-2-propynyl-, (1r)-
rasagiline [orange book]
1h-inden-1-amine, 2,3-dihydro-n-2-propynyl-, (r)-
AM84542
S5795
gtpl6641
CCG-213034
HY-14605A
SCHEMBL74699
smr002533187
MLS006012042
RUOKEQAAGRXIBM-GFCCVEGCSA-N
n-propargyl-1-(r)aminoindan
SCHEMBL2029054
AB01562963_01
AB01562963_02
DTXSID3041112
sr-00000006359
SR-00000006359-3
HMS3715L12
(r)-n-(prop-2-ynyl)-2,3-dihydro-1h-inden-1-amine
Q420685
1204184-69-9
EN300-150047
HMS3886N03
nsc-789038
nsc789038

Roles (2)

RoleDescription
EC 1.4.3.4 (monoamine oxidase) inhibitorAn EC 1.4.3.* (oxidoreductase acting on donor CH-NH2 group, oxygen as acceptor) inhibitor that interferes with the action of monoamine oxidase (EC 1.4.3.4).
neuroprotective agentAny compound that can be used for the treatment of neurodegenerative disorders.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (3)

ClassDescription
secondary amineA compound formally derived from ammonia by replacing two hydrogen atoms by hydrocarbyl groups.
indanes
terminal acetylenic compoundAn acetylenic compound which a carbon of the C#C moiety is attached to a hydrogen atom.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (9)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
CholinesteraseHomo sapiens (human)IC50 (µMol)2.38650.00001.559910.0000AID1465285; AID1556701
Amine oxidase [flavin-containing] BRattus norvegicus (Norway rat)IC50 (µMol)3.34220.00040.764912.5000AID1199581; AID1399984; AID1586574; AID1600694
Amine oxidase [flavin-containing] BRattus norvegicus (Norway rat)Ki0.17390.00081.09276.0000AID1192621; AID1192622; AID1796581
Amine oxidase [flavin-containing] A Rattus norvegicus (Norway rat)IC50 (µMol)133.91430.00071.979812.5000AID1199580; AID1399983; AID1586572
Amine oxidase [flavin-containing] A Rattus norvegicus (Norway rat)Ki0.01420.00190.55334.8000AID1192621
Amine oxidase [flavin-containing] AHomo sapiens (human)IC50 (µMol)64.85320.00002.37899.7700AID125558; AID1292320; AID1323962; AID1334743; AID1336724; AID1352195; AID1374197; AID1390035; AID1421879; AID1427512; AID1436076; AID1437168; AID1444065; AID1453105; AID1458405; AID1465287; AID1465302; AID1485915; AID1517859; AID1519692; AID1528913; AID1551696; AID1556700; AID1557173; AID1568798; AID1569980; AID1586573; AID1635482; AID1657150; AID1667262; AID1691660; AID1706696; AID1709260; AID1751716; AID1757198; AID1761631; AID1802599; AID1851411; AID314094; AID706469; AID743813
Amine oxidase [flavin-containing] AHomo sapiens (human)Ki5.16670.00192.379710.0000AID125561; AID1796578; AID1796579; AID1796581
AcetylcholinesteraseHomo sapiens (human)IC50 (µMol)0.01900.00000.933210.0000AID1465284
Amine oxidase [flavin-containing] BHomo sapiens (human)IC50 (µMol)3.93120.00001.89149.5700AID126541; AID1292322; AID1323961; AID1334745; AID1336725; AID1352196; AID1374198; AID1390036; AID1421880; AID1427513; AID1436077; AID1437169; AID1444066; AID1453106; AID1456237; AID1458404; AID1465288; AID1465303; AID1485916; AID1517860; AID1519691; AID1528914; AID1532335; AID1532341; AID1551697; AID1556701; AID1557174; AID1568796; AID1569982; AID1586575; AID1635461; AID1639030; AID1657151; AID1667263; AID1691662; AID1704813; AID1705912; AID1706697; AID1709261; AID1740536; AID1751717; AID1754140; AID1754141; AID1757197; AID1761632; AID1802599; AID1851412; AID1872726; AID1907519; AID314095; AID658202; AID706470; AID743812; AID779070
Amine oxidase [flavin-containing] BHomo sapiens (human)Ki2.52460.00061.777110.0000AID1192621; AID1192622; AID126542; AID1796578; AID1796579; AID1796581; AID254307
5-hydroxytryptamine receptor 6Homo sapiens (human)Ki0.00140.00020.522910.0000AID1705911
Amine oxidase [flavin-containing] BBos taurus (cattle)Ki0.50000.05401.83906.0000AID1796581
Amine oxidase [flavin-containing] BMus musculus (house mouse)Ki0.50000.10002.37906.0000AID1796581
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (46)

Processvia Protein(s)Taxonomy
xenobiotic metabolic processCholinesteraseHomo sapiens (human)
learningCholinesteraseHomo sapiens (human)
negative regulation of cell population proliferationCholinesteraseHomo sapiens (human)
neuroblast differentiationCholinesteraseHomo sapiens (human)
peptide hormone processingCholinesteraseHomo sapiens (human)
response to alkaloidCholinesteraseHomo sapiens (human)
cocaine metabolic processCholinesteraseHomo sapiens (human)
negative regulation of synaptic transmissionCholinesteraseHomo sapiens (human)
response to glucocorticoidCholinesteraseHomo sapiens (human)
response to folic acidCholinesteraseHomo sapiens (human)
choline metabolic processCholinesteraseHomo sapiens (human)
acetylcholine catabolic processCholinesteraseHomo sapiens (human)
biogenic amine metabolic processAmine oxidase [flavin-containing] AHomo sapiens (human)
positive regulation of signal transductionAmine oxidase [flavin-containing] AHomo sapiens (human)
dopamine catabolic processAmine oxidase [flavin-containing] AHomo sapiens (human)
acetylcholine catabolic process in synaptic cleftAcetylcholinesteraseHomo sapiens (human)
regulation of receptor recyclingAcetylcholinesteraseHomo sapiens (human)
osteoblast developmentAcetylcholinesteraseHomo sapiens (human)
acetylcholine catabolic processAcetylcholinesteraseHomo sapiens (human)
cell adhesionAcetylcholinesteraseHomo sapiens (human)
nervous system developmentAcetylcholinesteraseHomo sapiens (human)
synapse assemblyAcetylcholinesteraseHomo sapiens (human)
receptor internalizationAcetylcholinesteraseHomo sapiens (human)
negative regulation of synaptic transmission, cholinergicAcetylcholinesteraseHomo sapiens (human)
amyloid precursor protein metabolic processAcetylcholinesteraseHomo sapiens (human)
positive regulation of protein secretionAcetylcholinesteraseHomo sapiens (human)
retina development in camera-type eyeAcetylcholinesteraseHomo sapiens (human)
acetylcholine receptor signaling pathwayAcetylcholinesteraseHomo sapiens (human)
positive regulation of cold-induced thermogenesisAcetylcholinesteraseHomo sapiens (human)
response to xenobiotic stimulusAmine oxidase [flavin-containing] BHomo sapiens (human)
response to toxic substanceAmine oxidase [flavin-containing] BHomo sapiens (human)
response to aluminum ionAmine oxidase [flavin-containing] BHomo sapiens (human)
response to selenium ionAmine oxidase [flavin-containing] BHomo sapiens (human)
negative regulation of serotonin secretionAmine oxidase [flavin-containing] BHomo sapiens (human)
phenylethylamine catabolic processAmine oxidase [flavin-containing] BHomo sapiens (human)
substantia nigra developmentAmine oxidase [flavin-containing] BHomo sapiens (human)
response to lipopolysaccharideAmine oxidase [flavin-containing] BHomo sapiens (human)
dopamine catabolic processAmine oxidase [flavin-containing] BHomo sapiens (human)
response to ethanolAmine oxidase [flavin-containing] BHomo sapiens (human)
positive regulation of dopamine metabolic processAmine oxidase [flavin-containing] BHomo sapiens (human)
hydrogen peroxide biosynthetic processAmine oxidase [flavin-containing] BHomo sapiens (human)
response to corticosteroneAmine oxidase [flavin-containing] BHomo sapiens (human)
cerebral cortex cell migration5-hydroxytryptamine receptor 6Homo sapiens (human)
positive regulation of TOR signaling5-hydroxytryptamine receptor 6Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 6Homo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 6Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 6Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 6Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (23)

Processvia Protein(s)Taxonomy
amyloid-beta bindingCholinesteraseHomo sapiens (human)
catalytic activityCholinesteraseHomo sapiens (human)
acetylcholinesterase activityCholinesteraseHomo sapiens (human)
cholinesterase activityCholinesteraseHomo sapiens (human)
protein bindingCholinesteraseHomo sapiens (human)
hydrolase activity, acting on ester bondsCholinesteraseHomo sapiens (human)
enzyme bindingCholinesteraseHomo sapiens (human)
choline bindingCholinesteraseHomo sapiens (human)
identical protein bindingCholinesteraseHomo sapiens (human)
protein bindingAmine oxidase [flavin-containing] AHomo sapiens (human)
primary amine oxidase activityAmine oxidase [flavin-containing] AHomo sapiens (human)
aliphatic amine oxidase activityAmine oxidase [flavin-containing] AHomo sapiens (human)
monoamine oxidase activityAmine oxidase [flavin-containing] AHomo sapiens (human)
flavin adenine dinucleotide bindingAmine oxidase [flavin-containing] AHomo sapiens (human)
amyloid-beta bindingAcetylcholinesteraseHomo sapiens (human)
acetylcholinesterase activityAcetylcholinesteraseHomo sapiens (human)
cholinesterase activityAcetylcholinesteraseHomo sapiens (human)
protein bindingAcetylcholinesteraseHomo sapiens (human)
collagen bindingAcetylcholinesteraseHomo sapiens (human)
hydrolase activityAcetylcholinesteraseHomo sapiens (human)
serine hydrolase activityAcetylcholinesteraseHomo sapiens (human)
acetylcholine bindingAcetylcholinesteraseHomo sapiens (human)
protein homodimerization activityAcetylcholinesteraseHomo sapiens (human)
laminin bindingAcetylcholinesteraseHomo sapiens (human)
protein bindingAmine oxidase [flavin-containing] BHomo sapiens (human)
primary amine oxidase activityAmine oxidase [flavin-containing] BHomo sapiens (human)
electron transfer activityAmine oxidase [flavin-containing] BHomo sapiens (human)
identical protein bindingAmine oxidase [flavin-containing] BHomo sapiens (human)
aliphatic amine oxidase activityAmine oxidase [flavin-containing] BHomo sapiens (human)
monoamine oxidase activityAmine oxidase [flavin-containing] BHomo sapiens (human)
flavin adenine dinucleotide bindingAmine oxidase [flavin-containing] BHomo sapiens (human)
histamine receptor activity5-hydroxytryptamine receptor 6Homo sapiens (human)
protein binding5-hydroxytryptamine receptor 6Homo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 6Homo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 6Homo sapiens (human)
primary amine oxidase activityAmine oxidase [flavin-containing] BBos taurus (cattle)
aliphatic amine oxidase activityAmine oxidase [flavin-containing] BBos taurus (cattle)
monoamine oxidase activityAmine oxidase [flavin-containing] BBos taurus (cattle)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (23)

Processvia Protein(s)Taxonomy
extracellular regionCholinesteraseHomo sapiens (human)
nuclear envelope lumenCholinesteraseHomo sapiens (human)
endoplasmic reticulum lumenCholinesteraseHomo sapiens (human)
blood microparticleCholinesteraseHomo sapiens (human)
plasma membraneCholinesteraseHomo sapiens (human)
extracellular spaceCholinesteraseHomo sapiens (human)
mitochondrionAmine oxidase [flavin-containing] AHomo sapiens (human)
mitochondrial outer membraneAmine oxidase [flavin-containing] AHomo sapiens (human)
cytosolAmine oxidase [flavin-containing] AHomo sapiens (human)
mitochondrionAmine oxidase [flavin-containing] AHomo sapiens (human)
extracellular regionAcetylcholinesteraseHomo sapiens (human)
basement membraneAcetylcholinesteraseHomo sapiens (human)
extracellular spaceAcetylcholinesteraseHomo sapiens (human)
nucleusAcetylcholinesteraseHomo sapiens (human)
Golgi apparatusAcetylcholinesteraseHomo sapiens (human)
plasma membraneAcetylcholinesteraseHomo sapiens (human)
cell surfaceAcetylcholinesteraseHomo sapiens (human)
membraneAcetylcholinesteraseHomo sapiens (human)
neuromuscular junctionAcetylcholinesteraseHomo sapiens (human)
synaptic cleftAcetylcholinesteraseHomo sapiens (human)
synapseAcetylcholinesteraseHomo sapiens (human)
perinuclear region of cytoplasmAcetylcholinesteraseHomo sapiens (human)
side of membraneAcetylcholinesteraseHomo sapiens (human)
mitochondrionAmine oxidase [flavin-containing] BHomo sapiens (human)
mitochondrial envelopeAmine oxidase [flavin-containing] BHomo sapiens (human)
mitochondrial outer membraneAmine oxidase [flavin-containing] BHomo sapiens (human)
dendriteAmine oxidase [flavin-containing] BHomo sapiens (human)
neuronal cell bodyAmine oxidase [flavin-containing] BHomo sapiens (human)
mitochondrionAmine oxidase [flavin-containing] BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 6Homo sapiens (human)
cilium5-hydroxytryptamine receptor 6Homo sapiens (human)
synapse5-hydroxytryptamine receptor 6Homo sapiens (human)
dendrite5-hydroxytryptamine receptor 6Homo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 6Homo sapiens (human)
mitochondrionAmine oxidase [flavin-containing] BBos taurus (cattle)
mitochondrial outer membraneAmine oxidase [flavin-containing] BBos taurus (cattle)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (243)

Assay IDTitleYearJournalArticle
AID1796579MAO A and MAO B Activity Measurements from Article 10.1021/jm0310885: \\Inactivation of purified human recombinant monoamine oxidases A and B by rasagiline and its analogues.\\2004Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7
Inactivation of purified human recombinant monoamine oxidases A and B by rasagiline and its analogues.
AID1796578MAO A and MAO B Activity Measurements from Article 10.1021/jm0506266: \\Binding of rasagiline-related inhibitors to human monoamine oxidases: a kinetic and crystallographic analysis.\\2005Journal of medicinal chemistry, Dec-29, Volume: 48, Issue:26
Binding of rasagiline-related inhibitors to human monoamine oxidases: a kinetic and crystallographic analysis.
AID1802599MAO-A/MAO-B Inhibition Assay from Article 10.1016/j.bioorg.2017.02.016: \\Pyridoxine-resveratrol hybrids Mannich base derivatives as novel dual inhibitors of AChE and MAO-B with antioxidant and metal-chelating properties for the treatment of Alzheimer'2017Bioorganic chemistry, 04, Volume: 71Pyridoxine-resveratrol hybrids Mannich base derivatives as novel dual inhibitors of AChE and MAO-B with antioxidant and metal-chelating properties for the treatment of Alzheimer's disease.
AID1796581MAO Inhibition Assay from Article 10.1074/jbc.M500949200: \\Demonstration of isoleucine 199 as a structural determinant for the selective inhibition of human monoamine oxidase B by specific reversible inhibitors.\\2005The Journal of biological chemistry, Apr-22, Volume: 280, Issue:16
Demonstration of isoleucine 199 as a structural determinant for the selective inhibition of human monoamine oxidase B by specific reversible inhibitors.
AID1336724Inhibition of recombinant human MAO-A expressed in baculovirus infected High 5 insect cells using kynuramine as substrate incubated for 30 mins by spectrofluorometric method2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Design, synthesis and biological evaluation of 4'-aminochalcone-rivastigmine hybrids as multifunctional agents for the treatment of Alzheimer's disease.
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID126541Inhibitory concentration towards in human monoamine oxidase B was measured2004Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7
Inactivation of purified human recombinant monoamine oxidases A and B by rasagiline and its analogues.
AID1437169Inhibition of recombinant human MAO-B using kynuramine as substrate after 30 mins by fluorescence assay2017Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4
DL-3-n-butylphthalide-Edaravone hybrids as novel dual inhibitors of amyloid-β aggregation and monoamine oxidases with high antioxidant potency for Alzheimer's therapy.
AID232415Ratio of inactive monoamine oxidase A between kinact and Ki2004Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7
Inactivation of purified human recombinant monoamine oxidases A and B by rasagiline and its analogues.
AID1568798Inhibition of recombinant human MAO-A expressed in baculovirus infected BTI insect cells using kynuramine as substrate measured after 30 mins by fluorescence based assay2019European journal of medicinal chemistry, Sep-15, Volume: 178Design, synthesis, in-silico and biological evaluation of novel chalcone-O-carbamate derivatives as multifunctional agents for the treatment of Alzheimer's disease.
AID232324Ratio of A450 decay monoamine oxidase A between kinact and Ki2004Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7
Inactivation of purified human recombinant monoamine oxidases A and B by rasagiline and its analogues.
AID1751722Time dependent inhibition of recombinant human MAO-B expressed in baculovirus infected BTI-TN- 5B1-4 insect cells assessed as decay in enzyme residual activity at IC80 measured after 30 mins2021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
Mapping Chromone-3-Phenylcarboxamide Pharmacophore:
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1199587Neuroprotective activity against rotenone-treated rat PC12 cells assessed as survival at 10 uM after 4 hrs by MTT assay (Rvb = 100 +/- 1.88%)2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Novel arylalkenylpropargylamines as neuroprotective, potent, and selective monoamine oxidase B inhibitors for the treatment of Parkinson's disease.
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1754150Neuroprotective activity against MPTP-induced C57BL/6J mouse model of Parkinson's disease assessed as decrease in immobility time at 0.2 mg/kg, ip pretreated for 7 consecutive days followed by MPTP challenge and further treated with compound until day 14 2021Bioorganic & medicinal chemistry letters, 07-01, Volume: 43Novel 1-(prop-2-yn-1-ylamino)-2,3-dihydro-1H-indene-4-thiol derivatives as potent selective human monoamine oxidase B inhibitors: Design, SAR development, and biological evaluation.
AID1556700Inhibition of human recombinant MAO-A expressed in baculovirus infected BTI-TN-5B1-4 insect cells assessed as decrease in H2O2 production using p-tyramine as substrate incubated for 20 mins by horse-radish peroxidase/amplex red-based fluorescence method2019European journal of medicinal chemistry, Oct-01, Volume: 179Carboxamides vs. methanimines: Crystal structures, binding interactions, photophysical studies, and biological evaluation of (indazole-5-yl)methanimines as monoamine oxidase B and acetylcholinesterase inhibitors.
AID1691660Inhibition of recombinant human MAO-A2020European journal of medicinal chemistry, May-15, Volume: 194Design, synthesis and biological evaluation of novel O-carbamoyl ferulamide derivatives as multi-target-directed ligands for the treatment of Alzheimer's disease.
AID1519684Irreversible inhibition of human microsomal MAO-B expressed in baculovirus infected BTI-TN-5B1-4 cells assessed as decay in enzyme residual activity continuously by measuring 4-hydroxyquinoline formation using kynuramine as substrate measured after first 2020European journal of medicinal chemistry, Jan-01, Volume: 185Design of novel monoamine oxidase-B inhibitors based on piperine scaffold: Structure-activity-toxicity, drug-likeness and efflux transport studies.
AID1528915Selectivity ratio of IC50 for recombinant human microsomal MAOA expressed in baculovirus infected BTI insect cells to IC50 for recombinant human microsomal MAOB expressed in baculovirus infected BTI insect cells
AID1458404Inhibition of human recombinant microsomal MAOB expressed in baculovirus infected BTI-TN-5B1- 4 cells using p-tyramine as substrate assessed as decrease in H2O2 production after 15 mins by amplex red-based fluorescence assay2017Journal of medicinal chemistry, 08-24, Volume: 60, Issue:16
Coumarin versus Chromone Monoamine Oxidase B Inhibitors: Quo Vadis?
AID1399984Inhibition of rat MAOB using benzylamine as substrate pretreated for 1200 secs followed by substrate addition and measured after 3600 secs2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
Design, synthesis and biological evaluation of lazabemide derivatives as inhibitors of monoamine oxidase.
AID1437173Antioxidant activity assessed as trolox equivalent of AAPH radical scavenging activity at 1 uM preincubated for 15 mins followed by AAPH addition measured every min for 90 mins by ORAC-FL assay2017Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4
DL-3-n-butylphthalide-Edaravone hybrids as novel dual inhibitors of amyloid-β aggregation and monoamine oxidases with high antioxidant potency for Alzheimer's therapy.
AID1600694Inhibition of rat brain MAO-B using [14C]-phenylethylamine as substrate preincubated for 60 mins followed by substrate addition and measured after 20 mins by liquid scintillation counting method2019Bioorganic & medicinal chemistry letters, 10-01, Volume: 29, Issue:19
Rasagiline derivatives combined with histamine H
AID1352197Selectivity index, ratio of IC50 for recombinant human MAO-A to IC50 for recombinant human MAO-B2018European journal of medicinal chemistry, Feb-10, Volume: 145Design, synthesis and bioevalucation of novel 2,3-dihydro-1H-inden-1-amine derivatives as potent and selective human monoamine oxidase B inhibitors based on rasagiline.
AID1323964Cytotoxicity against rat PC12 cells assessed as cell survival at 100 uM after 24 hrs by MTT assay relative to control2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Neuroprotective effects of benzyloxy substituted small molecule monoamine oxidase B inhibitors in Parkinson's disease.
AID1323966Neuroprotective activity against 6-OHDA-induced toxicity in rat PC12 cells assessed as cell survival at 20 uM preincubated for 24 hrs followed by 6-OHDA addition measured after 24 hrs by MTT assay relative to control2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Neuroprotective effects of benzyloxy substituted small molecule monoamine oxidase B inhibitors in Parkinson's disease.
AID1757197Inhibition of human recombinant MAO-B by multimode plate reader assay2021European journal of medicinal chemistry, Apr-15, Volume: 216Design, synthesis and evaluation of novel dimethylamino chalcone-O-alkylamines derivatives as potential multifunctional agents against Alzheimer's disease.
AID1453105Inhibition of recombinant human MAO-A expressed in baculovirus infected BTI insect cells using kynuramine as substrate after 30 mins by fluorescence assay2017Bioorganic & medicinal chemistry, 06-15, Volume: 25, Issue:12
Design, synthesis and biological evaluation of 3,4-dihydro-2(1H)-quinoline-O-alkylamine derivatives as new multipotent cholinesterase/monoamine oxidase inhibitors for the treatment of Alzheimer's disease.
AID1851412Inhibition of human MAO-B assessed as inhibition of H2O2 production using p-tyramine as substrate2022Bioorganic & medicinal chemistry letters, 10-15, Volume: 74Synthesis and human monoamine oxidase inhibitory activity of novel C2-, C3- and C4-substituted phthalonitriles.
AID1519691Inhibition of human microsomal MAO-B expressed in baculovirus infected BTI-TN-5B1-4 cells assessed as reduction in 4-hydroxyquinoline formation using kynuramine as substrate preincubated with substrate for 10 mins followed by enzyme addition by spectropho2020European journal of medicinal chemistry, Jan-01, Volume: 185Design of novel monoamine oxidase-B inhibitors based on piperine scaffold: Structure-activity-toxicity, drug-likeness and efflux transport studies.
AID1557170Inhibition of equine serum BuChE using S-butyrylthiocholine chloride as substrate incubated for 15 mins by Ellman's method2019Bioorganic & medicinal chemistry letters, 10-01, Volume: 29, Issue:19
The development of 2-acetylphenol-donepezil hybrids as multifunctional agents for the treatment of Alzheimer's disease.
AID1754139Cytotoxicity against human SH-SY5Y cells at 5 to 50 uM after 24 hrs by MTT assay2021Bioorganic & medicinal chemistry letters, 07-01, Volume: 43Novel 1-(prop-2-yn-1-ylamino)-2,3-dihydro-1H-indene-4-thiol derivatives as potent selective human monoamine oxidase B inhibitors: Design, SAR development, and biological evaluation.
AID1667259Antioxidant activity assessed as AAPH-induced radical scavenging activity by measuring trolox equivalents for oxygen radical absorbance capacity measured every minute for 90 mins by ORAC-FL assay2020Bioorganic & medicinal chemistry, 04-01, Volume: 28, Issue:7
Design, synthesis and evaluation of flurbiprofen-clioquinol hybrids as multitarget-directed ligands against Alzheimer's disease.
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID1586574Inhibition of Sprague-Dawley rat liver MAO-B using p-tyramine as substrate preincubated for 15 mins and measured after 45 mins by resorufin-based fluorescence assay2019European journal of medicinal chemistry, Jan-15, Volume: 162(Pyrrolo-pyridin-5-yl)benzamides: BBB permeable monoamine oxidase B inhibitors with neuroprotective effect on cortical neurons.
AID1754143Cytotoxicity against C57/BL6 mouse BV-2 cells at 5 to 50 uM after 24 hrs by MTT assay2021Bioorganic & medicinal chemistry letters, 07-01, Volume: 43Novel 1-(prop-2-yn-1-ylamino)-2,3-dihydro-1H-indene-4-thiol derivatives as potent selective human monoamine oxidase B inhibitors: Design, SAR development, and biological evaluation.
AID1754149Neuroprotective activity against MPTP-induced C57BL/6J mouse model of Parkinson's disease assessed as increase in total distance at 0.2 mg/kg, ip pretreated for 7 consecutive days followed by MPTP challenge and further treated with compound until day 14 b2021Bioorganic & medicinal chemistry letters, 07-01, Volume: 43Novel 1-(prop-2-yn-1-ylamino)-2,3-dihydro-1H-indene-4-thiol derivatives as potent selective human monoamine oxidase B inhibitors: Design, SAR development, and biological evaluation.
AID1761238Cytotoxicity against mouse SIM-A9 cells measured after 24 hrs by MTT assay2021European journal of medicinal chemistry, Feb-05, Volume: 2112-Propargylamino-naphthoquinone derivatives as multipotent agents for the treatment of Alzheimer's disease.
AID317112Activation of ERK1/2 in T20 cells at 10 uM relative to nontreated cells2008Bioorganic & medicinal chemistry, Feb-15, Volume: 16, Issue:4
New 1,2,3,4-tetrahydroisoquinoline derivatives as modulators of proteolytic cleavage of amyloid precursor proteins.
AID1421879Inhibition of human recombinant microsomal MAOA expressed in baculovirus infected BTI-TN-5B1- 4 cells using p-tyramine as substrate assessed as decrease in H2O2 production by amplex red-based fluorescence assay2018European journal of medicinal chemistry, Oct-05, Volume: 158Multi-target-directed ligands for Alzheimer's disease: Discovery of chromone-based monoamine oxidase/cholinesterase inhibitors.
AID1751717Inhibition of recombinant human MAO-B expressed in baculovirus infected BTI-TN- 5B1-4 insect cells using kynuramine as substrate preincubated for 10 mins in presence of substrate followed by enzyme addition and measured every minute for 30 mins by spectro2021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
Mapping Chromone-3-Phenylcarboxamide Pharmacophore:
AID1458405Inhibition of human recombinant microsomal MAOA expressed in baculovirus infected BTI-TN-5B1- 4 cells using p-tyramine as substrate assessed as decrease in H2O2 production after 15 mins by amplex red-based fluorescence assay2017Journal of medicinal chemistry, 08-24, Volume: 60, Issue:16
Coumarin versus Chromone Monoamine Oxidase B Inhibitors: Quo Vadis?
AID1704813Inhibition of recombinant human MAO-B expressed in baculovirus infected BTI cells using p-tyramine as substrate by fluorometric assay
AID1465288Inhibition of human recombinant MAO-B expressed in baculovirus infected BTI insect cells using kynuramine as substrate after 30 mins by fluorescence assay2017Bioorganic & medicinal chemistry letters, 11-15, Volume: 27, Issue:22
Design, synthesis and biological evaluation of phthalimide-alkylamine derivatives as balanced multifunctional cholinesterase and monoamine oxidase-B inhibitors for the treatment of Alzheimer's disease.
AID1635461Inhibition of human microsomal MAO-B expressed in recombinant baculovirus infected insect BTI-TN-5B1-4 cells assessed as reduction in H2O2 production using p-tyramine as substrate after 15 mins by fluorescence assay2016Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
Discovery of New Chemical Entities for Old Targets: Insights on the Lead Optimization of Chromone-Based Monoamine Oxidase B (MAO-B) Inhibitors.
AID1456237Inhibition of recombinant human MAO-B expressed in baculovirus infected BTI insect cells using tyramine as substrate pretreated for 30 mins followed by substrate addition incubated for 30 mins measured at 5 mins interval by horse-radish peroxidase/amplex 2017European journal of medicinal chemistry, May-05, Volume: 131MAO enzymes inhibitory activity of new benzimidazole derivatives including hydrazone and propargyl side chains.
AID743813Inhibition of human recombinant microsomal MAO-A expressed in baculovirus infected BTI-TN-5B1-4 cells using p-tyramine as substrate assessed as production of H2O2 incubated for 15 mins followed by substrate addition measured over 15 mins by fluorimetric a2013European journal of medicinal chemistry, May, Volume: 63Novel (coumarin-3-yl)carbamates as selective MAO-B inhibitors: synthesis, in vitro and in vivo assays, theoretical evaluation of ADME properties and docking study.
AID1667263Inhibition of recombinant human MAOB expressed in baculovirus infected in BTI cells using kynuramine as substrate after 30 mins by fluorescence based assay2020Bioorganic & medicinal chemistry, 04-01, Volume: 28, Issue:7
Design, synthesis and evaluation of flurbiprofen-clioquinol hybrids as multitarget-directed ligands against Alzheimer's disease.
AID1192622Inhibition of human recombinant soluble MAO-B expressed in Pichia pastoris incubated for 30 mins prior to substrate addition measured after 60 mins by MAO-Glo assay2015Bioorganic & medicinal chemistry, Feb-15, Volume: 23, Issue:4
Reversible and irreversible small molecule inhibitors of monoamine oxidase B (MAO-B) investigated by biophysical techniques.
AID1427513Inhibition of recombinant human MAO-B expressed in baculovirus infected BTI insect cells using kynuramine as substrate after 30 mins by fluorimetric method2017Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6
Multifunctional thioxanthone derivatives with acetylcholinesterase, monoamine oxidases and β-amyloid aggregation inhibitory activities as potential agents against Alzheimer's disease.
AID125726In vitro inhibitory concentration against Monoamine oxidase A of rat brain homogenates; value ranges from 0.28-0.542002Journal of medicinal chemistry, Nov-21, Volume: 45, Issue:24
Novel dual inhibitors of AChE and MAO derived from hydroxy aminoindan and phenethylamine as potential treatment for Alzheimer's disease.
AID1374194Inhibition of cupric ion-mediated amyloid beta (1 to 42) aggregation at 25 uM after 24 hrs by thioflavin T fluorescence assay relative to control2018Bioorganic & medicinal chemistry, 03-01, Volume: 26, Issue:5
Design, synthesis and evaluation of 4'-OH-flurbiprofen-chalcone hybrids as potential multifunctional agents for Alzheimer's disease treatment.
AID1336725Inhibition of recombinant human MAO-B expressed in baculovirus infected High 5 insect cells using kynuramine as substrate incubated for 30 mins by spectrofluorometric method2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Design, synthesis and biological evaluation of 4'-aminochalcone-rivastigmine hybrids as multifunctional agents for the treatment of Alzheimer's disease.
AID1525506Inhibition of MAO-B in rat brain using [14C]-phenylethylamine as substrate preincubated for 60 mins followed by substrate addition and measured after 30 mins by liquid scintillation counting method2019Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20
Rational Design of Multitarget-Directed Ligands: Strategies and Emerging Paradigms.
AID1751716Inhibition of recombinant human MAO-A expressed in baculovirus infected BTI-TN- 5B1-4 insect cells using kynuramine as substrate preincubated for 10 mins in presence of substrate followed by enzyme addition and measured every minute for 30 mins by spectro2021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
Mapping Chromone-3-Phenylcarboxamide Pharmacophore:
AID1532334Displacement of [3H]-N-alpha-methylhistamine from human H3 receptor expressed in CHO-K1 cell membranes after 60 mins by microbeta2 scintillation counting analysis2018Bioorganic & medicinal chemistry letters, 12-15, Volume: 28, Issue:23-24
4-tert-Pentylphenoxyalkyl derivatives - Histamine H
AID743812Inhibition of human recombinant microsomal MAO-B expressed in baculovirus infected BTI-TN-5B1-4 cells using p-tyramine as substrate assessed as production of H2O2 incubated for 15 mins followed by substrate addition measured over 15 mins by fluorimetric a2013European journal of medicinal chemistry, May, Volume: 63Novel (coumarin-3-yl)carbamates as selective MAO-B inhibitors: synthesis, in vitro and in vivo assays, theoretical evaluation of ADME properties and docking study.
AID1485917Selectivity index, ratio of IC50 for recombinant human MAO-A expressed in baculovirus infected BTI insect cells to IC50 for recombinant human MAO-B expressed in baculovirus infected BTI insect cells2017Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
Synthesis and pharmacological evaluation of novel chromone derivatives as balanced multifunctional agents against Alzheimer's disease.
AID1568796Inhibition of recombinant human MAO-B expressed in baculovirus infected BTI insect cells using kynuramine as substrate measured after 30 mins by fluorescence based assay2019European journal of medicinal chemistry, Sep-15, Volume: 178Design, synthesis, in-silico and biological evaluation of novel chalcone-O-carbamate derivatives as multifunctional agents for the treatment of Alzheimer's disease.
AID1851414Selectivity index, ratio of IC50 for inhibition of human MAO-A to IC50 for inhibition of human MAO-B2022Bioorganic & medicinal chemistry letters, 10-15, Volume: 74Synthesis and human monoamine oxidase inhibitory activity of novel C2-, C3- and C4-substituted phthalonitriles.
AID232322Ratio of A415 rise monoamine oxidase A between kinact and Ki2004Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7
Inactivation of purified human recombinant monoamine oxidases A and B by rasagiline and its analogues.
AID126546Compound was evaluated for A 450 rise towards monoamine oxidase B enzyme2004Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7
Inactivation of purified human recombinant monoamine oxidases A and B by rasagiline and its analogues.
AID1551697Inhibition of recombinant human MAO-B expressed in baculovirus infected BTI insect cells using p-tyramine as substrate preincubated for 60 mins followed by substrate addition and measured after 30 mins by horse-radish peroxidase-coupled amplex red reagent2019European journal of medicinal chemistry, Jul-01, Volume: 173Discovery of coumarin Mannich base derivatives as multifunctional agents against monoamine oxidase B and neuroinflammation for the treatment of Parkinson's disease.
AID706468Selectivity ratio of IC50 for human recombinant MAOA to IC50 for human recombinant MAOB2012Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19
Multitarget-directed benzylideneindanone derivatives: anti-β-amyloid (Aβ) aggregation, antioxidant, metal chelation, and monoamine oxidase B (MAO-B) inhibition properties against Alzheimer's disease.
AID1437168Inhibition of recombinant human MAO-A using kynuramine as substrate after 30 mins by fluorescence assay2017Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4
DL-3-n-butylphthalide-Edaravone hybrids as novel dual inhibitors of amyloid-β aggregation and monoamine oxidases with high antioxidant potency for Alzheimer's therapy.
AID1551698Selectivity index, ratio of IC50 for recombinant human MAO-A expressed in baculovirus infected BTI insect cells to IC50 for recombinant human MAO-B expressed in baculovirus infected BTI insect cells2019European journal of medicinal chemistry, Jul-01, Volume: 173Discovery of coumarin Mannich base derivatives as multifunctional agents against monoamine oxidase B and neuroinflammation for the treatment of Parkinson's disease.
AID1292322Inhibition of human recombinant MAO-B using kynuramine as substrate after 30 mins by fluorescence spectrophotometry2016Bioorganic & medicinal chemistry, 05-15, Volume: 24, Issue:10
Synthesis and evaluation of 4-hydroxyl aurone derivatives as multifunctional agents for the treatment of Alzheimer's disease.
AID229512Ratio of IC50 value against MAO-A to that of MAO-B.2002Journal of medicinal chemistry, Nov-21, Volume: 45, Issue:24
Novel dual inhibitors of AChE and MAO derived from hydroxy aminoindan and phenethylamine as potential treatment for Alzheimer's disease.
AID1199578Selectivity ratio of IC50 for rat brain MAO-A to IC50 for rat brain MAO-B2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Novel arylalkenylpropargylamines as neuroprotective, potent, and selective monoamine oxidase B inhibitors for the treatment of Parkinson's disease.
AID1754141Inhibition of human MAO-A2021Bioorganic & medicinal chemistry letters, 07-01, Volume: 43Novel 1-(prop-2-yn-1-ylamino)-2,3-dihydro-1H-indene-4-thiol derivatives as potent selective human monoamine oxidase B inhibitors: Design, SAR development, and biological evaluation.
AID317110Inhibition of monoamino oxidase B from F344/N rat brain cortex2008Bioorganic & medicinal chemistry, Feb-15, Volume: 16, Issue:4
New 1,2,3,4-tetrahydroisoquinoline derivatives as modulators of proteolytic cleavage of amyloid precursor proteins.
AID232323Ratio of A415 rise monoamine oxidase B between kinact and Ki2004Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7
Inactivation of purified human recombinant monoamine oxidases A and B by rasagiline and its analogues.
AID1427512Inhibition of recombinant human MAO-A expressed in baculovirus infected BTI insect cells using kynuramine as substrate after 30 mins by fluorimetric method2017Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6
Multifunctional thioxanthone derivatives with acetylcholinesterase, monoamine oxidases and β-amyloid aggregation inhibitory activities as potential agents against Alzheimer's disease.
AID1444065Irreversible inhibition of human cerebral cortex MAO-A using [14C]-5-hydroxytryptamine creatinine disulphate as substrate pretreated for 60 mins followed by substrate addition after 30 mins by liquid scintillation counting method2017European journal of medicinal chemistry, Apr-21, Volume: 130Discovery of highly selective and potent monoamine oxidase B inhibitors: Contribution of additional phenyl rings introduced into 2-aryl-1,3,4-oxadiazin-5(6H)-one.
AID126700In vitro inhibitory concentration against Monoamine oxidase B of rat brain homogenates; value ranges from 0.0035-0.0532002Journal of medicinal chemistry, Nov-21, Volume: 45, Issue:24
Novel dual inhibitors of AChE and MAO derived from hydroxy aminoindan and phenethylamine as potential treatment for Alzheimer's disease.
AID1519692Inhibition of human microsomal MAO-A expressed in baculovirus infected BTI-TN-5B1-4 cells assessed as reduction in 4-hydroxyquinoline formation using kynuramine as substrate preincubated with substrate for 10 mins followed by enzyme addition by spectropho2020European journal of medicinal chemistry, Jan-01, Volume: 185Design of novel monoamine oxidase-B inhibitors based on piperine scaffold: Structure-activity-toxicity, drug-likeness and efflux transport studies.
AID1528913Inhibition of recombinant human microsomal MAOA expressed in baculovirus infected BTI insect cells using p-tyramine as substrate preincubated for 15 mins followed by substrate addition and measured over 20 mins by amplex red reagent-based horseradish pero
AID1586575Inhibition of human recombinant MAO-B expressed in baculovirus infected BTI-TN-5B1-4 insect cells using p-tyramine as substrate preincubated for 15 mins and measured after 45 mins by resorufin-based fluorescence assay2019European journal of medicinal chemistry, Jan-15, Volume: 162(Pyrrolo-pyridin-5-yl)benzamides: BBB permeable monoamine oxidase B inhibitors with neuroprotective effect on cortical neurons.
AID1352195Inhibition of recombinant human MAO-A using p-tyramine as substrate preincubated for 15 mins followed by substrate addition measured over 15 mins by Amplex red reagent-based fluorimetric method2018European journal of medicinal chemistry, Feb-10, Volume: 145Design, synthesis and bioevalucation of novel 2,3-dihydro-1H-inden-1-amine derivatives as potent and selective human monoamine oxidase B inhibitors based on rasagiline.
AID1192621Inhibition of human recombinant microsomal MAO-B expressed in Pichia pastoris incubated for 30 mins prior to substrate addition measured after 60 mins by MAO-Glo assay2015Bioorganic & medicinal chemistry, Feb-15, Volume: 23, Issue:4
Reversible and irreversible small molecule inhibitors of monoamine oxidase B (MAO-B) investigated by biophysical techniques.
AID126542Binding affinity towards monoamine oxidase B activity was measured using a benzylamine assay2004Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7
Inactivation of purified human recombinant monoamine oxidases A and B by rasagiline and its analogues.
AID635338Selectivity ratio of Ki for human recombinant MAO-A to Ki for human recombinant MAO-B2011Bioorganic & medicinal chemistry, Dec-15, Volume: 19, Issue:24
Molecular insights into human monoamine oxidase (MAO) inhibition by 1,4-naphthoquinone: evidences for menadione (vitamin K3) acting as a competitive and reversible inhibitor of MAO.
AID125568Compound was evaluated for A 450 rise towards monoamine oxidase A enzyme2004Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7
Inactivation of purified human recombinant monoamine oxidases A and B by rasagiline and its analogues.
AID1667262Inhibition of recombinant human MAOA expressed in baculovirus infected in BTI cells using kynuramine as substrate after 30 mins by fluorescence based assay2020Bioorganic & medicinal chemistry, 04-01, Volume: 28, Issue:7
Design, synthesis and evaluation of flurbiprofen-clioquinol hybrids as multitarget-directed ligands against Alzheimer's disease.
AID254307Inhibition constant against human recombinant Monoamine oxidase-B 2005Bioorganic & medicinal chemistry letters, Oct-15, Volume: 15, Issue:20
Docking studies on monoamine oxidase-B inhibitors: estimation of inhibition constants (K(i)) of a series of experimentally tested compounds.
AID1399983Inhibition of rat MAOA using 5-hydroxytryptamine as substrate pretreated for 1200 secs followed by substrate addition and measured after 3600 secs2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
Design, synthesis and biological evaluation of lazabemide derivatives as inhibitors of monoamine oxidase.
AID1336728Selectivity index, ratio of IC50 for recombinant human MAO-A expressed in baculovirus infected High 5 insect cells to IC50 for recombinant human MAO-B expressed in baculovirus infected High 5 insect cells2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Design, synthesis and biological evaluation of 4'-aminochalcone-rivastigmine hybrids as multifunctional agents for the treatment of Alzheimer's disease.
AID1453106Inhibition of recombinant human MAO-B expressed in baculovirus infected BTI insect cells using kynuramine as substrate after 30 mins by fluorescence assay2017Bioorganic & medicinal chemistry, 06-15, Volume: 25, Issue:12
Design, synthesis and biological evaluation of 3,4-dihydro-2(1H)-quinoline-O-alkylamine derivatives as new multipotent cholinesterase/monoamine oxidase inhibitors for the treatment of Alzheimer's disease.
AID317111Lipophilicity, log P of the compound2008Bioorganic & medicinal chemistry, Feb-15, Volume: 16, Issue:4
New 1,2,3,4-tetrahydroisoquinoline derivatives as modulators of proteolytic cleavage of amyloid precursor proteins.
AID1650986Inhibition of MAO-B in Wistar rat liver using 4-trifluoromethyl benzylamine as substrate preincubated for 20 mins followed by substrate addition measured after 90 mins by microplate reader assay2020Bioorganic & medicinal chemistry letters, 02-15, Volume: 30, Issue:4
Synthesis and biological evaluation of 4-arylcoumarins as potential anti-Alzheimer's disease agents.
AID1374193Inhibition of self-induced aggregation of amyloid beta (1 to 42) (unknown origin) at 25 uM after 24 hrs by thioflavin T fluorescence method relative to control2018Bioorganic & medicinal chemistry, 03-01, Volume: 26, Issue:5
Design, synthesis and evaluation of 4'-OH-flurbiprofen-chalcone hybrids as potential multifunctional agents for Alzheimer's disease treatment.
AID125558Inhibitory concentration towards in human monoamine oxidase A was measured2004Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7
Inactivation of purified human recombinant monoamine oxidases A and B by rasagiline and its analogues.
AID1851411Inhibition of human MAO-A assessed as inhibition of H2O2 production using p-tyramine as substrate2022Bioorganic & medicinal chemistry letters, 10-15, Volume: 74Synthesis and human monoamine oxidase inhibitory activity of novel C2-, C3- and C4-substituted phthalonitriles.
AID125570Compound was evaluated for inactivation for monoamine oxidase A2004Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7
Inactivation of purified human recombinant monoamine oxidases A and B by rasagiline and its analogues.
AID1334746Selectivity index, ratio of IC50 for human recombinant MAO-A to IC50 for human recombinant MAO-B2017Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
Multitarget drug design strategy against Alzheimer's disease: Homoisoflavonoid Mannich base derivatives serve as acetylcholinesterase and monoamine oxidase B dual inhibitors with multifunctional properties.
AID125557Compound was evaluated for observed mass inactivation in human monoamine oxidase A enzyme2004Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7
Inactivation of purified human recombinant monoamine oxidases A and B by rasagiline and its analogues.
AID314094Inhibition of MAOA2008Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
Multi-target-directed ligands to combat neurodegenerative diseases.
AID1390035Inhibition of recombinant human MAO-A using kynuramine as substrate after 30 mins by fluorescence assay2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
Multifunctional 5,6-dimethoxybenzo[d]isothiazol-3(2H)-one-N-alkylbenzylamine derivatives with acetylcholinesterase, monoamine oxidases and β-amyloid aggregation inhibitory activities as potential agents against Alzheimer's disease.
AID1465284Inhibition of human erythrocyte AChE using acetylthiocholine chloride as substrate incubated for 15 mins by Ellman's method2017Bioorganic & medicinal chemistry letters, 11-15, Volume: 27, Issue:22
Design, synthesis and biological evaluation of phthalimide-alkylamine derivatives as balanced multifunctional cholinesterase and monoamine oxidase-B inhibitors for the treatment of Alzheimer's disease.
AID1532340Irreversible inhibition of human MAO-B expressed in baculovirus infected BTI insect cells at IC80 preincubated with compound and p-tyramine for 22 mins followed by p-tyramine increase to 1 mM and measured every minute for 5 hrs by fluorescence assay2018Bioorganic & medicinal chemistry letters, 12-15, Volume: 28, Issue:23-24
4-tert-Pentylphenoxyalkyl derivatives - Histamine H
AID1517859Inhibition of recombinant human MAO-A expressed in baculovirus infected BTI insect cells using kynuramine as substrate after 30 mins by fluorescence based assay2019European journal of medicinal chemistry, Dec-01, Volume: 183Development of chalcone-O-alkylamine derivatives as multifunctional agents against Alzheimer's disease.
AID1586573Inhibition of human recombinant MAO-A expressed in baculovirus infected BTI-TN-5B1-4 insect cells using p-tyramine as substrate preincubated for 15 mins and measured after 45 mins by resorufin-based fluorescence assay2019European journal of medicinal chemistry, Jan-15, Volume: 162(Pyrrolo-pyridin-5-yl)benzamides: BBB permeable monoamine oxidase B inhibitors with neuroprotective effect on cortical neurons.
AID1323963Selectivity index, ratio of IC50 for recombinant human MAO-A to IC50 for recombinant human MAO-B incubated for 15 mins2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Neuroprotective effects of benzyloxy substituted small molecule monoamine oxidase B inhibitors in Parkinson's disease.
AID1706696Inhibition of recombinant human MAO-A expressed in baculovirus infected BTI-TN-5B1-4 insect cells using p-tyramine as substrate preincubated for 15 mins followed by substrate addition and measured over 20 mins by horse-radish peroxidase/Amplex Red coupled2021European journal of medicinal chemistry, Jan-01, Volume: 209Pyrimido[1,2-b]indazole derivatives: Selective inhibitors of human monoamine oxidase B with neuroprotective activity.
AID232416Ratio of inactive monoamine oxidase B between kinact and Ki2004Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7
Inactivation of purified human recombinant monoamine oxidases A and B by rasagiline and its analogues.
AID1761635Selectivity index, ratio of IC50 for inhibition of human MAOA to IC50 for inhibition of human MAOB2021European journal of medicinal chemistry, Mar-05, Volume: 2134-Oxoquinolines and monoamine oxidase: When tautomerism matters.
AID1465302Inhibition of recombinant human MAO-A using kynuramine as substrate after 30 mins by fluorescence method2017Bioorganic & medicinal chemistry letters, 11-15, Volume: 27, Issue:22
Design, synthesis and biological evaluation of 2-acetyl-5-O-(amino-alkyl)phenol derivatives as multifunctional agents for the treatment of Alzheimer's disease.
AID779070Inhibition of recombinant human MAO-B expressed in insect cells using kynuramine as substrate assessed as formation of 4-hydroxyquinoline measured every 5 mins for 30 mins2013Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21
Development of a novel fluorine-18 labeled deuterated fluororasagiline ([(18)F]fluororasagiline-D2) radioligand for PET studies of monoamino oxidase B (MAO-B).
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID1390036Inhibition of recombinant human MAO-B using kynuramine as substrate after 30 mins by fluorescence assay2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
Multifunctional 5,6-dimethoxybenzo[d]isothiazol-3(2H)-one-N-alkylbenzylamine derivatives with acetylcholinesterase, monoamine oxidases and β-amyloid aggregation inhibitory activities as potential agents against Alzheimer's disease.
AID1525505Inhibition of MAO-A in rat brain using [14C]-5-hydroxytryptamine creatinine disulfate as substrate preincubated for 60 mins followed by substrate addition and measured after 30 mins by liquid scintillation counting method2019Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20
Rational Design of Multitarget-Directed Ligands: Strategies and Emerging Paradigms.
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1199580Inhibition of rat brain MAO-A in nuclei-free homogenates using [14C]hydroxytryptamine substrate after 20 mins by liquid scintillation counting2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Novel arylalkenylpropargylamines as neuroprotective, potent, and selective monoamine oxidase B inhibitors for the treatment of Parkinson's disease.
AID1292324Selectivity ratio of IC50 for human recombinant MAO-A to IC50 for human recombinant MAO-B2016Bioorganic & medicinal chemistry, 05-15, Volume: 24, Issue:10
Synthesis and evaluation of 4-hydroxyl aurone derivatives as multifunctional agents for the treatment of Alzheimer's disease.
AID1569980Inhibition of recombinant human MAO-A expressed in baculovirus infected BTI insect cells using kynuramine as substrate incubated for 30 mins by fluorescence based assay2019European journal of medicinal chemistry, Oct-15, Volume: 180Design, synthesis, in-silico and biological evaluation of novel chalcone derivatives as multi-function agents for the treatment of Alzheimer's disease.
AID1761632Inhibition of recombinant human MAOB using kynuramine as substrate measured for 30 mins by fluorescence spectrophotometric assay2021European journal of medicinal chemistry, Mar-05, Volume: 2134-Oxoquinolines and monoamine oxidase: When tautomerism matters.
AID1465299Inhibition of equine serum BuChE incubated for 15 mins by Ellman's method2017Bioorganic & medicinal chemistry letters, 11-15, Volume: 27, Issue:22
Design, synthesis and biological evaluation of 2-acetyl-5-O-(amino-alkyl)phenol derivatives as multifunctional agents for the treatment of Alzheimer's disease.
AID1437172Selectivity index, ratio of IC50 for recombinant human MAO-A to IC50 for recombinant human MAO-B2017Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4
DL-3-n-butylphthalide-Edaravone hybrids as novel dual inhibitors of amyloid-β aggregation and monoamine oxidases with high antioxidant potency for Alzheimer's therapy.
AID1706698Selectivity index, ratio of IC50 for recombinant human MAO-A to IC50 for recombinant human MAO-B2021European journal of medicinal chemistry, Jan-01, Volume: 209Pyrimido[1,2-b]indazole derivatives: Selective inhibitors of human monoamine oxidase B with neuroprotective activity.
AID1323961Inhibition of recombinant human MAO-B using p-tyramine as substrate assessed as decrease in H2O2 production incubated for 15 mins by fluorimetric method2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Neuroprotective effects of benzyloxy substituted small molecule monoamine oxidase B inhibitors in Parkinson's disease.
AID1458408Selectivity index, ratio of IC50 for human recombinant microsomal MAOA to IC50 for human recombinant microsomal MAOB2017Journal of medicinal chemistry, 08-24, Volume: 60, Issue:16
Coumarin versus Chromone Monoamine Oxidase B Inhibitors: Quo Vadis?
AID1192631Binding affinity to human recombinant microsomal MAO-B by ITC2015Bioorganic & medicinal chemistry, Feb-15, Volume: 23, Issue:4
Reversible and irreversible small molecule inhibitors of monoamine oxidase B (MAO-B) investigated by biophysical techniques.
AID1691657Disaggregation of self-induced amyloid beta (1 to 42) (unknown origin) preformed fibrils at 25 uM measured after 24 hrs by thioflavin-T fluorescence assay relative to control2020European journal of medicinal chemistry, May-15, Volume: 194Design, synthesis and biological evaluation of novel O-carbamoyl ferulamide derivatives as multi-target-directed ligands for the treatment of Alzheimer's disease.
AID1754144Cytotoxicity against C57/BL6 mouse BV-2 cells assessed as induction of cell death at 50 uM after 24 hrs by MTT assay relative to control2021Bioorganic & medicinal chemistry letters, 07-01, Volume: 43Novel 1-(prop-2-yn-1-ylamino)-2,3-dihydro-1H-indene-4-thiol derivatives as potent selective human monoamine oxidase B inhibitors: Design, SAR development, and biological evaluation.
AID1872726Inhibition of MAO-B (unknown origin) incubated for 30 mins2022European journal of medicinal chemistry, Apr-05, Volume: 233Resveratrol-based compounds and neurodegeneration: Recent insight in multitarget therapy.
AID1517856Selectivity index, ratio of IC50 for recombinant human MAO-A expressed in baculovirus infected BTI cells to IC50 for recombinant human MAO-B expressed in baculovirus infected BTI cells2019European journal of medicinal chemistry, Dec-01, Volume: 183Development of chalcone-O-alkylamine derivatives as multifunctional agents against Alzheimer's disease.
AID1532341Irreversible inhibition of human MAOB2018Bioorganic & medicinal chemistry letters, 12-15, Volume: 28, Issue:23-24
4-tert-Pentylphenoxyalkyl derivatives - Histamine H
AID658202Inhibition of human recombinant MAO-B expressed in insect cells assessed as kynuramine hydrobromide oxidation after 20 mins by spectrophotometric analysis2012Bioorganic & medicinal chemistry, May-01, Volume: 20, Issue:9
Synthesis and evaluation of [¹⁸F]fluororasagiline, a novel positron emission tomography (PET) radioligand for monoamine oxidase B (MAO-B).
AID1639029Inhibition of recombinant human MAOA expressed in baculovirus infected BTI insect cells using p-tyramine as substrate preincubated for 30 mins followed by substrate addition and measured over 45 mins by horseradish peroxidase-Amplex Red-coupled fluorometr2019Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7
Novel multi-target directed ligands based on annelated xanthine scaffold with aromatic substituents acting on adenosine receptor and monoamine oxidase B. Synthesis, in vitro and in silico studies.
AID1323965Cytotoxicity against rat PC12 cells assessed as cell survival at 20 uM after 72 hrs by MTT assay relative to control2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Neuroprotective effects of benzyloxy substituted small molecule monoamine oxidase B inhibitors in Parkinson's disease.
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1485919Inhibition of HFIP-pretreated amyloid beta (1 to 42) (unknown origin) self-induced aggregation at 20 uM after 46 to 48 hrs by thioflavin-T fluorescence assay relative to control2017Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
Synthesis and pharmacological evaluation of novel chromone derivatives as balanced multifunctional agents against Alzheimer's disease.
AID1568801Disaggregation of Cu2+ induced preformed fibrils of amyloid beta (1 to 42) (unknown origin) at 25 uM preincubated with Cu2+ for 24 hrs followed by compound addition and measured after 24 hrs by thioflavin-T based fluorescence assay relative to control2019European journal of medicinal chemistry, Sep-15, Volume: 178Design, synthesis, in-silico and biological evaluation of novel chalcone-O-carbamate derivatives as multifunctional agents for the treatment of Alzheimer's disease.
AID1761237Cytotoxicity against human SH-SY5Y cells measured after 24 hrs by MTT assay2021European journal of medicinal chemistry, Feb-05, Volume: 2112-Propargylamino-naphthoquinone derivatives as multipotent agents for the treatment of Alzheimer's disease.
AID1709260Inhibition of recombinant human MAOA using kynuramine as substrate preincubated for 30 mins followed by substrate addition and measured after 30 mins by fluorescence assay2021Bioorganic & medicinal chemistry, 04-01, Volume: 35Novel 3-benzylidene/benzylphthalide Mannich base derivatives as potential multifunctional agents for the treatment of Alzheimer's disease.
AID635344Selectivity ratio of Ki for rat MAO-A to Ki for rat MAO-B2011Bioorganic & medicinal chemistry, Dec-15, Volume: 19, Issue:24
Molecular insights into human monoamine oxidase (MAO) inhibition by 1,4-naphthoquinone: evidences for menadione (vitamin K3) acting as a competitive and reversible inhibitor of MAO.
AID1826662Inhibition of human recombinant MAO-B at 18 nM preincubated upto 30 mins using tyramine as substrate by fluorescence assay relative to control2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Resveratrol-Based MTDLs to Stimulate Defensive and Regenerative Pathways and Block Early Events in Neurodegenerative Cascades.
AID1740547Neuroprotective activity against 6-OHDA-induced cell death in human SH-SY5Y cells assessed as increase in cell survival at 1.563 to 25 uM incubated for 24 hrs by MTT assay2020European journal of medicinal chemistry, Sep-15, Volume: 202Design, synthesis and biological evaluation of rasagiline-clorgyline hybrids as novel dual inhibitors of monoamine oxidase-B and amyloid-β aggregation against Alzheimer's disease.
AID1465285Inhibition of human serum BChE using butyrylthiocholine chloride as substrate incubated for 15 mins by Ellman's method2017Bioorganic & medicinal chemistry letters, 11-15, Volume: 27, Issue:22
Design, synthesis and biological evaluation of phthalimide-alkylamine derivatives as balanced multifunctional cholinesterase and monoamine oxidase-B inhibitors for the treatment of Alzheimer's disease.
AID1740534Inhibition of recombinant human MAOA expressed in baculovirus infected BTI insect cells at 100 uM using p-tyramine as substrate measured after 15 mins by Amplex red reagent based fluorescence assay relative to control2020European journal of medicinal chemistry, Sep-15, Volume: 202Design, synthesis and biological evaluation of rasagiline-clorgyline hybrids as novel dual inhibitors of monoamine oxidase-B and amyloid-β aggregation against Alzheimer's disease.
AID1485914Antioxidant activity assessed as trolox equivalent of APPH-induced radical scavenging activity at 1 to 10 uM preincubated for 15 mins followed by AAPH addition measured every minute for 120 mins by ORAC fluorescein assay2017Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
Synthesis and pharmacological evaluation of novel chromone derivatives as balanced multifunctional agents against Alzheimer's disease.
AID1421881Selectivity index, ratio of IC50 for human recombinant MAOA to IC50 for human recombinant MAOB2018European journal of medicinal chemistry, Oct-05, Volume: 158Multi-target-directed ligands for Alzheimer's disease: Discovery of chromone-based monoamine oxidase/cholinesterase inhibitors.
AID1517863Inhibition of equine butyrylcholinesterase using butyrylthiocholine iodide as substrate incubated for 15 mins by Ellman's method2019European journal of medicinal chemistry, Dec-01, Volume: 183Development of chalcone-O-alkylamine derivatives as multifunctional agents against Alzheimer's disease.
AID1436077Inhibition of recombinant human MAO-B expressed in baculovirus infected BTI insect cells using kynuramine as substrate incubated for 30 mins by fluorescence assay2017European journal of medicinal chemistry, Jan-27, Volume: 126Aurone Mannich base derivatives as promising multifunctional agents with acetylcholinesterase inhibition, anti-β-amyloid aggragation and neuroprotective properties for the treatment of Alzheimer's disease.
AID1751720Selectivity index, ratio of IC50 for recombinant human MAO-A expressed in baculovirus infected BTI-TN- 5B1-4 insect cells to IC50 for recombinant human MAO-B expressed in baculovirus infected BTI-TN- 5B1-4 insect cells using kynuramine as substrate preinc2021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
Mapping Chromone-3-Phenylcarboxamide Pharmacophore:
AID1635465Selectivity index, ratio of IC50 for human microsomal MAO-A expressed in recombinant baculovirus infected insect BTI-TN-5B1-4 cells to IC50 for human microsomal MAO-B expressed in recombinant baculovirus infected insect BTI-TN-5B1-4 cells2016Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
Discovery of New Chemical Entities for Old Targets: Insights on the Lead Optimization of Chromone-Based Monoamine Oxidase B (MAO-B) Inhibitors.
AID1754145Cytotoxicity against human SH-SY5Y cells assessed as induction of cell death at 50 uM after 24 hrs by MTT assay relative to control2021Bioorganic & medicinal chemistry letters, 07-01, Volume: 43Novel 1-(prop-2-yn-1-ylamino)-2,3-dihydro-1H-indene-4-thiol derivatives as potent selective human monoamine oxidase B inhibitors: Design, SAR development, and biological evaluation.
AID1740538Selectivity index, ratio of IC50 for recombinant human MAOA expressed in baculovirus infected BTI insect cells to IC50 for recombinant human MAOB expressed in baculovirus infected BTI insect cells2020European journal of medicinal chemistry, Sep-15, Volume: 202Design, synthesis and biological evaluation of rasagiline-clorgyline hybrids as novel dual inhibitors of monoamine oxidase-B and amyloid-β aggregation against Alzheimer's disease.
AID1568800Inhibition of Cu2+-induced amyloid beta (1 to 42 residues) (unknown origin) aggregation at 25 uM after 24 hrs by thioflavin-T based fluorescence assay relative to control2019European journal of medicinal chemistry, Sep-15, Volume: 178Design, synthesis, in-silico and biological evaluation of novel chalcone-O-carbamate derivatives as multifunctional agents for the treatment of Alzheimer's disease.
AID1754147Neuroprotective activity against LPS-induced oxidative stress in human SH-SY5Y cells assessed as decrease in ROS level at < 20 uM after 24 hrs by DCFH-DA dye based fluorescence assay2021Bioorganic & medicinal chemistry letters, 07-01, Volume: 43Novel 1-(prop-2-yn-1-ylamino)-2,3-dihydro-1H-indene-4-thiol derivatives as potent selective human monoamine oxidase B inhibitors: Design, SAR development, and biological evaluation.
AID1556701Inhibition of human recombinant MAO-B expressed in baculovirus infected BTI-TN-5B1-4 insect cells assessed as decrease in H2O2 production using p-tyramine as substrate incubated for 20 mins by horse-radish peroxidase/amplex red-based fluorescence method2019European journal of medicinal chemistry, Oct-01, Volume: 179Carboxamides vs. methanimines: Crystal structures, binding interactions, photophysical studies, and biological evaluation of (indazole-5-yl)methanimines as monoamine oxidase B and acetylcholinesterase inhibitors.
AID125566Compound was evaluated for A 450 decay towards monoamine oxidase A enzyme2004Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7
Inactivation of purified human recombinant monoamine oxidases A and B by rasagiline and its analogues.
AID1709261Inhibition of recombinant human MAOB using kynuramine as substrate preincubated for 30 mins followed by substrate addition and measured after 30 mins by fluorescence assay2021Bioorganic & medicinal chemistry, 04-01, Volume: 35Novel 3-benzylidene/benzylphthalide Mannich base derivatives as potential multifunctional agents for the treatment of Alzheimer's disease.
AID1754142Selectivity index, ratio of IC50 for human MAO-A to IC50 for human MAO-B2021Bioorganic & medicinal chemistry letters, 07-01, Volume: 43Novel 1-(prop-2-yn-1-ylamino)-2,3-dihydro-1H-indene-4-thiol derivatives as potent selective human monoamine oxidase B inhibitors: Design, SAR development, and biological evaluation.
AID1657150Inhibition of recombinant human MAO-A expressed in baculovirus infected BTI insect cells using kynuramine as substrate measured after 30 mins by fluorescence based assay2020Bioorganic & medicinal chemistry, 04-15, Volume: 28, Issue:8
Design, synthesis and evaluation of phthalide alkyl tertiary amine derivatives as promising acetylcholinesterase inhibitors with high potency and selectivity against Alzheimer's disease.
AID1519690Selectivity index, ratio of IC50 for human microsomal MAO-A expressed in baculovirus infected BTN-TN-5B1-4 cells to IC50 for human microsomal MAO-B expressed in baculovirus infected BTN-TN-5B1-4 cells using kynuramine as substrate2020European journal of medicinal chemistry, Jan-01, Volume: 185Design of novel monoamine oxidase-B inhibitors based on piperine scaffold: Structure-activity-toxicity, drug-likeness and efflux transport studies.
AID1485915Inhibition of recombinant human MAO-A expressed in baculovirus infected BTI insect cells using p-tyramine as substrate pretreated for 15 mins followed by substrate addition after 20 mins by Amplex red reagent based fluorimetric method2017Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
Synthesis and pharmacological evaluation of novel chromone derivatives as balanced multifunctional agents against Alzheimer's disease.
AID1635472Irreversible inhibition of human microsomal MAO-B expressed in recombinant baculovirus infected insect BTI-TN-5B1-4 cells assessed as decay of residual enzyme activity at 200 nM measured after first 15 mins of 60 mins2016Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
Discovery of New Chemical Entities for Old Targets: Insights on the Lead Optimization of Chromone-Based Monoamine Oxidase B (MAO-B) Inhibitors.
AID1709264Antioxidant activity assessed as trolox equivalent of AAPH radical scavenging activity measured every min for 90 mins by ORAC-FL assay2021Bioorganic & medicinal chemistry, 04-01, Volume: 35Novel 3-benzylidene/benzylphthalide Mannich base derivatives as potential multifunctional agents for the treatment of Alzheimer's disease.
AID1528914Inhibition of recombinant human microsomal MAOB expressed in baculovirus infected BTI insect cells using p-tyramine as substrate preincubated for 15 mins followed by substrate addition and measured over 20 mins by amplex red reagent-based horseradish pero
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1556702Selectivity index, ratio of IC50 for human recombinant MAO-A expressed in baculovirus infected BTI-TN-5B1-4 cells to IC50 for human recombinant MAO-B expressed in baculovirus infected BTI-TN-5B1-4 cells2019European journal of medicinal chemistry, Oct-01, Volume: 179Carboxamides vs. methanimines: Crystal structures, binding interactions, photophysical studies, and biological evaluation of (indazole-5-yl)methanimines as monoamine oxidase B and acetylcholinesterase inhibitors.
AID1635482Inhibition of human microsomal MAO-A expressed in recombinant baculovirus infected insect BTI-TN-5B1-4 cells assessed as reduction in H2O2 production using p-tyramine as substrate after 15 mins by fluorescence assay2016Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
Discovery of New Chemical Entities for Old Targets: Insights on the Lead Optimization of Chromone-Based Monoamine Oxidase B (MAO-B) Inhibitors.
AID1691662Inhibition of recombinant human MAO-B2020European journal of medicinal chemistry, May-15, Volume: 194Design, synthesis and biological evaluation of novel O-carbamoyl ferulamide derivatives as multi-target-directed ligands for the treatment of Alzheimer's disease.
AID1569977Inhibition of electric eel AChE using acetylthiocholine iodide as substrate incubated for 15 mins by Ellman's method2019European journal of medicinal chemistry, Oct-15, Volume: 180Design, synthesis, in-silico and biological evaluation of novel chalcone derivatives as multi-function agents for the treatment of Alzheimer's disease.
AID126540Compound was evaluated for observed mass inactivation in human monoamine oxidase B enzyme2004Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7
Inactivation of purified human recombinant monoamine oxidases A and B by rasagiline and its analogues.
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1705912Inhibition of recombinant human MAO-B expressed in baculovirus infected BTI insect cells using p-tyramine as substrate preincubated for 30 mins followed by substrate addition and measured after 1 hr by fluorimetric analysis
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1390039Selectivity index, ratio of IC50 for recombinant human MAO-A to IC50 for recombinant human MAO-B2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
Multifunctional 5,6-dimethoxybenzo[d]isothiazol-3(2H)-one-N-alkylbenzylamine derivatives with acetylcholinesterase, monoamine oxidases and β-amyloid aggregation inhibitory activities as potential agents against Alzheimer's disease.
AID1586572Inhibition of Sprague-Dawley rat liver MAO-A using p-tyramine as substrate preincubated for 15 mins and measured after 45 mins by resorufin-based fluorescence assay2019European journal of medicinal chemistry, Jan-15, Volume: 162(Pyrrolo-pyridin-5-yl)benzamides: BBB permeable monoamine oxidase B inhibitors with neuroprotective effect on cortical neurons.
AID1453107Selectivity index, ratio of IC50 for recombinant human MAO-B to IC50 for recombinant human MAO-A2017Bioorganic & medicinal chemistry, 06-15, Volume: 25, Issue:12
Design, synthesis and biological evaluation of 3,4-dihydro-2(1H)-quinoline-O-alkylamine derivatives as new multipotent cholinesterase/monoamine oxidase inhibitors for the treatment of Alzheimer's disease.
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID743809Selectivity index, ratio of IC50 for human recombinant microsomal MAO-A to IC50 for human recombinant microsomal MAO-B2013European journal of medicinal chemistry, May, Volume: 63Novel (coumarin-3-yl)carbamates as selective MAO-B inhibitors: synthesis, in vitro and in vivo assays, theoretical evaluation of ADME properties and docking study.
AID1458414Time dependent inhibition of human recombinant microsomal MAOB expressed in baculovirus infected BTI-TN-5B1- 4 cells assessed as decrease in H2O2 production at 200 nM after 15 mins by amplex red-based fluorescence assay2017Journal of medicinal chemistry, 08-24, Volume: 60, Issue:16
Coumarin versus Chromone Monoamine Oxidase B Inhibitors: Quo Vadis?
AID1761631Inhibition of recombinant human MAOA using kynuramine as substrate measured for 30 mins by fluorescence spectrophotometric assay2021European journal of medicinal chemistry, Mar-05, Volume: 2134-Oxoquinolines and monoamine oxidase: When tautomerism matters.
AID1557173Inhibition of human recombinant MAO-A using kynuramine as substrate measured after 30 mins by fluorimetric assay2019Bioorganic & medicinal chemistry letters, 10-01, Volume: 29, Issue:19
The development of 2-acetylphenol-donepezil hybrids as multifunctional agents for the treatment of Alzheimer's disease.
AID1517860Inhibition of recombinant human MAO-B expressed in baculovirus infected BTI insect cells using kynuramine as substrate after 30 mins by fluorescence based assay2019European journal of medicinal chemistry, Dec-01, Volume: 183Development of chalcone-O-alkylamine derivatives as multifunctional agents against Alzheimer's disease.
AID1374197Inhibition of recombinant human MAO-A expressed in baculovirus infected BTI insect cells using kynuramine as substrate after 30 mins by fluorescence assay2018Bioorganic & medicinal chemistry, 03-01, Volume: 26, Issue:5
Design, synthesis and evaluation of 4'-OH-flurbiprofen-chalcone hybrids as potential multifunctional agents for Alzheimer's disease treatment.
AID1569978Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate incubated for 15 mins by Ellman's method2019European journal of medicinal chemistry, Oct-15, Volume: 180Design, synthesis, in-silico and biological evaluation of novel chalcone derivatives as multi-function agents for the treatment of Alzheimer's disease.
AID1465287Inhibition of human recombinant MAO-A expressed in baculovirus infected BTI insect cells using kynuramine as substrate after 30 mins by fluorescence assay2017Bioorganic & medicinal chemistry letters, 11-15, Volume: 27, Issue:22
Design, synthesis and biological evaluation of phthalimide-alkylamine derivatives as balanced multifunctional cholinesterase and monoamine oxidase-B inhibitors for the treatment of Alzheimer's disease.
AID1485916Inhibition of recombinant human MAO-B expressed in baculovirus infected BTI insect cells using p-tyramine as substrate pretreated for 15 mins followed by substrate addition after 20 mins by Amplex red reagent based fluorimetric method2017Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
Synthesis and pharmacological evaluation of novel chromone derivatives as balanced multifunctional agents against Alzheimer's disease.
AID1551696Inhibition of recombinant human MAO-A expressed in baculovirus infected BTI insect cells using p-tyramine as substrate preincubated for 60 mins followed by substrate addition and measured after 30 mins by horse-radish peroxidase-coupled amplex red reagent2019European journal of medicinal chemistry, Jul-01, Volume: 173Discovery of coumarin Mannich base derivatives as multifunctional agents against monoamine oxidase B and neuroinflammation for the treatment of Parkinson's disease.
AID1334743Inhibition of human recombinant MAO-A using kynuramine as substrate measured after 30 mins by fluorescence assay2017Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
Multitarget drug design strategy against Alzheimer's disease: Homoisoflavonoid Mannich base derivatives serve as acetylcholinesterase and monoamine oxidase B dual inhibitors with multifunctional properties.
AID1352196Inhibition of recombinant human MAO-B using p-tyramine as substrate preincubated for 15 mins followed by substrate addition measured over 15 mins by Amplex red reagent-based fluorimetric method2018European journal of medicinal chemistry, Feb-10, Volume: 145Design, synthesis and bioevalucation of novel 2,3-dihydro-1H-inden-1-amine derivatives as potent and selective human monoamine oxidase B inhibitors based on rasagiline.
AID125561Binding affinity towards monoamine oxidase A activity was measured using a kynuramine assay2004Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7
Inactivation of purified human recombinant monoamine oxidases A and B by rasagiline and its analogues.
AID1557174Inhibition of human recombinant MAO-B using kynuramine as substrate measured after 30 mins by fluorimetric assay2019Bioorganic & medicinal chemistry letters, 10-01, Volume: 29, Issue:19
The development of 2-acetylphenol-donepezil hybrids as multifunctional agents for the treatment of Alzheimer's disease.
AID1557169Inhibition of electric eel AChE using acetylthiocholine iodide incubated for 15 mins as substrate by Ellman's method2019Bioorganic & medicinal chemistry letters, 10-01, Volume: 29, Issue:19
The development of 2-acetylphenol-donepezil hybrids as multifunctional agents for the treatment of Alzheimer's disease.
AID1192634Inhibition of human recombinant soluble MAO-B assessed as change in melting temperature at 10 uM after 20 mins by SYPRO orange staining-based fluorescence assay2015Bioorganic & medicinal chemistry, Feb-15, Volume: 23, Issue:4
Reversible and irreversible small molecule inhibitors of monoamine oxidase B (MAO-B) investigated by biophysical techniques.
AID1323962Inhibition of recombinant human MAO-A using p-tyramine as substrate assessed as decrease in H2O2 production incubated for 15 mins by fluorimetric method2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Neuroprotective effects of benzyloxy substituted small molecule monoamine oxidase B inhibitors in Parkinson's disease.
AID1706697Inhibition of recombinant human MAO-B expressed in baculovirus infected BTI-TN-5B1-4 insect cells using p-tyramine as substrate preincubated for 15 mins followed by substrate addition and measured over 20 mins by horse-radish peroxidase/Amplex Red coupled2021European journal of medicinal chemistry, Jan-01, Volume: 209Pyrimido[1,2-b]indazole derivatives: Selective inhibitors of human monoamine oxidase B with neuroprotective activity.
AID706469Inhibition of human recombinant MAOA assessed as H2O2 production by Amplex Red reagent-based assay2012Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19
Multitarget-directed benzylideneindanone derivatives: anti-β-amyloid (Aβ) aggregation, antioxidant, metal chelation, and monoamine oxidase B (MAO-B) inhibition properties against Alzheimer's disease.
AID1444066Irreversible inhibition of human cerebral cortex MAO-B using [14C]-phenylethylamin as substrate pretreated for 60 mins followed by substrate addition after 20 mins by liquid scintillation counting method2017European journal of medicinal chemistry, Apr-21, Volume: 130Discovery of highly selective and potent monoamine oxidase B inhibitors: Contribution of additional phenyl rings introduced into 2-aryl-1,3,4-oxadiazin-5(6H)-one.
AID1657140Inhibition of HFIP-pretreated self-induced amyloid beta (1 to 42) (unknown origin) aggregation at 25 uM measured after 24 hrs by ThT fluorescence assay relative to control2020Bioorganic & medicinal chemistry, 04-15, Volume: 28, Issue:8
Design, synthesis and evaluation of phthalide alkyl tertiary amine derivatives as promising acetylcholinesterase inhibitors with high potency and selectivity against Alzheimer's disease.
AID1639030Inhibition of recombinant human MAOB expressed in baculovirus infected BTI insect cells using p-tyramine as substrate preincubated for 30 mins followed by substrate addition and measured over 45 mins by horseradish peroxidase-Amplex Red-coupled fluorometr2019Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7
Novel multi-target directed ligands based on annelated xanthine scaffold with aromatic substituents acting on adenosine receptor and monoamine oxidase B. Synthesis, in vitro and in silico studies.
AID1427514Selectivity index, ratio of IC50 for recombinant human MAO-A expressed in baculovirus infected BTI insect cells to IC50 for recombinant human MAO-B expressed in baculovirus infected BTI insect cells2017Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6
Multifunctional thioxanthone derivatives with acetylcholinesterase, monoamine oxidases and β-amyloid aggregation inhibitory activities as potential agents against Alzheimer's disease.
AID1517864Inhibition of Electric eel AChE using acetylthiocholine iodide as substrate after 15 mins by Ellman's method2019European journal of medicinal chemistry, Dec-01, Volume: 183Development of chalcone-O-alkylamine derivatives as multifunctional agents against Alzheimer's disease.
AID1465286Selectivity index, ratio of IC50 for human serum BChE to IC50 for human erythrocyte AChE2017Bioorganic & medicinal chemistry letters, 11-15, Volume: 27, Issue:22
Design, synthesis and biological evaluation of phthalimide-alkylamine derivatives as balanced multifunctional cholinesterase and monoamine oxidase-B inhibitors for the treatment of Alzheimer's disease.
AID1199581Inhibition of rat brain MAO-B in nuclei-free homogenates using [14C]phenylacetaldehyde substrate after 20 mins by liquid scintillation counting2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Novel arylalkenylpropargylamines as neuroprotective, potent, and selective monoamine oxidase B inhibitors for the treatment of Parkinson's disease.
AID1199586Neuroprotective activity against 6-OHDA-treated rat PC12 cells assessed as survival at 10 uM after 4 hrs by MTT assay (Rvb = 100 +/- 2.31%)2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Novel arylalkenylpropargylamines as neuroprotective, potent, and selective monoamine oxidase B inhibitors for the treatment of Parkinson's disease.
AID1704812Inhibition of equine serum BChE using BTCI as substrate incubated for 5 mins followed by substrate addition and measured after 5 mins by spectrophotometric based Ellman's method
AID1568799Inhibition of self-induced amyloid beta (1 to 42) (unknown origin) aggregation at 25 uM after 24 hrs by thioflavin-T based fluorescence assay relative to control2019European journal of medicinal chemistry, Sep-15, Volume: 178Design, synthesis, in-silico and biological evaluation of novel chalcone-O-carbamate derivatives as multifunctional agents for the treatment of Alzheimer's disease.
AID1334745Inhibition of human recombinant MAO-B using kynuramine as substrate measured after 30 mins by fluorescence assay2017Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
Multitarget drug design strategy against Alzheimer's disease: Homoisoflavonoid Mannich base derivatives serve as acetylcholinesterase and monoamine oxidase B dual inhibitors with multifunctional properties.
AID706470Inhibition of human recombinant MAOB assessed as H2O2 production by Amplex Red reagent-based assay2012Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19
Multitarget-directed benzylideneindanone derivatives: anti-β-amyloid (Aβ) aggregation, antioxidant, metal chelation, and monoamine oxidase B (MAO-B) inhibition properties against Alzheimer's disease.
AID314095Inhibition of MAOB2008Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
Multi-target-directed ligands to combat neurodegenerative diseases.
AID1704814Inhibition of recombinant human MAO-A expressed in baculovirus infected BTI cells at 1 uM using p-tyramine as substrate by fluorometric assay relative to control
AID1740536Inhibition of recombinant human MAOB expressed in baculovirus infected BTI insect cells using p-tyramine as substrate measured after 15 mins by Amplex red reagent based fluorescence assay2020European journal of medicinal chemistry, Sep-15, Volume: 202Design, synthesis and biological evaluation of rasagiline-clorgyline hybrids as novel dual inhibitors of monoamine oxidase-B and amyloid-β aggregation against Alzheimer's disease.
AID1705913Inhibition of recombinant human MAO-B expressed in baculovirus infected BTI insect cells at 1 uM using p-tyramine as substrate preincubated for 30 mins followed by substrate addition and measured after 1 hr by fluorimetric analysis relative to control
AID1569983Selectivity index, ratio of IC50 for recombinant human MAO-A expressed in baculovirus infected BTI insect cells to IC50 for recombinant human MAO-B expressed in baculovirus infected BTI insect cells2019European journal of medicinal chemistry, Oct-15, Volume: 180Design, synthesis, in-silico and biological evaluation of novel chalcone derivatives as multi-function agents for the treatment of Alzheimer's disease.
AID126670Compound was evaluated for inactivation for monoamine oxidase B2004Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7
Inactivation of purified human recombinant monoamine oxidases A and B by rasagiline and its analogues.
AID1465296Inhibition of electric eel AChE using acetylthiocholine as substrate incubated for 15 mins by Ellman's method2017Bioorganic & medicinal chemistry letters, 11-15, Volume: 27, Issue:22
Design, synthesis and biological evaluation of 2-acetyl-5-O-(amino-alkyl)phenol derivatives as multifunctional agents for the treatment of Alzheimer's disease.
AID1704811Inhibition of Electric eel AChE using ATCI as substrate incubated for 5 mins followed by substrate addition and measured after 5 mins by spectrophotometric based Ellman's method
AID1757198Inhibition of human recombinant MAO-A by multimode plate reader assay2021European journal of medicinal chemistry, Apr-15, Volume: 216Design, synthesis and evaluation of novel dimethylamino chalcone-O-alkylamines derivatives as potential multifunctional agents against Alzheimer's disease.
AID1754148Neuroprotective activity against MPTP-induced C57BL/6J mouse model of Parkinson's disease assessed as increase in average speed at 0.2 mg/kg, ip pretreated for 7 consecutive days followed by MPTP challenge and further treated with compound until day 14 by2021Bioorganic & medicinal chemistry letters, 07-01, Volume: 43Novel 1-(prop-2-yn-1-ylamino)-2,3-dihydro-1H-indene-4-thiol derivatives as potent selective human monoamine oxidase B inhibitors: Design, SAR development, and biological evaluation.
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID232325Ratio of A450 decay monoamine oxidase B between kinact and Ki2004Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7
Inactivation of purified human recombinant monoamine oxidases A and B by rasagiline and its analogues.
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1374198Inhibition of recombinant human MAO-B expressed in baculovirus infected BTI insect cells using kynuramine as substrate after 30 mins by fluorescence assay2018Bioorganic & medicinal chemistry, 03-01, Volume: 26, Issue:5
Design, synthesis and evaluation of 4'-OH-flurbiprofen-chalcone hybrids as potential multifunctional agents for Alzheimer's disease treatment.
AID1323967Neuroprotective activity against rotenone-induced toxicity in rat PC12 cells assessed as cell survival at 20 uM preincubated for 24 hrs followed by rotenone addition measured after 24 hrs by MTT assay relative to control2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Neuroprotective effects of benzyloxy substituted small molecule monoamine oxidase B inhibitors in Parkinson's disease.
AID1421880Inhibition of human recombinant MAOB expressed in baculovirus infected BTI-TN-5B1- 4 cells using p-tyramine as substrate assessed as decrease in H2O2 production by amplex red-based fluorescence assay2018European journal of medicinal chemistry, Oct-05, Volume: 158Multi-target-directed ligands for Alzheimer's disease: Discovery of chromone-based monoamine oxidase/cholinesterase inhibitors.
AID1754146Neuroprotective activity against LPS-induced oxidative stress in C57/BL6 mouse BV-2 cells assessed as decrease in ROS level at < 20 uM after 24 hrs by DCFH-DA dye based fluorescence assay2021Bioorganic & medicinal chemistry letters, 07-01, Volume: 43Novel 1-(prop-2-yn-1-ylamino)-2,3-dihydro-1H-indene-4-thiol derivatives as potent selective human monoamine oxidase B inhibitors: Design, SAR development, and biological evaluation.
AID1704810Displacement of [3H]N-alpha-methylhistamine from recombinant human histamine H3 receptor expressed in CHO-K1 cells by microbeta scintillation analysis
AID1569982Inhibition of recombinant human MAO-B expressed in baculovirus infected BTI insect cells using kynuramine as substrate incubated for 30 mins by fluorescence based assay2019European journal of medicinal chemistry, Oct-15, Volume: 180Design, synthesis, in-silico and biological evaluation of novel chalcone derivatives as multi-function agents for the treatment of Alzheimer's disease.
AID1705911Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method
AID1907519Inhibition of human recombinant MAO-B using p-tyramine as substrate preincubated for 30 mins followed by substrate addition and measured after 1 hr by fluorometric analysis2022European journal of medicinal chemistry, Jun-05, Volume: 236Overcoming undesirable hERG affinity by incorporating fluorine atoms: A case of MAO-B inhibitors derived from 1 H-pyrrolo-[3,2-c]quinolines.
AID1657151Inhibition of recombinant human MAO-B expressed in baculovirus infected BTI insect cells using kynuramine as substrate measured after 30 mins by fluorescence based assay2020Bioorganic & medicinal chemistry, 04-15, Volume: 28, Issue:8
Design, synthesis and evaluation of phthalide alkyl tertiary amine derivatives as promising acetylcholinesterase inhibitors with high potency and selectivity against Alzheimer's disease.
AID1436076Inhibition of recombinant human MAO-A expressed in baculovirus infected BTI insect cells using kynuramine as substrate incubated for 30 mins by fluorescence assay2017European journal of medicinal chemistry, Jan-27, Volume: 126Aurone Mannich base derivatives as promising multifunctional agents with acetylcholinesterase inhibition, anti-β-amyloid aggragation and neuroprotective properties for the treatment of Alzheimer's disease.
AID1691659Inhibition of self-induced Amyloid beta (1 to 42 residues) (unknown origin) aggregation at 25 uM measured after 24 hrs by thioflavin T-based fluorimetric assay relative to control2020European journal of medicinal chemistry, May-15, Volume: 194Design, synthesis and biological evaluation of novel O-carbamoyl ferulamide derivatives as multi-target-directed ligands for the treatment of Alzheimer's disease.
AID126544Compound was evaluated for A 450 decay towards monoamine oxidase B enzyme2004Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7
Inactivation of purified human recombinant monoamine oxidases A and B by rasagiline and its analogues.
AID1532335Inhibition of human MAO-B expressed in baculovirus infected BTI insect cells using p-tyramine as substrate preincubated for 30 mins followed by substrate addition and measured after 1 hr by fluorescence-based Amplex Red MAO assay2018Bioorganic & medicinal chemistry letters, 12-15, Volume: 28, Issue:23-24
4-tert-Pentylphenoxyalkyl derivatives - Histamine H
AID1465303Inhibition of recombinant human MAO-B using kynuramine as substrate after 30 mins by fluorescence method2017Bioorganic & medicinal chemistry letters, 11-15, Volume: 27, Issue:22
Design, synthesis and biological evaluation of 2-acetyl-5-O-(amino-alkyl)phenol derivatives as multifunctional agents for the treatment of Alzheimer's disease.
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1754140Inhibition of human MAO-B2021Bioorganic & medicinal chemistry letters, 07-01, Volume: 43Novel 1-(prop-2-yn-1-ylamino)-2,3-dihydro-1H-indene-4-thiol derivatives as potent selective human monoamine oxidase B inhibitors: Design, SAR development, and biological evaluation.
AID1757199Selectivity index, ratio of IC50 for recombinant human MAO-A to IC50 for recombinant human MAO-B2021European journal of medicinal chemistry, Apr-15, Volume: 216Design, synthesis and evaluation of novel dimethylamino chalcone-O-alkylamines derivatives as potential multifunctional agents against Alzheimer's disease.
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1691661Selectivity index, ratio of IC50 for recombinant human MAO-A to IC50 for recombinant human MAO-B2020European journal of medicinal chemistry, May-15, Volume: 194Design, synthesis and biological evaluation of novel O-carbamoyl ferulamide derivatives as multi-target-directed ligands for the treatment of Alzheimer's disease.
AID1586576Selectivity index, ratio of IC50 for human recombinant MAO-A expressed in baculovirus infected BTI-TN-5B1-4 insect cells to IC50 for human recombinant MAO-B expressed in baculovirus infected BTI-TN-5B1-4 insect cells2019European journal of medicinal chemistry, Jan-15, Volume: 162(Pyrrolo-pyridin-5-yl)benzamides: BBB permeable monoamine oxidase B inhibitors with neuroprotective effect on cortical neurons.
AID1292320Inhibition of human recombinant MAO-A using kynuramine as substrate after 30 mins by fluorescence spectrophotometry2016Bioorganic & medicinal chemistry, 05-15, Volume: 24, Issue:10
Synthesis and evaluation of 4-hydroxyl aurone derivatives as multifunctional agents for the treatment of Alzheimer's disease.
AID1421899Irreversible inhibition of human recombinant microsomal MAOB expressed in baculovirus infected BTI-TN-5B1- 4 cells using p-tyramine as substrate assessed as decrease in H2O2 production at IC80 after 15 mins2018European journal of medicinal chemistry, Oct-05, Volume: 158Multi-target-directed ligands for Alzheimer's disease: Discovery of chromone-based monoamine oxidase/cholinesterase inhibitors.
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1345977Human Monoamine oxidase B (Catecholamine turnover)2001British journal of pharmacology, Jan, Volume: 132, Issue:2
Rasagiline [N-propargyl-1R(+)-aminoindan], a selective and potent inhibitor of mitochondrial monoamine oxidase B.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (516)

TimeframeStudies, This Drug (%)All Drugs %
pre-19907 (1.36)18.7374
1990's14 (2.71)18.2507
2000's145 (28.10)29.6817
2010's277 (53.68)24.3611
2020's73 (14.15)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials72 (13.46%)5.53%
Reviews108 (20.19%)6.00%
Case Studies34 (6.36%)4.05%
Observational5 (0.93%)0.25%
Other316 (59.07%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (56)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Evaluation of the Tolerance and Acceptability of Rasagiline in the Treatment of Early-stage Parkinson's Disease[NCT01048229]Phase 4112 participants (Actual)Interventional2008-10-31Terminated(stopped due to recruitment)
A Randomized, Double-Blind, Placebo-Controlled, Parallel Group Study to Assess the Efficacy, Safety and Tolerability of Rasagiline in Subjects With Progressive Supranuclear Palsy (Phase III)[NCT01187888]Phase 344 participants (Actual)Interventional2010-01-31Terminated(stopped due to IMP used off label by phys. in pat. with PSP. Thus no more eligible patients were available for the study(pre-treatm.with Rasagiline=exclusion criterion)
Safety and Efficacy of Rasagiline in Restless Legs Syndrome[NCT01192503]Phase 2/Phase 352 participants (Actual)Interventional2010-09-30Terminated(stopped due to Slow enrollment)
Effect of 2.5 Years of Rasagiline Therapy on Progression of Cognitive Biomarkers Assessed by MRI in Parkinson's Disease.[NCT02278588]45 participants (Actual)Observational2014-11-30Completed
Spontaneous and Evoked Pain in Parkinson's Disease With Motor Fluctuations: an Observational, Prospective, Clinical and Neurophysiological Study in Patients Under L-dopa Add on Therapies.[NCT03648671]48 participants (Anticipated)Observational2018-03-28Recruiting
Efficacy and Safety of Rasagiline in Prodromal Parkinson's Disease[NCT05611372]Phase 2/Phase 3732 participants (Anticipated)Interventional2023-01-01Not yet recruiting
A Multicenter, Randomized, Double-blind Placebo Controlled Study to Assess the Effect of Rasagiline on Sleep-wake Disturbances in Patients With Parkinson's Disease (PD)[NCT01178047]Phase 41 participants (Actual)Interventional2011-09-30Terminated(stopped due to payments stopped by grant provider)
[NCT01382342]Phase 450 participants (Actual)Interventional2011-06-30Completed
A Multi-centered, Randomized, Double-blind, Placebo-controlled Clinical Trial to Assess the Efficacy, Safety, and Tolerability of Rasagiline Mesylate 1 mg in Patients With Multiple System Atrophy of the Parkinsonian Subtype (MSA-P)[NCT00977665]Phase 2174 participants (Actual)Interventional2009-12-31Completed
Rasagiline (Azilect) - Neuroprotection for Macula-off Retinal Detachment[NCT02068625]Phase 423 participants (Actual)Interventional2010-09-30Terminated(stopped due to Persisting recruitment difficulties)
Investigation of the Occurrence of Serotonin Toxicity in Parkinson's Disease (PD) Patients Treated Concomitantly With Rasagiline and Antidepressants, Using Retrospective Chart Review[NCT00955604]1,500 participants (Anticipated)Observational2009-07-31Completed
A Randomised Placebo-controlled Trial of Rasagiline in Parkinson Disease Patients With Symptoms of Apathy[NCT00755027]Phase 440 participants (Actual)Interventional2008-09-30Completed
A Sensorimotor Contingency-based Musical Walking Program for People Living With Parkinson's Disease[NCT02207387]60 participants (Anticipated)Interventional2013-10-31Recruiting
Reversibility of Olfactory Loss in Patients With Idiopathic Parkinson's Disease Following Treatment With Rasagiline[NCT00902941]Phase 434 participants (Actual)Interventional2009-05-31Completed
Efficacy, Safety and Tolerability Study of 1 mg Rasagiline in Patients With Amyotrophic Lateral Sclerosis (ALS) Receiving Standard Therapy (Riluzole) - An AMG Trial With a Market Authorized Substance[NCT01879241]Phase 2252 participants (Actual)Interventional2013-06-30Completed
A Prospective Randomized Placebo-Controlled Double-Blind Study Assessing Change in Olfactory Function After Initiation of Rasagiline in Idiopathic Parkinson's Disease[NCT01007630]Phase 436 participants (Anticipated)Interventional2009-11-30Active, not recruiting
The Effects of Rasagiline on Cognitive Deficits Associated With Parkinson's Disease: A Randomized, Double-Blind, Placebo-Controlled, Multi-Center Study Over 3 Months[NCT00696215]Phase 440 participants (Anticipated)Interventional2007-06-30Recruiting
A Phase 3, 40-Week, Active-Controlled, Double-Blind, Double-Dummy Extension Study of Preladenant in Subjects With Moderate to Severe Parkinson's Disease (Phase 3, Protocol No. P06153)[NCT01215227]Phase 3839 participants (Actual)Interventional2010-11-18Terminated
Rasagiline for the Symptomatic Treatment of Fatigue in Parkinson's Disease: A Bi-Center, Placebo-Controlled Study (The REST Fatigue Trial)[NCT01168596]Phase 430 participants (Actual)Interventional2009-12-31Completed
A Phase 3, Double-Blind, Double-Dummy, Placebo- and Active-Controlled Dose-Range-Finding Efficacy and Safety Study of Preladenant in Subjects With Early Parkinson's Disease[NCT01155479]Phase 31,022 participants (Actual)Interventional2010-07-06Terminated(stopped due to Termininated for business reasons)
An Open-Label, Multi-Center, Follow-Up Study Designed to Evaluate the Long-Term Effects of Rasagiline in Parkinson's Disease Subjects Who Participated in the ADAGIO Study[NCT00936676]684 participants (Actual)Observational2009-07-31Completed
Effects of Azilect (Rasagiline) on Processing of Emotions, Mood and Executive Function in Parkinson's Disease[NCT01385735]Phase 470 participants (Anticipated)Interventional2011-10-31Not yet recruiting
A Phase 2B, Twelve-week Multi-Center, Randomized, Double-Blind, Placebo-Controlled, Parallel Group Study, To Determine the Safety, Tolerability and Efficacy of Two Doses of Once Daily P2B001 in Subjects With Early Parkinson's Disease[NCT01968460]Phase 2/Phase 3149 participants (Actual)Interventional2013-12-31Completed
Evaluation for the Efficacy,Tolerability,and Safety of Rasagiline in Levodopa-treated PD Patients With Motor Fluctuations: A Multicenter, Double Blind, Randomized, Placebo-Controlled Group Study (China)[NCT01736891]Phase 3268 participants (Actual)Interventional2011-11-30Completed
A Randomised, Double-blind, Placebo-controlled Study to Evaluate if Rasagiline Can Improve Depressive Symptoms and Cognitive Function in Non-demented, Idiopathic Parkinson's Disease Patients: ACCORDO Study[NCT01055379]Phase 4121 participants (Actual)Interventional2010-03-31Completed
An Open-Label, Multi-Center, Single Arm Study to Evaluate the Effects of Azilect® on Sleep Disturbances in Parkinson's Disease Subjects[NCT01032486]120 participants (Actual)Observational2009-12-31Completed
A Multi Center, Double Blind, Randomized Start, Placebo-Controlled, Parallel-Group Study to Assess Rasagiline as a Disease Modifying Therapy in Early Parkinson's Disease Subjects[NCT00256204]Phase 31,174 participants (Actual)Interventional2005-11-30Completed
A Randomized, Double-Blind, Placebo-Controlled, Study to Assess the Pharmacokinetics, Safety, and Tolerability of Single and Multiple Doses (0.5, 1.0, and 2.0 mg) of Rasagiline Administered to Healthy Japanese and Caucasian Subjects[NCT01879748]Phase 164 participants (Actual)Interventional2013-06-30Completed
A Multicenter, Double-Blind, Placebo-Controlled, Parallel Group, Phase III Clinical Trial For The Efficacy, Tolerability And Safety Of Two Doses Of Rasagiline Mesylate In Early Parkinson's Disease (PD) Patients Not Treated With Levodopa[NCT00203060]Phase 3404 participants (Actual)Interventional1997-07-31Completed
A Multicenter, Open-Label, Phase III Study for the Safety, Tolerability and Clinical Effect of Rasagiline Mesylate in Patients With Parkinson's Disease[NCT00203138]Phase 3306 participants (Actual)Interventional2004-06-30Completed
A Bi-national, Multicenter, Double-Blind, Randomized Study to Evaluate the Safety and Tolerability of Rasagiline Mesylate in Advanced Parkinson's Disease (PD) Patients With Motor Fluctuations Treated With Chronic Levodopa/Carbidopa Therapy.[NCT00203177]Phase 3254 participants (Actual)Interventional2001-10-31Completed
A Phase 3, Twelve-week Study to Determine the Efficacy, Safety and Tolerability of P2B001 Once Daily Compared to Its Individual Components in Subjects With Early Parkinson's Disease and to a Calibration Arm of Pramipexole ER.[NCT03329508]Phase 3544 participants (Actual)Interventional2018-01-19Completed
A Phase 3, 12-Week, Double-Blind, Double-Dummy, Placebo- and Active-Controlled Efficacy and Safety Study of Preladenant in Subjects With Moderate to Severe Parkinson's Disease (Phase 3;Protocol No. P04938)[NCT01155466]Phase 3778 participants (Actual)Interventional2010-07-14Completed
Azilect® In Wearing-Off (AIWO) Non-interventional Study on Efficacy and Tolerability of Rasagiline (1mg/d) add-on in Ambulatory Parkinson's Disease Patients With Wearing-off Symptoms Diagnosed by Wearing-off Questionnaire (WOQ-32)[NCT02384512]261 participants (Actual)Observational2014-01-31Completed
A Multi-Center Controlled Screening Trial of Safety and Efficacy of Rasagiline in Subjects With Amyotrophic Lateral Sclerosis (ALS)[NCT01232738]Phase 236 participants (Actual)Interventional2011-12-31Completed
A Multicenter, US and Canada, Double Blind, Randomized, Placebo-Controlled, Parallel Group Study, for the Efficacy, Tolerability and Safety of Rasagiline Mesylate in Levodopa Treated Parkinson's Disease Patients With Motor Fluctuations[NCT00203034]Phase 3472 participants (Actual)Interventional2000-05-31Completed
Image Parkinson's Disease Progression Study[NCT02789020]Phase 296 participants (Actual)Interventional2016-12-31Completed
Randomised, Double-blind, Parallel-group, Placebo-controlled, Fixed-dose Study of [Azilect®] Rasagiline in Levodopa-treated Parkinson's Patients With Motor Fluctuations in China[NCT01479530]Phase 3321 participants (Actual)Interventional2011-12-31Completed
A 1-Year, Double-Blind, Randomized, Placebo-Controlled, Study of Rasagiline 1 mg and 2 mg Added to Aricept 10 mg Daily in Patients With Mild to Moderate Dementia of the Alzheimer's Type[NCT00104273]Phase 2376 participants (Actual)Interventional2004-08-31Completed
Rasagiline in the Treatment of Persistent Negative Symptoms of Schizophrenia[NCT00492336]Phase 484 participants (Actual)Interventional2007-01-31Completed
Randomised, Double-blind, Parallel-group, Placebo-controlled, Fixed-dose Study of [Azilect®] Rasagiline in Levodopa-treated Parkinson's Patients With Motor Fluctuations in Korea[NCT01268891]Phase 3132 participants (Actual)Interventional2011-01-31Completed
Sub-study to Evaluate the Effect of An Oral Dose of Tyramine in Subjects Completing 26 Weeks of Participation in PRESTO (TVP-1012/133)[NCT00203125]Phase 355 participants (Actual)Interventional2000-10-31Completed
A Bi-national, Multicenter, Double-Blind, Randomized Study to Evaluate the Safety and Tolerability of Rasagiline Mesylate in Advanced Parkinson's Disease (PD) Patients With Motor Fluctuations Treated With Chronic Levodopa/Carbidopa Therapy[NCT00203164]Phase 3254 participants (Actual)Interventional2002-05-31Completed
Open-label, Multicenter, Effectiveness and Safety Study of Once Daily AZILECT® as Mono- or Adjunct Therapy in Patients With Idiopathic Parkinson's Disease (PD)[NCT00399477]Phase 4200 participants (Actual)Interventional2006-10-31Completed
"AZILECT Tablets Special Drug Use-Results Survey Survey on Long-term Safety"[NCT03727139]1,021 participants (Actual)Observational2018-11-01Completed
Effect of Rasagiline on BIA 9-1067 Pharmacokinetics in Healthy Subjects[NCT01532141]Phase 125 participants (Actual)Interventional2009-11-30Completed
A Double Blind Placebo Controlled Trial Evaluating Rasagiline Effects on Cognition in Parkinson's Disease Patients With Mild Cognitive Impairment Receiving Dopaminergic Therapy[NCT01497652]Phase 434 participants (Actual)Interventional2012-01-31Completed
A Double-blind, Placebo Controlled, Randomized, Multicenter Study to Assess the Safety and Clinical Benefit of Rasagiline as an Add on Therapy to Stable Dose of Dopamine Agonists in the Treatment of Early Parkinson's Disease[NCT01049984]Phase 4328 participants (Actual)Interventional2009-12-31Completed
A Single Centre, Open-label, Multiple-dose Interventional Study Investigating the Pharmacokinetic Properties of Rasagiline (Lu 00-773) in Healthy Young Chinese Men and Women[NCT01652313]Phase 112 participants (Actual)Interventional2012-05-31Completed
Evaluation of the Efficacy of Rasagiline in Apathy in Drug-naïve Patients With Parkinson's Disease by a Multi-center, Randomized, Double-blind, Parallel-group, Placebo-controlled Study.[NCT01765257]Phase 450 participants (Anticipated)Interventional2013-06-30Not yet recruiting
Effects of Rasagiline on Sleep Disturbances in PD: A Single Center, Randomized, Double-blind, Placebo run-in, Polysomnographic Clinical Phase IV Trial[NCT01442610]Phase 430 participants (Actual)Interventional2011-10-31Completed
Randomised, Double-blind, Parallel-group, Placebo-controlled, Fixed-dose Study of Rasagiline in Early Parkinson's Disease Patients Not Treated With Levodopa in China[NCT01556165]Phase 3130 participants (Actual)Interventional2012-04-30Completed
A 24-Week, Multicenter, Randomized, Double-blind, Placebo-Controlled, Add-on, Parallel-Group Study to Assess the Effect of Rasagiline on Cognition in Patients With Parkinson's Disease[NCT01723228]Phase 4170 participants (Actual)Interventional2012-11-30Completed
Phase 2 Study of Rasagiline for Treatment of Amyotrophic Lateral Sclerosis[NCT01786603]Phase 280 participants (Actual)Interventional2013-11-21Completed
Effect of BIA 9-1067 on Rasagiline Pharmacokinetics in Healthy Subjects[NCT01532128]Phase 124 participants (Actual)Interventional2009-11-30Completed
A 24-week, Three-site, Randomized, Double Blind, Placebo Controlled, Parallel Group, Proof-of-concept Study to Evaluate Rasagiline in the Regional Brain Metabolism on FDG PET in Patients With Mild to Moderate Alzheimer's Disease[NCT02359552]Phase 250 participants (Actual)Interventional2015-05-31Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

Change From Baseline to Week 12 in Total UMSARS Score for Symptomatic Effect

This outcome represents the sum of 2 UMSARS sub-scales: Part I: Historical Review that includes 12 items and Part II: Motor Examination that includes 14 items. All items range from 0 to 4. Each subscale score is the sum of its items and the total UMSARS score is the sum of all 26 items. Hence the total UMSARS score can range from 0 to 104, with 0 meaning no impairment and 104 indicating severe impairment. Negative change from baseline scores indicate improvement. (NCT00977665)
Timeframe: Day 0 (baseline), Week 12

Interventionunits on a scale (Mean)
Rasagiline Mesylate1.875
Placebo1.574

Change From Baseline to Week 24 in Total Unified Multiple System Atrophy Rating Scale (UMSARS) Score

"The UMSARS is composed of 2 sub-scales: Part I: Historical Review that includes 12 items and Part II: Motor Examination that includes 14 items. All items range from 0 to 4. Each subscale score is the sum of its items and the total UMSARS score is the sum of all 26 items. Hence the total UMSARS score can range from 0 to 104, with 0 meaning no impairment and 104 indicating severe impairment. Negative change from baseline scores indicate improvement.~In the case that 6 items or more (out of 26) were missing at a certain visit, the UMSARS score for that visit was assigned a missing value." (NCT00977665)
Timeframe: Day 0 (baseline), Week 24

Interventionunits on a scale (Least Squares Mean)
Rasagiline Mesylate3.8
Placebo3.0

Change From Baseline to Week 48 or Termination in the Beck Depression Inventory Scale (BDI-II)

The Beck Depression Inventory (BDI-II), is a 21-question multiple-choice self-report inventory, one of the most widely used instruments for measuring the severity of depression. Participants are asked to pick the answer for each question that best describes the way they have been feeling in the past two weeks, including the day participants complete the questionnaire. Each question is rated on a scale of 0-3, with 0 meaning the participant does not feel the emotion described in the question, and 3 meaning the participant has extremely strong feelings. Total scale is 0 (no evidence of depression) to 63 (extreme depression). Negative change from baseline scores indicate improvement in level of depression. (NCT00977665)
Timeframe: Day 0 (baseline), Week 48 or termination visit

Interventionunits on a scale (Least Squares Mean)
Rasagiline Mesylate0.4894
Placebo0.7145

Change From Baseline to Week 48 or Termination in the Montreal Cognitive Assessment Scale (MoCA) Scale

MoCA is a cognitive screening test which helps health professionals identify mild cognitive impairment. The total scale is 0 (significant cognitive impairment) to 30 (no impairment detected). Scores >=26 are considered normal. Positive change from baseline scores indicate improvement in cognition. (NCT00977665)
Timeframe: Day 0 (baseline), Week 48 or termination visit

Interventionunits on a scale (Least Squares Mean)
Rasagiline Mesylate-1.1572
Placebo-0.5786

Change From Baseline to Week 48/Termination Visit in the Multiple System Atrophy (MSA) Health-related Quality of Life (QoL) Scale

"The Multiple System Atrophy Quality of Life questionnaire (MSA-QoL) is a self-reported questionnaire focusing on MSA-specific symptoms and has a scale ranging from 0 - 160, with 0= 'no problem' and 160= extreme problem." (NCT00977665)
Timeframe: Day 0 (baseline), Week 48

Interventionunits on a scale (Least Squares Mean)
Rasagiline Mesylate4.6
Placebo9.3

Change From Baseline to Week 48/Termination Visit in the Total Unified Multiple System Atrophy Rating Scale (UMSARS Part I and II)

"This outcome represents the sum of 2 UMSARS sub-scales: Part I: Historical Review that includes 12 items and Part II: Motor Examination that includes 14 items. All items range from 0 to 4. Each subscale score is the sum of its items and the total UMSARS score is the sum of all 26 items. Hence the total UMSARS score can range from 0 to 104, with 0 meaning no impairment and 104 indicating severe impairment. Negative change from baseline scores indicate improvement.~In the case that 6 items or more (out of 26) were missing at a certain visit, the UMSARS score for that visit was assigned a missing value." (NCT00977665)
Timeframe: Day 0 (baseline), Week 48

Interventionunits on a scale (Least Squares Mean)
Rasagiline Mesylate7.2
Placebo7.8

Clinical Global Impression Improvement (CGI-I) at Week 48/Termination Visit

"Outcome measures the investigator's clinical impression of the participants' improvement at Week 48 as compared to Week 12. CGI scale range from 1-7, with 1=very much improved, 4= no change, and 7=very much worse.~In order to maintain the overall (hypotheses about primary and key secondary endpoints) type I error at the 0.05 level an hierarchy will be employed as follows: If the primary endpoint will be found to be significant at a significance level of 0.05 then the first key secondary endpoint will be tested, if this endpoint will be found to be significant in a significance level of 0.05 then the second key secondary endpoint will be tested and so on. The 'key' secondary endpoints are outcomes 2-6." (NCT00977665)
Timeframe: Week 48

Interventionunits on a scale (Least Squares Mean)
Rasagiline Mesylate4.9
Placebo4.8

Estimates for Time to Change in Anti-Parkinsonian or Anti-Orthostatis Hypotension Medications

"Change in anti-parkinsonian or anti-orthostatic hypotension medication is defined by at least one of the following events:~An addition of a new anti-parkinsonian or anti-orthostatic hypotension medication during study.~Dose modification of anti-parkinsonian or anti-orthostatic hypotension concomitant medications reflecting disease progression.~The event of interest, determined on a by patient basis, therefore, is the earliest event of the two events defined above. Otherwise, patient is right censored according to his/her study termination date.~Since less than 25% of participants had an event, median estimatation for time to change in medications is not possible." (NCT00977665)
Timeframe: Day 0 (baseline) to Week 48 or termination visit

Interventiondays (Median)
Rasagiline Mesylate246
Placebo294

Mean Score of the Composite Autonomic Symptom Scale Select (COMPASS_Select Change) at Week 48/Termination Visit

COMPASS_Select change is comprised of 5 of the 11 domains in the COMPASS scale: Orthostatic Intolerance, Bladder Disorder, Sweating, Vasomotor, and Sleep Disorder COMPASS_Select change has a range of -150 to 150, with -150 indicating symptoms are much better and 150 indicating symptoms are much worse. (NCT00977665)
Timeframe: 48 weeks

Interventionunits on a scale (Least Squares Mean)
Rasagiline Mesylate34.1
Placebo42.7

Percentage of Participants Who Achieved a Score of >=3 on the Unified Multiple System Atrophy Rating Scale (UMSARS) Question #7 Regarding Ambulation

UMSARS' Question #7 concerns the participant's ability to walk, rated on a scale of 0=normal to 4=cannot walk at all even with assistance. This endpoint counts participants rated a 3 or worse. Rating 3 = Severely impaired; assistance and/or walking aid needed occasionally. (NCT00977665)
Timeframe: up to week 48

Interventionpercentage of participants (Number)
Rasagiline Mesylate46.4
Placebo52.2

Rate of Progression in Total Unified Multiple System Atrophy Rating Scale (UMSARS) Score From Baseline to Weeks 12-48

"The UMSARS is composed of 2 sub-scales: Part I: Historical Review that includes 12 items and Part II: Motor Examination that includes 14 items. All items range from 0 to 4. Each subscale score is the sum of its items and the total UMSARS score is the sum of all 26 items. Hence the total UMSARS score can range from 0 to 104, with 0 meaning no impairment and 104 indicating severe impairment.~The rate of progression of atrophy is represented by the slope of change from baseline scores for visits between Weeks 12 and 48." (NCT00977665)
Timeframe: Day 0 (baseline), Weeks 12-48

Interventionunits on a scale/week (Mean)
Rasagiline Mesylate0.1496
Placebo0.1788

Total Number of Falls During the Study

Participants recorded each time they fell during the study in a diary. (NCT00977665)
Timeframe: Day 1 up to week 48

Interventionfalls (Median)
Rasagiline Mesylate4.00
Placebo5.00

Change From Baseline to Week 48 or Termination in UMSARS Subscores for Parts I, II and IV

UMSARS Part I is an historical review and scores symptoms of neurological and autonomic dysfunction with 12 items rated on a scale of 0 (normal) to 4 (extreme dysfunction). The full scale for Part 1 is therefore 0 (normal) to 48 (extreme dysfunction). Part II is a motor examination and has 14 items also rated on a scale of 0 to 4 for a full scale of 0 (normal) to 56 (extreme dysfunction). Part IV is a global disability scale with rates the extent of disease from 1 (normal) to 5 (severe disease). (NCT00977665)
Timeframe: Day 0 (baseline), Week 48 or termination visit

,
Interventionunits on a scale (Least Squares Mean)
UMSARS Part IUMSARS Part IIUMSARS Part IV
Placebo4.37853.50680.6763
Rasagiline Mesylate3.82333.64780.7100

Percentage of Participants Who Achieved a Score of >=3 on the Unified Multiple System Atrophy Rating Scale (UMSARS) Question #1 (Speech Impairment), Question #2 (Swallowing Impairment) and Question #8 (Falling)

"UMSARS' questions are rated on a scale of 0=normal to 4=extreme impairment.~This endpoint reports the percentage of participants rated a 3 or worse. Rating 3 = Severely impaired speech (Question #1), swallowing (Question #2) or falling more frequently than once per week (Question #8)." (NCT00977665)
Timeframe: up to week 48

,
Interventionpercentage of participants (Number)
Q1. Speech ImpairmentQ2. Swallowing ImpairmentQ8. Falling
Placebo30.06.715.6
Rasagiline Mesylate35.73.619.0

Percentage Change From Baseline in Total Epworth Sleepiness Scale (ESS) Score at Week 40

The ESS is a self-administered questionnaire providing a measure of a person's general level of daytime sleepiness, or their average sleep propensity in daily life. The scale consists of 8 situations in which the participant rates their tendency to become sleepy on a scale of 0=no chance of dozing to 3=high chance of dozing. The overall score is the sum of the scores for the 8 situations for a minimum of 0 and a maximum of 24 with a higher score indicating greater sleepiness. (NCT01215227)
Timeframe: Baseline and Week 40

InterventionPercentage change (Mean)
Preladenant 2 mg15.5
Preladenant 5 mg24.0
Preladenant 5 mg (on Placebo in Parent Study)22.5
Preladenant 10 mg13.2
Rasagiline 1 mg8.3
Rasagiline 1 mg (on Placebo in Parent Study)16.3

Percentage of Participants With Alanine Aminotransferase (ALT) ≥3 Times Upper Limit of Normal and ≥10% Increase From Baseline

The number of participants with ALT ≥3 times the upper limit of normal and a ≥10% increase was reported. Laboratory safety blood work was collected from participants at Week 4, Week 6, and Week 8 visits. (NCT01215227)
Timeframe: Up to 42 weeks

InterventionPercentage of participants (Number)
Preladenant 2 mg1.4
Preladenant 5 mg0.5
Preladenant 5 mg (on Placebo in Parent Study)0.0
Preladenant 10 mg1.0
Rasagiline 1 mg0.0
Rasagiline 1 mg (on Placebo in Parent Study)1.9

Percentage of Participants With Aspartate Aminotransferase (AST) ≥3 Times Upper Limit of Normal and ≥10% Increase From Baseline

The number of participants with AST ≥3 times the upper limit of normal and a ≥10% increase was reported. Laboratory safety blood work was collected from participants at Week 4, Week 6, and Week 8 visits. (NCT01215227)
Timeframe: Up to 42 weeks

InterventionPercentage of participants (Number)
Preladenant 2 mg1.4
Preladenant 5 mg0.5
Preladenant 5 mg (on Placebo in Parent Study)0.0
Preladenant 10 mg2.1
Rasagiline 1 mg1.1
Rasagiline 1 mg (on Placebo in Parent Study)2.8

Percentage of Participants With Diastolic Blood Pressure ≥105 mmHg

The percentage of participants with Diastolic Blood Pressure ≥105 mmHg was reported. On Day 1 and Early Termination, blood pressure was measured as follows: Participant lay supine for 5 minutes, then had blood pressure taken; then stood for 3 minutes and had blood pressure taken; then rested for 10 minutes, at which time the process was repeated twice (ie, three rounds total). For all other blood pressure measurements, the procedure needed only to be done once (ie, one round). (NCT01215227)
Timeframe: Up to 42 weeks

InterventionPercentage of participants (Number)
Preladenant 2 mg5.0
Preladenant 5 mg4.2
Preladenant 5 mg (on Placebo in Parent Study)5.7
Preladenant 10 mg5.2
Rasagiline 1 mg7.5
Rasagiline 1 mg (on Placebo in Parent Study)8.3

Percentage of Participants With Suicidality

The number of participants with suicidality using the Columbia - Suicide Severity Rating Scale (C-SSRS) was reported. The C-SSR was used in this study only for the purpose of safety monitoring by measuring the incidence of different types of suicidality categories during treatment. The assessment was done by the nature of the responses, not by a numbered scale. Participants who reported at least one occurrence of suicidal behavior or suicidal ideation were counted as having experienced suicidality. Suicidal behavior included suicide attempt, aborted attempt, interrupted attempt, or preparatory behavior. Suicidal ideation included a wish to die or active suicidal thought with or without method, intent or plan. (NCT01215227)
Timeframe: Up to 42 weeks

InterventionPercentage of participants (Number)
Preladenant 2 mg4.1
Preladenant 5 mg5.6
Preladenant 5 mg (on Placebo in Parent Study)0.0
Preladenant 10 mg4.2
Rasagiline 1 mg2.2
Rasagiline 1 mg (on Placebo in Parent Study)2.8

Percentage of Participants With Systolic Blood Pressure ≥180 mmHg

The percentage of participants with Systolic Blood Pressure ≥180 mm Hg was reported. On Day 1 and Early Termination, blood pressure was measured as follows: Participant lay supine for 5 minutes, then had blood pressure taken; then stood for 3 minutes and had blood pressure taken; then rested for 10 minutes, at which time the process was repeated twice (ie, three rounds total). For all other blood pressure measurements, the procedure needed only to be done once (ie, one round). (NCT01215227)
Timeframe: Up to 42 weeks

InterventionPercentage of participants (Number)
Preladenant 2 mg1.4
Preladenant 5 mg0.0
Preladenant 5 mg (on Placebo in Parent Study)0.9
Preladenant 10 mg1.0
Rasagiline 1 mg0.0
Rasagiline 1 mg (on Placebo in Parent Study)0.9

Becks Depression Inventory (BDI-II)

The Becks Depression Inventory (BDI-II) is a 21-question inventory measuring the severity of depression. Each subject is instructed to choose an answer on a scale value of 0 to 3 with the total score from 0 to 63. Higher total scores indicate more severe depressive symptoms. (NCT01168596)
Timeframe: Change from baseline to week 12

Interventionunits on a scale (Mean)
Rasagiline3.69
Sugar Pill2.31

Fatigue Severity Scale (FSS)

The Fatigue Severity Score consists of a nine-item questionnaire to identify common features of fatigue. Patients are instructed to choose a number from 1 to 7 that indicates their degree of agreement with each statement, where 1 = strongly disagree and 7 = strongly agree. Scores can range from a minimum of 9 to a maximum of 63. The higher the score, the more fatigue the subject. (NCT01168596)
Timeframe: Change from baseline to week 12

Interventionunits on a scale (Mean)
Rasagiline12.38
Sugar Pill2.25

Finger Tapping

The patient is asked to use the index finger on the side most affected by Parkinson's disease to tap for sixty seconds with the number of taps at 30 seconds and 60 seconds recorded. (NCT01168596)
Timeframe: Change from baseline to week 12

Interventionfinger taps per sixty seconds (Mean)
Rasagiline.46
Sugar Pill-0.23

Hand-grip Strength

The patients use the hand on the side most affected by Parkinson's disease to grip the dynamometer with as much strength as they can for 3 consecutive tries. The highest score will be their maximal voluntary contraction (MVC). The subject then rests for 60 seconds. The subject is asked to try to maintain 70% of their MVC and the duration the subject is able to maintain above 50% of their MVC is recorded. Immediately after the maintenance test, the subject performs three more MVCs and each one is recorded. These results are the duration the subject is able to maintain above 50% of their MVC. (NCT01168596)
Timeframe: Change from baseline to week 12

Interventionseconds (Mean)
Rasagiline-9.08
Sugar Pill-8.36

Marin Apathy Inventory (Apathy Evaluation Scale)

The Marin Apathy Inventory (Apathy Evaluation Scale) is a 14-item inventory measuring apathy of the subject over the past 2 to 4 weeks. Subjects are instructed to choose an answer from 0 to 3: 0=not at all, 1 = slightly, 2 = some, 3 = a lot, to questions related to apathy. The range would be 0 to 42, the higher the score the worse the apathy. (NCT01168596)
Timeframe: Change from baseline to week 12

Interventionunits on a scale (Mean)
Rasagiline.23
Sugar Pill.46

Modified Fatigue Impact Scale (MFIS)

The MFIS rates how much of a problem fatigue has caused the subjects during the past month, including the day of testing. It consists of 21 questions of fatigue on quality of life. Each subject is asked to circle the appropriate response for each item: 0=never, 1=rarely, 2=sometimes, 3=often, 4=always, 5=almost always. The minimum score is 0 and the maximum is 105. The higher the score, the more fatigue the subject. (NCT01168596)
Timeframe: Change from baseline to week 12

Interventionunits on a scale (Mean)
Rasagiline12.92
Sugar Pill12.69

Multidimensional Fatigue Inventory (MFIS)

The Multidimensional Fatigue Inventory (MFIS) is a 20-item self-report instrument designed to measure fatigue. It covers the following dimensions: general fatigue, physical fatigue, mental fatigue, reduced motivation and reduced activity. Subjects are instructed to choose a number from 1 to 5 that indicates their degree of agreement with each statement where 1 indicates that it is true and 5 that it is not true. There are positive and negative statements in the questionnaire. The range is 1 to 100, the higher the number the higher the fatigue. (NCT01168596)
Timeframe: Change from baseline to week 12

Interventionunits on a scale (Mean)
Rasagiline2.62
Sugar Pill6.83

Paced Auditory Serial Addition Test (PASAT)

The Paced Auditory Serial Addition Test (PASAT) is a neuropsychological test used to assess capacity and rate of information processing and sustained and divided attention. Where subjects are given a number (every 3 seconds for the first series and 2 seconds for the second series) and are asked to add the number they just heard with the number they heard before. This is a challenging task that involves working memory, attention, and arithmetic capabilities. (NCT01168596)
Timeframe: Change from baseline to week 12

Interventionunits on a scale (Mean)
Rasagiline-11.31
Sugar Pill-10.31

Parkinson's Disease Sleep Scale (PDSS)

The Parkinson's disease sleep scale (PDSS) is a 15-item visual analogue scale that assesses the profile of nocturnal disturbances in Parkinson's disease patients. The severity of symptoms of sleep over the past week is marked with a cross along a 10 cm line (labeled worst to best state). Responses are quantified by measuring the distance along each line to the intersection with the cross in centimetres, to the nearest 0.1 cm. The scores for each item range from 0 (symptom severe and always experienced) to 10 (symptom-free). The maximum score for PDSS is 150. (NCT01168596)
Timeframe: Change from baseline to week 12

Interventionunits on a scale (Mean)
Rasagiline-13.46
Sugar Pill.64

PD Quality of Life Scale (PDQ39)

PD Quality of Life Scale (PDQ39) is a 39-item questionnaire, which measures eight dimensions of health (mobility, activities of daily living, emotional well-being, stigma, social support, cognitions, communication and bodily discomfort) over the past 30 days. Dimension scores are coded on a scale of 0 (never) to 5 (always). The higher the score, the worse the quality of life affected by PD. The range for this test is 0 to 195. All eight dimensions are added for a total score. (NCT01168596)
Timeframe: Change from baseline to week 12

Interventionunits on a scale (Mean)
Rasagiline7.54
Sugar Pill5.67

State-Trait Anxiety Inventory (STAI)

The State-Trait Anxiety Inventory (STAI) is 40-item psychological inventory based on a 4-point Likert scale. Higher scores are positively correlated with higher levels of anxiety. The range for this test is 0 to 160. (NCT01168596)
Timeframe: Change from baseline to week 12

Interventionunits on a scale (Mean)
Rasagiline3.62
Sugar Pill6.08

Unified Parkinson's Disease Rating Scale - Motor (UPDRS Part III)

Unified Parkinson's Disease Rating Scale - Motor (UPDRS Part III)is a 14-question inventory measuring the motor functions of patients with Parkinson's Disease. Each subject is rated on a scale of 0 to 4 with the total score from 0 to 56. Higher total scores indicate more impairment of motor function. (NCT01168596)
Timeframe: Change from baseline to week 12

Interventionunits on a scale (Mean)
Rasagiline7.5
Sugar Pill-0.83

Visual Analog Scale - Subset: Afraid

The Visual Analog Scale is a measurement instrument for subjective characteristics or attitudes that cannot be directly measured. The severity of attitude at the time of testing is marked with a cross along a 10 cm line (labeled neutral to afraid, confused, sad, angry, energetic, tired, happy or tense). Responses are quantified by measuring the distance along each line to the intersection with the cross in centimetres, to the nearest 0.1 cm. The scores for each item range from 0 (symptoms-free) to 10 (symptom severe). (NCT01168596)
Timeframe: Change from baseline to week 12

Interventionunits on a scale (Mean)
Rasagiline-.77
Sugar Pill-.83

Visual Analog Scale - Subset: Angry

The Visual Analog Scale is a measurement instrument for subjective characteristics or attitudes that cannot be directly measured. The severity of attitude at the time of testing is marked with a cross along a 10 cm line (labeled neutral to afraid, confused, sad, angry, energetic, tired, happy or tense). Responses are quantified by measuring the distance along each line to the intersection with the cross in centimetres, to the nearest 0.1 cm. The scores for each item range from 0 (symptoms-free) to 10 (symptom severe). (NCT01168596)
Timeframe: Change from baseline to week 12

Interventionunits on a scale (Mean)
Rasagiline.19
Sugar Pill.33

Visual Analog Scale - Subset: Confused

The Visual Analog Scale is a measurement instrument for subjective characteristics or attitudes that cannot be directly measured. The severity of attitude at the time of testing is marked with a cross along a 10 cm line (labeled neutral to afraid, confused, sad, angry, energetic, tired, happy or tense). Responses are quantified by measuring the distance along each line to the intersection with the cross in centimetres, to the nearest 0.1 cm. The scores for each item range from 0 (symptoms-free) to 10 (symptom severe). (NCT01168596)
Timeframe: Change from baseline to week 12

Interventionunits on a scale (Mean)
Rasagiline-.35
Sugar Pill-.21

Visual Analog Scale - Subset: Energetic

The Visual Analog Scale is a measurement instrument for subjective characteristics or attitudes that cannot be directly measured. The severity of attitude at the time of testing is marked with a cross along a 10 cm line (labeled neutral to afraid, confused, sad, angry, energetic, tired, happy or tense). Responses are quantified by measuring the distance along each line to the intersection with the cross in centimetres, to the nearest 0.1 cm. The scores for each item range from 0 (symptoms-free) to 10 (symptom severe). (NCT01168596)
Timeframe: Change from baseline to week 12

Interventionunits on a scale (Mean)
Rasagiline-1.19
Sugar Pill-2.12

Visual Analog Scale - Subset: Happy

The Visual Analog Scale is a measurement instrument for subjective characteristics or attitudes that cannot be directly measured. The severity of attitude at the time of testing is marked with a cross along a 10 cm line (labeled neutral to afraid, confused, sad, angry, energetic, tired, happy or tense). Responses are quantified by measuring the distance along each line to the intersection with the cross in centimetres, to the nearest 0.1 cm. The scores for each item range from 0 (symptoms-free) to 10 (symptom severe). (NCT01168596)
Timeframe: Change from baseline to week 12

Interventionunits on a scale (Mean)
Rasagiline.04
Sugar Pill-0.33

Visual Analog Scale - Subset: Sad

The Visual Analog Scale is a measurement instrument for subjective characteristics or attitudes that cannot be directly measured. The severity of attitude at the time of testing is marked with a cross along a 10 cm line (labeled neutral to afraid, confused, sad, angry, energetic, tired, happy or tense). Responses are quantified by measuring the distance along each line to the intersection with the cross in centimetres, to the nearest 0.1 cm. The scores for each item range from 0 (symptoms-free) to 10 (symptom severe). (NCT01168596)
Timeframe: Change from baseline to week 12

Interventionunits on a scale (Mean)
Rasagiline-.19
Sugar Pill-.5

Visual Analog Scale - Subset: Tense

The Visual Analog Scale is a measurement instrument for subjective characteristics or attitudes that cannot be directly measured. The severity of attitude at the time of testing is marked with a cross along a 10 cm line (labeled neutral to afraid, confused, sad, angry, energetic, tired, happy or tense). Responses are quantified by measuring the distance along each line to the intersection with the cross in centimetres, to the nearest 0.1 cm. The scores for each item range from 0 (symptoms-free) to 10 (symptom severe). (NCT01168596)
Timeframe: Change from baseline to week 12

Interventionunits on a scale (Mean)
Rasagiline.25
Sugar Pill.83

Visual Analog Scale - Subset: Tired

The Visual Analog Scale is a measurement instrument for subjective characteristics or attitudes that cannot be directly measured. The severity of attitude at the time of testing is marked with a cross along a 10 cm line (labeled neutral to afraid, confused, sad, angry, energetic, tired, happy or tense). Responses are quantified by measuring the distance along each line to the intersection with the cross in centimetres, to the nearest 0.1 cm. The scores for each item range from 0 (symptoms-free) to 10 (symptom severe). (NCT01168596)
Timeframe: Change from baseline to week 12

Interventionunits on a scale (Mean)
Rasagiline.04
Sugar Pill.75

Change From Baseline in the Sum of Unified Parkinson's Disease Rating Scale Parts 2 and 3 Scores (UPDRS2+3)

The UPDRS is a clinician based rating scale used to measure motor impairments and disability. The UPDRS assesses six features of PD impairment. These are evaluated using a combination of data collected by interview and examination of the participant. The UPDRS Part 2 is the Activities of Daily Living (ADL) score and can range from 0-52 as determined by the physician. The UPDRS Part 3 is the Motor Examination (Total Motor Score [TMS]) and is defined as the total score, ranging from 0-108 as determined by the physician, of the tests given in the motor examination section. The combined scores of Parts 2 and 3 can range from 0-160 with the higher score indicating the worse condition. Change from baseline was analyzed using a constrained longitudinal analysis (cLDA) model with treatment, time, strata and treatment-by-time interaction as fixed effects and participant as a random effect. (NCT01155479)
Timeframe: Baseline and Week 26

InterventionScore on a Scale (Mean)
Preladenant 2 mg (Part 1)0.3
Preladenant 5 mg (Part 1)-1.0
Preladenant 10 mg (Part 1)-1.8
Placebo (Part 1)-2.2
Rasagiline (Part 1)-1.9

Change From Baseline in the UPDRS Part 2 Score (Activities of Daily Living [ADL])

The UPDRS is a clinician based rating scale used to measure motor impairments and disability. The UPDRS assesses six features of PD impairment. These are evaluated using a combination of data collected by interview and examination of the participant. The UPDRS Part 2 is the Activities of Daily Living (ADL) score and can range from 0-52 as determined by the physician with the higher score indicating the worse condition. Change from baseline was analyzed using a cLDA model with treatment, time, strata and treatment-by-time interaction as fixed effects and participant as a random effect. (NCT01155479)
Timeframe: Baseline and Week 26

InterventionScore on a Scale (Mean)
Preladenant 2 mg (Part 1)0.30
Preladenant 5 mg (Part 1)0.10
Preladenant 10 mg (Part 1)-0.20
Placebo (Part 1)-0.40
Rasagiline (Part 1)-0.20

Number of Participants Who Discontinued Study Due to an AE in Part 1

An AE is defined as any untoward medical occurrence in a participant administered a pharmaceutical product and which does not necessarily have to have a causal relationship with this treatment. An AE can therefore be any unfavorable and unintended sign (including an abnormal laboratory finding, for example), symptom, or disease temporally associated with the use of a medicinal product, whether or not considered related to this medicinal product. (NCT01155479)
Timeframe: Day 1 to Week 26

InterventionParticipants (Number)
Preladenant 2 mg (Part 1)13
Preladenant 5 mg (Part 1)8
Preladenant 10 mg (Part 1)20
Placebo (Part 1)8
Rasagiline (Part 1)6

Number of Participants Who Discontinued Study Due to an AE in Part 2

An AE is defined as any untoward medical occurrence in a participant administered a pharmaceutical product and which does not necessarily have to have a causal relationship with this treatment. An AE can therefore be any unfavorable and unintended sign (including an abnormal laboratory finding, for example), symptom, or disease temporally associated with the use of a medicinal product, whether or not considered related to this medicinal product. (NCT01155479)
Timeframe: Week 27 to Week 52

InterventionParticipants (Number)
Preladenant 2 mg (Part 2)7
Preladenant 5 mg (Part 2)5
Preladenant 10 mg (Part 2)8
Placebo (Part 2)3
Rasagiline (Part 2)4

Number of Participants With Adverse Events (AEs) in Part 1

An adverse event (AE) is defined as any untoward medical occurrence in a participant administered a pharmaceutical product and which does not necessarily have to have a causal relationship with this treatment. An AE can therefore be any unfavorable and unintended sign (including an abnormal laboratory finding, for example), symptom, or disease temporally associated with the use of a medicinal product, whether or not considered related to this medicinal product. (NCT01155479)
Timeframe: Day 1 to Week 26

InterventionParticipants (Number)
Preladenant 2 mg (Part 1)108
Preladenant 5 mg (Part 1)110
Preladenant 10 mg (Part 1)121
Placebo (Part 1)102
Rasagiline (Part 1)105

Number of Participants With Adverse Events (AEs) in Part 2

An adverse event (AE) is defined as any untoward medical occurrence in a participant administered a pharmaceutical product and which does not necessarily have to have a causal relationship with this treatment. An AE can therefore be any unfavorable and unintended sign (including an abnormal laboratory finding, for example), symptom, or disease temporally associated with the use of a medicinal product, whether or not considered related to this medicinal product. (NCT01155479)
Timeframe: Week 27 to Week 52

InterventionParticipants (Number)
Preladenant 2 mg (Part 2)116
Preladenant 5 mg (Part 2)120
Preladenant 10 mg (Part 2)113
Placebo (Part 2)120
Rasagiline (Part 2)119

Percentage of Responders (Participants With a ≥20% Improvement in UPDRS2+3)

UPDRS is a clinician based rating scale used to measure motor impairments and disability; it assesses 6 features of PD impairment. These are evaluated using a combination of data collected by interview and examination of the participant. UPDRS Part 2 is Activities of Daily Living score and ranges from 0-52. UPDRS Part 3 is Motor Examination and ranges from 0-108. The combined scores of Parts 2 and 3 can range from 0-160 with the higher score indicating the worse condition. A Responder is defined as a participant with at least 20% improvement in UPDRS2+3 from Baseline to Week 26 (End of Part 1 Treatment); a participant with at least a 20% decrease from Baseline score in UPDRS2+3 is defined as a responder. The proportion of Responders was analyzed using a generalized linear mixed model with treatment effect, strata and Baseline UPDRS2+3 as a covariate, and treatment-by-time interaction as fixed effects and subject as random effect. (NCT01155479)
Timeframe: Baseline and Week 26

InterventionPercentage of Responders (Number)
Preladenant 2 mg (Part 1)25.90
Preladenant 5 mg (Part 1)29.50
Preladenant 10 mg (Part 1)31.50
Placebo (Part 1)35.20
Rasagiline (Part 1)33.10

CGI-S

Change from baseline in individual Clinical Global Impression - Severity. Severity scale (CGI-S) is a 7-point scale that requires the clinician to rate the severity of the patient's illness (Parkinson's Disease) at the time of assessment relative to the clinician's past experience with patients who have the same diagnosis as one of the following:. 1 is normal and 7 is the most extremely ill patients. A subject defined as a treatment responder when the improvement from baseline to the Week12 / Last Observed Value (LOV) was of at least 1 point or more. (NCT01968460)
Timeframe: 12 weeks

InterventionParticipants (Count of Participants)
P2B001 Treatment A13
P2B001 Treatment B9
Placebo3

PDQ39

Change from baseline in individual Parkinson's Disease Questionnaire - 39. Score 0-100 where 0 is indicative of no problem at all and 100 is the maximum level of problem. (NCT01968460)
Timeframe: 12 weeks

Interventionunits on a scale (Least Squares Mean)
P2B001 Treatment A-3.01
P2B001 Treatment B-2.19
Placebo0.26

Total UPDRS I, II, III Scores

"Change from baseline to final visit (week 12) in total UPDRS score (defined as sum of parts I, II and III, scores (0-176). UPDRS- Unified Parkinson's Disease Rating Scale, minimum value is 0 points and maximum value is 176.~High score mean worse outcome." (NCT01968460)
Timeframe: Week 12

Interventionunits on a scale (Least Squares Mean)
P2B001 Treatment A-5.97
P2B001 Treatment B-5.15
Placebo-1.31

UPDRS ADL (Part II)

Change from baseline in individual UPDRS ADL (part II). Activity of daily Life UPDRS part II minimum is 0 point and max is 52 point (worse outcome) (NCT01968460)
Timeframe: Week 12

Interventionunits on a scale (Least Squares Mean)
P2B001 Treatment A-1.49
P2B001 Treatment B-1.06
Placebo0.36

UPDRS Motor (Part III)

Change from baseline in individual UPDRS motor (part III). UPDRS- Unified Parkinson's Disease Rating Scale, part III motor . min is 0 and Max is 108 (Worse outcome) (NCT01968460)
Timeframe: 12 weeks

Interventionunits on a scale (Mean)
P2B001 Treatment A-4.43
P2B001 Treatment B-3.95
Placebo-1.62

Change in Unified Parkinson's Disease Rating Scale (UPDRS) Score From Baseline to Last Observed Value in the Placebo Phase

Subjects were assessed according to the United Parkinson's Disease Rating Scale UPDRS,(version 3;) Parts I and II are historical data and are designed to rate mentation, behavior and mood; Part III is done as a motor examination at the time of a visit. The UPDRS measures patient status on a scale 0, which is normal or none, to 4, which is severe or the worst scenario. (NCT00256204)
Timeframe: 36 weeks

InterventionScores on a scale (Mean)
1mg Delayed Start3.9
1mg Early Start1.0
2mg Early Start0.8

Change in Total Unified Parkinson's Disease Rating Scale (UPDRS) Score From Baseline

The primary efficacy endpoint was defined as the change in Total UPDRS from Baseline. Subjects were assessed according to the United Parkinson's Disease Rating Scale (UPDRS,(version 3;) Parts I and II are historical data and are designed to rate mentation, behavior and mood; Part III is done as a motor examination at the time of a visit. The UPDRS measures patient status on a scale 0, which is normal or none, to 4, which is severe or the worst scenario. (NCT00256204)
Timeframe: 12w, 24w, 36w, 42w, 48w, 54w, 60w, 66w, 72w

,,,
InterventionScores on a scale (Mean)
Week 12Week 24Week 36Week 42Week 48Week 54Week 60Week 66Week 72
1mg Delayed Start0.93.03.72.41.91.91.92.53.3
1mg Early Start-1.2-1.10.60.20.70.71.11.51.9
2mg Delayed Start0.72.23.01.71.41.11.62.02.3
2mg Early Start-0.7-0.50.80.40.50.81.21.52.2

Change From Baseline to End of Week 12 Visit in ADL Subscale of PDQ39

"The efficacy of P2B 0.6/0.75 mg as compared to Pramipexole ER tablet titrated to optimal dose.~ADL PDQ39- Activity of daily life part in Parkinson's Disease Questionaries' 39 Score 0-100 when 100 is the worse outcome" (NCT03329508)
Timeframe: Baseline to week 12

Interventionscore on a scale (Least Squares Mean)
P2B001-5.30
Rasagiline Capsule-2.04
Pramipexole Capsule-3.40
Pramipexole Extended Release-3.12

Change From Baseline to Week 12 in Total UPDRS II ADL

Differences between of P2B 0.6/0.75 mg as compared to its individual components in the change of ADL UPDRS score (UPDRS part II) Activity of daily Life UPDRS part II minimum is 0 point and max is 52 point (worse outcome) (NCT03329508)
Timeframe: Baseline to week 12

Interventionscore on a scale (Least Squares Mean)
P2B001-2.14
Rasagiline Capsule-0.62
Pramipexole Capsule-0.97
Pramipexole Extended Release-2.02

Change From Baseline to Week 12 in Total UPDRS III Motor

"Differences between P2B 0.6/0.75 mg as compared to its individual components in the change of Motor UPDRS score (UPDRS Part III ).~UPDRS- Unified Parkinson's Disease Rating Scale, part III motor . min is 0 and Max is 108 (Worse outcome)" (NCT03329508)
Timeframe: baseline to week 12

Interventionscore on a scale (Least Squares Mean)
P2B001-5.82
Rasagiline Capsule-4.07
Pramipexole Capsule-4.30
Pramipexole Extended Release-6.36

Change in Epworth Sleepiness Scale (ESS) Score.

"Differences between P2B 0.6/0.75 mg as compared to pramipexole ER tablets in the change of Epworth Sleepiness Scale (ESS) score.~Scale is 0-24 , when 24 is worse outcome" (NCT03329508)
Timeframe: baseline to week 12

Interventionscore on a scale (Least Squares Mean)
P2B001-0.33
Rasagiline Capsule-0.81
Pramipexole Capsule0.39
Pramipexole Extended Release2.33

Change in Total Unified Parkinson's Disease Rating Scale (UPDRS) Score (Defined as Sum of Parts II and III, Scores (0-160).

"Differences between P2B 0.6/0.75 mg as compared to its individual components in the change of total UPDRS score (defined as sum of parts II and III, scores (0-160).~UPDRS- Unified Parkinson's Disease Rating Scale, minimum value is 0 points and maximum value is 160.~High score mean worse outcome." (NCT03329508)
Timeframe: baseline to week 12

Interventionscore on a scale (Least Squares Mean)
P2B001-7.98
Rasagiline Capsule-4.69
Pramipexole Capsule-5.32
Pramipexole Extended Release-8.35

"Change From Baseline at Week 12 in Mean On Time Without Troublesome Dyskinesia"

"When a participant is on without dyskinesias, parkinsonian symptoms have dissipated and the participant is experiencing no uncontrollable extraneous movements. Study participants reported their parkinsonian symptoms at half-hour intervals as off, on without dyskinesia, on with non-troublesome dyskinesia, on with troublesome dyskinesia, or asleep on their daily diary for 3 days before randomization and for the 3 days immediately before their Week-12 visit. The mean change from baseline in on without troublesome dyskinesia time was based on a constrained longitudinal data analysis with treatment, time, and treatment-by-time interaction as fixed effects and subject as random effect." (NCT01155466)
Timeframe: Baseline and Week 12

InterventionHours/day (Mean)
Preladenant 2 mg0.8
Preladenant 5 mg0.9
Preladenant 10 mg0.5
Placebo0.4
Rasagiline 1 mg0.7

"Change From Baseline in Mean Off Time"

"The on state is defined as the period of time during which a patient's symptoms of PD improve or disappear following treatment with L-dopa or dopamine agonists. The off state is defined as the period of time characterized by the return of symptoms (i..e. tremor, slowness, and rigidity) following treatment with L-dopa or dopamine agonists. Study participants reported their symptoms at half-hour intervals as off, on, or asleep on their daily diary for 3 days before randomization (baseline) and for the 3 days immediately before their Week-12 visit. The mean change from baseline in off time was based on a constrained longitudinal data analysis with treatment, time, and treatment-by-time interaction as fixed effects and subject as random effect." (NCT01155466)
Timeframe: Baseline and Week 12

InterventionHours/day (Mean)
Preladenant 2 mg-0.9
Preladenant 5 mg-0.9
Preladenant 10 mg-0.8
Placebo-0.8
Rasagiline 1 mg-1.1

"Percentage of Participants With >30% Change (Reduction) From Baseline at Week 12 in Mean Off Time"

"The on state is defined as the period of time during which a patient's symptoms of PD improve or disappear following treatment with L-dopa or dopamine agonists. The off state is defined as the period of time characterized by the return of symptoms (i..e. tremor, slowness, and rigidity) following treatment with L-dopa or dopamine agonists. Study participants reported their symptoms at half-hour intervals as off, on, or asleep on their daily diary for 3 days before randomization and for the 3 days immediately before their Week-12 visit." (NCT01155466)
Timeframe: Baseline and Week 12

InterventionPercentage of participants (Number)
Preladenant 2 mg30.4
Preladenant 5 mg33.6
Preladenant 10 mg35.1
Placebo32.8
Rasagiline 1 mg33.9

Change From Baseline at Week 12 in Epworth Sleepiness Scale (ESS)

The ESS is a self-administered questionnaire providing a measure of a person's general level of daytime sleepiness, or their average sleep propensity in daily life. The scale consists of 8 situations in which the participant rates their tendency to become sleepy on a scale of 0=no chance of dozing to 3=high chance of dozing. The overall score is the sum of the scores for the 8 situations for a minimum of 0 and a maximum of 24. (NCT01155466)
Timeframe: Baseline and Week 12

InterventionScores on a scale (Mean)
Preladenant 2 mg-0.3
Preladenant 5 mg-0.1
Preladenant 10 mg0.0
Placebo-0.3
Rasagiline 1 mg0.1

Number of Participants With Alanine Aminotransferase >=3 Times the Upper Limit of Normal

The number of participants with alanine aminotransferase >=3 times the upper limit of normal and a >=10% increase was reported. (NCT01155466)
Timeframe: Up to Week 14

InterventionParticipants (Number)
Preladenant 2 mg1
Preladenant 5 mg1
Preladenant 10 mg1
Placebo1
Rasagiline 1 mg0

Number of Participants With Aspartate Aminotransferase >=3 Times the Upper Limit of Normal

The number of participants with aspartate aminotransferase >=3 times the upper limit of normal and a >=10% increase was reported. (NCT01155466)
Timeframe: Up to Week 14

InterventionParticipants (Number)
Preladenant 2 mg1
Preladenant 5 mg1
Preladenant 10 mg1
Placebo0
Rasagiline 1 mg0

Number of Participants With Diastolic Blood Pressure >=105 mm Hg

The number of participants with Diastolic Blood Pressure >=105 mm Hg was reported. (NCT01155466)
Timeframe: Up to Week 14

InterventionParticipants (Number)
Preladenant 2 mg3
Preladenant 5 mg4
Preladenant 10 mg9
Placebo7
Rasagiline 1 mg4

Numberof Participants With Systolic Blood Pressure >=180 mm Hg

The number of participants with Systolic Blood Pressure >=180 mm Hg was reported. (NCT01155466)
Timeframe: Up to Week 14

InterventionParticipants (Number)
Preladenant 2 mg1
Preladenant 5 mg1
Preladenant 10 mg3
Placebo1
Rasagiline 1 mg0

Percentage of Participants With Suicidality

The percentage of participants with suicidality using the Columbia - Suicide Severity Rating Scale (C-SSRS) was reported. The C-SSR was used in this study only for the purpose of safety monitoring by measuring the incidence of different types of suicidality categories during treatment. The assessment was done by the nature of the responses, not by a numbered scale. Participants who reported at least one occurrence of suicidal behavior or suicidal ideation were counted as having experienced suicidality. Suicidal behavior included suicide attempt, aborted attempt, interrupted attempt, or preparatory behavior. Suicidal ideation included a wish to die or active suicidal thought with or without method, intent or plan. (NCT01155466)
Timeframe: Up to Week 12

InterventionPercentage of participants (Number)
Preladenant 2 mg2.6
Preladenant 5 mg2.6
Preladenant 10 mg0.7
Placebo3.2
Rasagiline 1 mg0.6

Amyotrophic Lateral Sclerosis Functional Rating Scale - Revised (ALSFRS-R)

The primary outcome measure is the difference in the rate of decline in function, as detected by the ALS Functional Rating Scale - Revised (ALSFRS-R) in patients taking rasagiline compared to a database of patients from randomized clinical trials conducted during 1997-2007. Minimum score is 0 (no function) to Maximum score is 48 (normal function) (NCT01232738)
Timeframe: up to 12 months

Interventionunits on a scale (Mean)
ALSRFS-R Slope - Rasagiline-1.20
ALSFRS-R - Historical Placebo Control-0.94

Change in BCL2/BAX Mitochondrial Biomarkers

The 12 month change in mitochondrial biomarker BCL2/BAX. We measured at baseline, 6 months and 12 months. (NCT01232738)
Timeframe: Baseline, 6 months, 12 months

InterventionRatio (Mean)
Rasagiline0.24

Change in JC-1 Mitochondrial Biomarkers

The 12 month change in mitochondrial biomarkerJC-1 red/green fluorescence ratio. We measured at baseline, 6 months and 12 months. (NCT01232738)
Timeframe: Baseline, 6 months, 12 months

Interventionratio (Mean)
Rasagiline1.92

Change in Mitotracker Mitochondrial Biomarkers

The 12 month change in mitochondrial biomarkerMitotracker. We measured at baseline, 6 months and 12 months. (NCT01232738)
Timeframe: Baseline, 6 months, 12 months

InterventionRelative Fluorescent Intensity (Mean)
Rasagiline54.14

Change in ORAC Mitochondrial Biomarkers

The 12 month change in mitochondrial biomarker Oxygen Radical Antioxidant Capacity. We measured at baseline, 6 months and 12 months. (NCT01232738)
Timeframe: Baseline, 6 months, 12 months

InterventionTrolox equivalents (Mean)
Rasagiline1028.70

Change in ORAC Mitochondrial Biomarkers

The 12 month change in mitochondrial biomarker Oxygen Radical Antioxidant Capacity. We measured at baseline, 6 months and 12 months. (NCT01232738)
Timeframe: Baseline, 6 months, 12 months

Interventionumol Trolox equivalents (Mean)
Rasagiline1028.70

Change in Percent Annexin V Mitochondrial Biomarkers

The 12 month change in mitochondrial biomarker Annexin V %. We measured at baseline, 6 months and 12 months. (NCT01232738)
Timeframe: Baseline, 6 months, 12 months

InterventionAnnexin V % (Mean)
Rasagiline-6.67

Difference in Time to Treatment Failure

This group is defined as death, endotracheal intubation, tracheostomy-assisted ventilation or use of noninvasive ventilation >= 23 hours/day for 14 days or more. (NCT01232738)
Timeframe: up to 12 months

Interventionyears (Median)
Difference in Time to Treatment Failure - Rasagiline0.9367
Difference in Time to Treatment Failure - Historical Control0.8963

Change in Blood Oxygen Level-dependent(BOLD) Signal in the Posterior Putamen, M1, and Supplementary Motor Area(SMA).

12-month study in PD to watch the effect of an MAO-B inhibitor on BOLD signal in the posterior putamen, M1, and SMA. (NCT02789020)
Timeframe: Baseline and one-year

Interventionarbitrary units (A.U.s) (Mean)
Rasagiline-0.054
Placebo-0.086

Change in Free-water Accumulation in the Substantia Nigra

"12-month study in PD to watch the effect of an Monoamine Oxidase-B inhibitor on the progressive increase of free-water accumulation in the substantia nigra.~Recently, free-water diffusion MRI analysis using a bi-tensor model was developed to explicitly estimate the contribution of freely diffusing water molecules within the voxel. This free-water measure is expected to increase with atrophy-based neurodegeneration. Since substantia nigra degeneration occurs mostly in the posterior region of the substantia nigra in PD (ie. ventrolateral tier), we tested the hypothesis that free-water would be elevated in the posterior substantia nigra of PD." (NCT02789020)
Timeframe: Baseline and one-year

Interventionarbitrary units (A.U.s) (Mean)
Rasagiline0.0009
Placebo0.0041

Changes Between the Groups on fMRI

Participants will use their hand to squeeze an MRI compatible grip force transducer in the MRI unit. (NCT02789020)
Timeframe: Changes from baseline to 1 year

Interventionunitless (Mean)
Rasagiline-0.054
Placebo-0.086

Changes in Parkinson's Disease Motor Symptoms and Bradykinesia

Motor testing batteries such as the Purdue Pegboard Test will be administered to measure changes in the progression of the PD motor symptoms and bradykinesia. (NCT02789020)
Timeframe: Baseline and one-year

Interventioncount of pegs (Mean)
Rasagiline1.04
Placebo0.689

Change From Baseline in Mean Total Daily OFF Time Using Parkinson's Disease Patient Diary

"Parkinson's Disease Patient Diary is a self-administered diary designed to assess motor fluctuations throughout the day. It is divided into 30-minute intervals, and the patient selects one of four options for each interval: asleep; off; on with no dyskinesia or without troublesome dyskinesia; or on with troublesome dyskinesia.~The Change From Baseline in Mean Total Daily OFF time is calculated by taking the difference between the average of the total daily OFF time at Weeks 4, 8, 12, and 16, and the Baseline Total Daily OFF Time." (NCT01479530)
Timeframe: Baseline and Weeks 4, 8, 12, and 16

Interventionhours (Mean)
Placebo-0.76
Azilect®-1.25

Change From Baseline in UPDRS Motor Score During ON Time

UPDRS is a 42-item rating scale designed to assess Parkinson's Disease-related disability and impairment using a patient interview and a physical examination. It has 4 parts and 4 subsection scores. A higher score indicates a worse outcome. I: mentation, behaviour and mood symptoms - 0 to 16; II: ADL - 0 to 52; III: motor function - 0 to 108; IV: complications of dopaminergic therapy - 0 to 23. Subsection scores for I to III are used to calculate a total score that ranges from 0 (no disability) to 176 (total dependence). (NCT01479530)
Timeframe: Baseline and Week 16

Interventionunits on a scale (Mean)
Placebo-1.75
Azilect®-3.34

Change From Baseline in UPDRS-ADL Score During OFF Time

Unified Parkinson's Disease Rating Scale (UPDRS) is a 42-item rating scale designed to assess Parkinson's Disease-related disability and impairment using a patient interview and a physical examination. It has 4 parts and 4 subsection scores. A higher score indicates a worse outcome. I: mentation, behaviour and mood symptoms - 0 to 16; II: activities of daily living (ADL) - 0 to 52; III: motor function - 0 to 108; IV: complications of dopaminergic therapy - 0 to 23. Subsection scores for I to III are used to calculate a total score that ranges from 0 (no disability) to 176 (total dependence). (NCT01479530)
Timeframe: Baseline and Week 16

Interventionunits on a scale (Mean)
Placebo-1.20
Azilect®-2.21

Clinical Status Using CGI-I Score During ON Time

Clinical Global Impression - Global Improvement (CGI-I) is a single-item rating scale used to evaluate a patient's condition relative to baseline on a 7-point scale, regardless of whether the improvement is related to the investigational medicinal product (IMP). The scale ranges from 1 (very much improved) to 7 (very much worse). (NCT01479530)
Timeframe: Week 16

Interventionunits on a scale (Mean)
Placebo3.56
Azilect®3.15

Change in Negative Symptoms

"The Scale for the Assessment of Negative Symptoms (SANS) rating scale was used to assess the negative symptoms of schizophrenia. Scores on the subscales are combined (summed) to compute a total score. There are a total of 17 subscales. Each subscale ranges from 0=Not at all to 5=Severe. Every 4 weeks the summed subscale scores provide a total score for that week (0-85). Higher scores indicate more severe negative symptoms." (NCT00492336)
Timeframe: Every 4 weeks over a 12 week period

,
Interventionunits on a scale (Mean)
Week 0Week 4Week 8Week 12
Inactive Pill33.532.334.134.3
Rasagiline32.731.231.129.9

Change in Persistent Positive Symptoms

"The Brief Psychiatric Rating Scale (BPRS) positive symptom item total score was used to assess positive symptom change. The BPRS positive symptom items are: conceptual disorganization, hallucinatory behavior, unusual thought content, and suspiciousness. The total score is calculated by adding the scores for each item. Each scale ranges from 1=Not Present to 7=Very Severe. The minimum score is 4 and the maximum score is 28. A higher score indicates a more severe positive symptom rating." (NCT00492336)
Timeframe: Every 4 weeks for 12 weeks.

,
Interventionunits on a scale (Mean)
Week 0Week 4Week 8Week 12
Inactive Pill9.19.19.88.9
Rasagiline8.89.29.28.3

Cognitive Testing - Delayed Discounting

The monetary choice questionnaire for hypothetical monetary rewards was used to assess delayed discounting (Kirby et al, 1999). The measure includes 27 items in which participants choose between a smaller, immediate reward (SIR) and a larger, delayed reward (LDR). There are three LDR sizes: small ($25-35), medium ($50-60) and large ($75-85). By examining the pattern of choices that participants make across the set of 27 items it is possible to calculate their delay discounting rate, termed K. The discount rate determines the steepness of the reduction in the present value of a reward with increases in the delay to the possible receipt of that reward. Thus, higher values in K represent greater discounting of the value of future rewards. With this measure K values can range between a low of 0.00016 to a high of 0.25. Higher K values have been linked to measures of impulsivity. Shown in the table are the K values observed when the future rewards were small, medium, or large. (NCT00492336)
Timeframe: Beginning of treatment phase (week 0) and end of treatment phase (week 12)

,
Interventionunits on a scale (Geometric Mean)
Large Reward: Week 0Large Reward: Week 12Medium Reward: Week 0Medium Reward: Week 12Small Reward: Week 0Small Reward: Week 12
Inactive Pill0.0180.0100.0240.0110.0230.014
Rasagiline0.0040.0100.0030.0080.0090.016

Cognitive Testing - N-Back Neurocognitive Task

The N-Back task is a sequential letter working memory task. D-prime was used to measure accuracy on the 0-back, 1-back, and 2-back conditions. D-prime scores range from 0 to 8.6. Higher scores are better. As memory load increases from 0 to 1, from 1 to 2, D-prime scores are expected to be lower. (NCT00492336)
Timeframe: Beginning of treatment phase (week 0) and end of treatment phase (week 12)

,
Interventionunits on a scale (Mean)
0-Back: Week 00-Back: Week 120-Back: Change1-Back: Week 01-Back: Week 121-Back: Change2-Back: Week 02-Back: Week 122-Back: Change
Inactive Pill3.523.660.142.632.660.031.561.570.01
Rasagiline3.473.790.322.752.960.201.751.59-0.16

Cognitive Testing - Probabilistic Learning Task

To assess reward learning, participants used performance feedback to choose the most frequently rewarded item in each of three pairs of stimuli (one pair had reward probabilities: 80% vs 20%; one pair had reward probabilities of 70% vs 30%; one pair had the probabilities of 60% vs 40 %) (PL; Frank et al, 2004). A total of 240 trials were administered so each pair was seen 80 times. Higher scores represent more frequent choices of the optimal stimulus in each pair. The frequencies with which participants repeated an item choice that was rewarded on the previous presentation (win-stay) is also presented as a percentage. Similarly, the lose-shift score is the percentage of times that participants changed their choice for unrewarded items (lose-shift). The win-stay score serves as a measure of the impact of positive feedback on subsequent choices while the lost-shift score serves as a measure of the impact of negative feedback on subsequent choices. (NCT00492336)
Timeframe: Beginning of treatment phase (week 0) and end of treatment phase (week 12)

,
Interventionpercentage of optimal stimuli chosen (Mean)
80 vs 20: Week 080 vs 20: Week 1280 vs 20: Change70 vs 30: Week 070 vs 30: Week 1270 vs 30: Change60 vs 40: Week 060 vs 40: Week 1260 vs 40: ChangeLose Shifts: Week 0Lose Shifts: Week 12Lose Shifts: ChangeWin Stays: Week 0Win Stays: Week 12Win Stays: Change
Inactive Pill69.168.5-0.766.165.9-0.257.958.60.756.554.8-1.262.264.42.3
Rasagiline70.870.4-0.469.764.4-5.353.958.74.748.650.12.964.662.9-1.7

Cognitive Testing - Repeatable Battery for the Assessment of Neuropsychological Status (RBANS) Total Score

The RBANS is a brief, individually administered test designed to evaluate neuropsychological status of adults, ages 20-89. The 12 subtests measure attention, language, visuospatial/constructional abilities, and immediate and delayed memory. The raw scores from the subtests are scaled together to create index scores, and these are summed for conversion to a total scale score. Higher score equals a better outcome. The total index score range for the RBANS is 40-160. (NCT00492336)
Timeframe: Beginning of treatment phase (week 0) and end of treatment phase (week 12)

,
Interventionunits on a scale (Mean)
Week 0Week 12Change
Inactive Pill74.275.31.1
Rasagiline76.878.71.9

Depressive Symptoms

The Calgary Depression Scale (CDS; Addington et al, 1997) total score was used to assess depressive symptoms over the course of the study. Total scores were calculated by summing the scores of each of the 9 items. Total scores can range from 0-27, with higher scores indicating more severe depressive symptoms. (NCT00492336)
Timeframe: Every 4 weeks for 12 weeks.

,
Interventionunits on a scale (Mean)
Week 0Week 4Week 8Week 12
Inactive Pill2.021.961.521.52
Rasagiline2.292.192.312.58

Extrapyramidal Symptoms

The Simpson Angus Scale (SAS; Simpson and Angus, 1970) was used to assess extrapyramidal symptoms (EPS). The assessment consists of 11 items, each rating the severity of potential symptoms of movement disorders. Total scores are calculated by summing the scores of each of the 11 items for a potential total score of 0-44, with higher scores indicating more severe EPS. (NCT00492336)
Timeframe: Baseline (Week 0) and End of Study (Week 12)

,
Interventionunits on a scale (Mean)
Week 0Week 12Change
Inactive Pill1.931.89-0.04
Rasagiline1.820.96-0.85

Global Change in Illness Severity

"The Clinical Global Impression (CGI) severity of illness item was used to assess global changes. Scores on this item range from 1=Normal, not at all ill to 7=Among the most extremely ill." (NCT00492336)
Timeframe: Every 4 weeks for 12 weeks.

,
Interventionunits on a scale (Mean)
Week 0Week 4Week 8Week 12
Inactive Pill4.314.324.364.27
Rasagiline4.054.081.001.08

Number of Participants Exhibiting Side Effects

"The Side Effect Checklist (SEC) was used to assess side effects. The SEC is comprised of 22 common side effects, which are rated on a 1 (none)-4 (severe) scale. Side effects are determined to be clinically significant if there is a two or more point increase in severity from baseline, or any side effect that receives a severity rating of 4 (severe) at any point in the treatment phase of the study." (NCT00492336)
Timeframe: Every week for 12 weeks

,
InterventionParticipants (Count of Participants)
Abdominal PainAnorexiaBruising EasilyConstipationDiarrheaDizzinessDry MouthEnuresisFeverHeadacheHypersalivationInsomniaMalaiseMucosal UlcerationNauseaRashRestlessnessSedationSore ThroatStiffnessTremorUrticariaVomitingWeight Loss
Inactive Pill71019671135877141257855115412
Rasagiline57412957427428163483733410

Number of Participants With Akathisia

The Barnes Akathisia Scale (BAS; Barnes, 1989) was used to assess akathisia, a type of extrapyramidal symptom. The global clinical assessment of akathisia score is rated on a scale from 0=Absent to 5=Severe Akathisia. (NCT00492336)
Timeframe: Baseline and every two weeks throughout the double-blind phase of the study, for up to 12 weeks.

,
InterventionParticipants (Count of Participants)
Score 0=Absent : BaselineScore 0=Absent : End of StudyScore 1=Questionable : BaselineScore 1=Questionable : End of StudyScore 2=Mild Akathisia : BaselineScore 2=Mild Akathisia : End of StudyScore 3=Moderate Akathisia : BaselineScore 3=Moderate Akathisia : End of Study
Inactive Pill2121550000
Rasagiline2020322311

Change From Baseline in Mean Total Daily OFF Time Using Parkinson's Disease Patient Diary

"Parkinson's Disease Patient Diary is a self-administered diary designed to assess motor fluctuations throughout the day. It is divided into 30-minute intervals, and the patient selects one of four options for each interval: asleep; off; on with no dyskinesia or without troublesome dyskinesia; or on with troublesome dyskinesia.~The Change From Baseline in Mean Total Daily OFF Time is calculated by taking the difference between the average of the total daily OFF time at Weeks 6, 10, 14 and 18, and the Baseline Total Daily OFF Time." (NCT01268891)
Timeframe: Baseline and Weeks 6, 10, 14, and 18

Interventionhours (Mean)
Placebo-1.24
Azilect®-1.59

Change From Baseline in UPDRS Motor Score During ON Time

UPDRS is a 42-item rating scale designed to assess Parkinson's Disease-related disability and impairment using a patient interview and a physical examination. It has 4 parts and 4 subsection scores. A higher score indicates a worst outcome. I: mentation, behaviour and mood symptoms - 0 to 16; II: ADL - 0 to 52; III: motor function - 0 to 108; IV: complications of dopaminergic therapy - 0 to 23. Subsection scores for I to III are used to calculate a total score that ranges from 0 (no disability) to 176 (total dependence). (NCT01268891)
Timeframe: Baseline and Week 18

Interventionunits on a scale (Mean)
Placebo-1.52
Azilect®-2.87

Change From Baseline in UPDRS-ADL Score During OFF Time

Unified Parkinson's Disease Rating Scale (UPDRS) is a 42-item rating scale designed to assess Parkinson's Disease-related disability and impairment using a patient interview and a physical examination. It has 4 parts and 4 subsection scores. A higher score indicates a worst outcome. I: mentation, behaviour and mood symptoms - 0 to 16; II: activities of daily living (ADL) - 0 to 52; III: motor function - 0 to 108; IV: complications of dopaminergic therapy - 0 to 23. Subsection scores for I to III are used to calculate a total score that ranges from 0 (no disability) to 176 (total dependence). (NCT01268891)
Timeframe: Baseline and Week 18

Interventionunits on a scale (Mean)
Placebo0.13
Azilect®-0.57

Clinical Status Using CGI-I Score During ON Time

Clinical Global Impression - Global Improvement (CGI-I) is a single-item rating scale used to evaluate a patient's condition relative to baseline on a 7-point scale, regardless of whether the improvement is related to the investigational medicinal product (IMP). The scale ranges from 1 (very much improved) to 7 (very much worse). (NCT01268891)
Timeframe: Week 18

Interventionunits on a scale (Mean)
Placebo3.35
Azilect®3.05

AUC0-t - Area Under the Plasma Concentration-time Curve From Time 0 to Last Observed Concentration

(NCT01532141)
Timeframe: pre-dose, and 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12, 16 and 24 h post-dose

,,
Interventionng.h/mL (Mean)
BIA 9-1067Rasagiline
BIA 9-1067 1h Before Rasagiline21823277
BIA 9-1067 Alone1966NA
BIA 9-1067 Concomitant Rasagiline20643370

Cmax - Maximum Observed Plasma Drug Concentration

(NCT01532141)
Timeframe: pre-dose, and 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12, 16 and 24 h post-dose

,,
Interventionng/mL (Mean)
BIA 9-1067Rasagiline
BIA 9-1067 1h Before Rasagiline7034.260
BIA 9-1067 Alone647NA
BIA 9-1067 Concomitant Rasagiline6404.299

Time of Occurrence of Cmax (Tmax)

6-mL blood samples for the determination of plasma concentrations of BIA 9-1067 and/or rasagiline will be drawn by direct venipuncture or via an intravenous catheter into potassium ethylenediaminetetraacetic acid(EDTA)Vacutainers (NCT01532141)
Timeframe: pre-dose, and 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12, 16 and 24 h post-dose

,,
Interventionhours (Median)
BIA 9-1067Rasagiline
BIA 9-1067 1h Before Rasagiline3.000.5
BIA 9-1067 Alone3.00NA
BIA 9-1067 Concomitant Rasagiline2.500.5

Change From Baseline to Week 18 in the Unified Parkinson's Disease Rating Scale (UPDRS) Total Score for Part II - Activities of Daily Living

The UPDRS was developed as a comprehensive tool to monitor the impact of Parkinson's Disease and the degree of disability caused. UPDRS contains four parts, the second of which is reported in this outcome. Part II is the participants' evaluation of the disease's impact on normal activities. Part II contains a total of 13 questions, which are each rated on a scale of 0 (normal or no disease effect) to 4 (maximum negative effect), for a total scale of 0-52. Negative change from baseline values indicate improvement. (NCT01049984)
Timeframe: Day 0 (baseline), Week 18

Interventionunits on a scale (Least Squares Mean)
Rasagiline 1 mg-0.1
Placebo0.3

Change From Baseline to Week 18 in the Unified Parkinson's Disease Rating Scale (UPDRS) Total Score for Part III - Motor Function

"The UPDRS was developed as a comprehensive tool to monitor the impact of Parkinson's Disease and the degree of disability caused. Version 3 of UPDRS contains four parts, the third of which is reported in this outcome. Part III is a clinician's evaluation of motor function. Part III contains 14 questions, which are each rated on a scale of 0 (normal or no disease effect) to 4 (maximum negative effect), for a total scale of 0-56. Negative change from baseline values indicate improvement.~All site raters (medical doctor [MD], doctor of osteopathy [DO], nurse practitioner, or physician assistant) received training on how to complete the UPDRS. The same site rater completed the UPDRS at all visits" (NCT01049984)
Timeframe: Day 0 (baseline), Week 18

Interventionunits on a scale (Least Squares Mean)
Rasagiline 1 mg-3.4
Placebo-1.6

Change From Baseline to Week 18 in the Unified Parkinson's Disease Rating Scale (UPDRS) Total Score for Parts I, II and III

"The UPDRS was developed as a comprehensive tool to monitor the impact of Parkinson's Disease and the degree of disability caused. Version 3 of UPDRS contains four parts, three of which are totaled and reported in this outcome. Part I is a clinician's evaluation of mentation (mental activity or state of mind), cognition (ability to acquire knowledge), behaviour and mood. Part II is the participants' evaluation of the disease's impact on normal activities. Part III is a clinician's evaluation of motor function. Parts I, II, and III contain a total of 31 questions, which are each rated on a scale of 0 (normal or no disease effect) to 4 (maximum negative effect), for a total scale of 0-124. Negative change from baseline values indicate improvement.~All site raters (medical doctor [MD], doctor of osteopathy [DO], nurse practitioner, or physician assistant) received training on how to complete the UPDRS. The same site rater completed the UPDRS at all visits." (NCT01049984)
Timeframe: Day 0 (baseline), Week 18

Interventionunits on a scale (Least Squares Mean)
Rasagiline 1 mg-3.6
Placebo-1.2

Clinical Global Improvement (CGI) Score at Week 18 As Assessed by the Participant

CGI is used by the participant to rate his/her total improvement during the study. Specifically, participants are asked to compare their condition at the beginning of the study to his/her condition at Week 18, how much has he/she changed? Answers are 0 (not assessed), 1 (very much improved), 2 (much improved), 3 (minimally improved), 4 (no change), 5 (minimally worse), 6 (much worse), 7(very much worse). (NCT01049984)
Timeframe: 18 weeks

,
Interventionparticipants (Number)
Not assessed (0)Very much improved (1)Much improved (2)Minimally improved (3)No change (4)Minimally worse (5)Much worse (6)Very much worse (7)
Placebo171840523581
Rasagiline 1 mg071839523652

Clinical Global Improvement (CGI) Score at Week 18 As Assessed by the Site Rater

"CGI is used by the site rater to rate participants total improvement during the study whether or not, in the investigators' judgment, it is due entirely to drug treatment. Specifically, site raters are asked to compare the participants condition at the beginning of the study to his/her condition at Week 18, how much has he/she changed? Answers are 0 (not assessed), 1 (very much improved), 2 (much improved), 3 (minimally improved), 4 (no change), 5 (minimally worse), 6 (much worse), 7(very much worse).~Site raters can be the medical doctor [MD], doctor of osteopathy [DO], nurse practitioner, or physician assistant." (NCT01049984)
Timeframe: 18 weeks

,
Interventionparticipants (Number)
Not assessed (0)Very much improved (1)Much improved (2)Minimally improved (3)No change (4)Minimally worse (5)Much worse (6)Very much worse (7)
Placebo152039534211
Rasagiline 1 mg052145632131

Illness Severity Score at Day 0 and Week 18 As Assessed by the Site Rater

"Site raters were asked: Considering your total clinical experience with the particular population, how ill is the patient at this time? Answers were based on a 0-7 scale, with 0=not assessed, 1= normal, not at all ill, and 7= among the most extremely ill of patients.~Site raters can be the medical doctor [MD], doctor of osteopathy [DO], nurse practitioner, or physician assistant." (NCT01049984)
Timeframe: Day 0 (baseline), Week 18

,
Interventionparticipants (Number)
Day 0: Not assessed (0)Day 0: Normal, not at all ill (1)Day 0: Borderline ill (2)Day 0: Mildly Ill (3)Day 0: Moderately Ill (4)Day 0: Markedly ill (5)Day 0: Severely ill (6)Day 0: Among the most extremely ill (7)Week 18: Not assessed (0)Week 18: Normal, not at all ill (1)Week 18: Borderline ill (2)Week 18: Mildly ill (3)Week 18: Moderately ill (4)Week 18: Markedly ill (5)Week 18: Severely ill (6)Week 18: Among the most extremely ill (7)
Placebo05261002820025338931110
Rasagiline 1 mg04189539100010289029200

Change From Baseline to Week 26 in Subscale Scores of the UPDRS (Part I)

The Unified Parkinson's Disease Rating Scale (UPDRS) Part I evaluates mentation, behaviour and mood symptoms, it comprises 4 parts and the score ranges from 0 (normal) to 16 (severe impairement) (NCT01556165)
Timeframe: Baseline to Week 26

Interventionunits on a scale (Mean)
Placebo0.08
Rasagiline-0.54

Change From Baseline to Week 26 in Subscale Scores of the UPDRS (Part II)

The Unified Parkinson's Disease Rating Scale (UPDRS) Part II evaluates activities of daily living, it comprises 13 parts and the score ranges from 0 (normal) to 52 (severe impairement and disability) (NCT01556165)
Timeframe: Baseline to Week 26

Interventionunits on a scale (Mean)
Placebo0.25
Rasagiline-0.43

Change From Baseline to Week 26 in Subscale Scores of the UPDRS (Part III)

The Unified Parkinson's Disease Rating Scale (UPDRS) Part III evaluates motor function, it comprises 14 parts and the score ranges from 0 (normal) to 108 (severe impairement and disability) (NCT01556165)
Timeframe: Baseline to Week 26

Interventionunits on a scale (Mean)
Placebo-0.52
Rasagiline-2.23

Change From Baseline to Week 26 in UPDRS Total Score

The Unified Parkinson's Disease Rating Scale (UPDRS) is a 42-item rating scale designed to assess Parkinson's disease-related disability and impairment. The scale comprises four parts: Part I evaluates mentation, behaviour, and mood symptoms; Part II evaluates activities of daily living (ADL); Part III evaluates motor function; and Part IV evaluates complications of dopaminergic therapy. The total score is the sum of the subscale scores for Parts I to III and ranges from 0 (no disability) to 176 (total dependence). (NCT01556165)
Timeframe: Baseline to Week 26

Interventionunits on a scale (Mean)
Placebo-0.18
Rasagiline-3.18

Change From Baseline to Week 24 in the Montreal Cognitive Assessment (MoCA) Score

The MoCA assesses 8 cognitive areas: visuospatial/executive, naming, memory, attention, language, abstraction, delayed recall, and orientation. Scores range from 0 (worst) to 30 (best). (NCT01723228)
Timeframe: Baseline to Week 24 (or early discontinuation)

Interventionunits on a scale (Least Squares Mean)
Rasagiline 1.0 mg/Day0.9
Placebo1.0

Change From Baseline to Week 24 in the Penn Daily Activities Questionnaire (PDAQ) Score

The PDAQ is a 15-item questionnaire that assesses the patient's difficulty with activities of daily living. The total score has a range of 0 (no impairment) to 60 (severe impairment). (NCT01723228)
Timeframe: Baseline to Week 24 (or early discontinuation)

Interventionunits on a scale (Least Squares Mean)
Rasagiline 1.0 mg/Day-0.9
Placebo-0.1

Change From Baseline to Week 24 in the Unified Parkinson's Disease Rating Scale (UPDRS), Motor Subscale (Part 3), Version 3, Score

UPDRS Part 3 (motor examination subscale) comprises 14 items assessing the motor disabilities of the patient at the time of the visit. The participant's speech, facial expressions, ability to arise from a chair (with arms folded), posture, gait, postural stability (retropulsion test), and body bradykinesia and hypokinesia are assessed. In addition, the following evaluations require assessment of the face, neck or extremities: tremor at rest, action or postural tremor of hands, rigidity, finger taps, hand movements (open and close), rapid alternating movements of hands (pronation and supination), and leg agility (tap heel on ground). This evaluation is performed while the participant is in the 'on' phase. Each item is assessed on a scale from 0 (normal, absent, or none) to 4 (severe impairment), which are summed to get the sub-scale score. The total scale is 0-57 with a higher score indicating more severe symptoms; a decrease in the scores indicates improvement. (NCT01723228)
Timeframe: Baseline to Week 24 (or early discontinuation)

Interventionunits on a scale (Least Squares Mean)
Rasagiline 1.0 mg/Day-3.7
Placebo-1.2

Change From Baseline to Week 24 in UPDRS, Activities of Daily Living (ADL) Subscale (Part 2), Version 3, Score

UPDRS Part 2 (ADL subscale) comprises 13 items evaluating the impact of PD on patients' ADL (in both the on and off states) in the week prior to the visit. The following 13 ADL are assessed: speech, salivation, swallowing, handwriting, cutting food and handling utensils, dressing, hygiene, turning in bed and adjusting bed clothes, falling (unrelated to freezing), freezing when walking, walking, tremor, and sensory complaints related to Parkinsonism. Each item is assessed on a scale from 0 (normal, absent, or none) to 4 (severe impairment), which are summed to get the sub-scale score. The total scale is 0-52 with a higher score indicating more severe symptoms; a decrease in the scores indicates improvement. (NCT01723228)
Timeframe: Baseline to week 24 (or early discontinuation)

Interventionunits on a scale (Least Squares Mean)
Rasagiline 1.0 mg/Day-0.9
Placebo1.4

Mean Change From Baseline to Week 24 in the Scales for Outcomes in Parkinson's Disease-Cognition (SCOPA-COG) Summary Score

The SCOPA-COG consists of evaluations in 4 domains: memory, attention, executive functioning, and visuospatial functioning.Scores range from 0 to 43, with higher scores reflecting better performance. (NCT01723228)
Timeframe: Baseline to Week 24 (or early discontinuation)

Interventionunits on a scale (Least Squares Mean)
Rasagiline 1.0 mg/Day1.6
Placebo0.8

Alzheimer's Disease Cooperative Study's Clinical Global Impression of Change Modified for Mild Cognitive Impairment (ADCS MCI-CGIC) Score at Week 24

The ADCS MCI-CGIC score is generated in the context of a semi-structured interview and is an indication of the change in the participant's global status, cognition, behavior, and functional abilities (FA) on a 7-point scale, with the best score being 'marked improvement' and the worst being 'marked worsening.' (NCT01723228)
Timeframe: Week 24 (or early discontinuation)

,
Interventionparticipants (Number)
CGIC: Marked improvement; n=78, 79CGIC: Moderate improvement; n=78, 79CGIC: Minimal improvement; n=78, 79CGIC: No change; n=78, 79CGIC: Minimal worsening; n=78, 79CGIC: Moderate worsening; n=78, 79CGIC: Marked worsening; n=78, 79CGIC Cognition: Marked improvement; n=77, 79CGIC Cognition: Moderate improvement; n=77, 79CGIC Cognition: Minimal improvement; n=77, 79CGIC Cognition: No change; n=77, 79CGIC Cognition: Minimal worsening; n=77, 79CGIC Cognition: Moderate worsening; n=77, 79CGIC Cognition: Marked worsening; n=77, 79CGIC Behavior: Marked improvement; n=76, 79CGIC Behavior: Moderate improvement; n=76, 79CGIC Behavior: Minimal improvement; n=76, 79CGIC Behavior: No change; n=76, 79CGIC Behavior: Minimal worsening; n=76, 79CGIC Behavior: Moderate worsening; n=76, 79CGIC Behavior: Marked worsening; n=76, 79CGIC FA: Marked improvement; n=76, 79CGIC FA: Moderate improvement; n=76, 79CGIC FA: Minimal improvement; n=76, 79CGIC FA: No change; n=76, 79CGIC FA: Minimal worsening; n=76, 79CGIC FA: Moderate worsening; n=76, 79CGIC FA: Marked worsening; n=76, 79
Placebo4723331200341844820311162200341255500
Rasagiline 1.0 mg/Day19114214100915419300411547000513441220

ALS Functional Rating Scale-Revised (ALSFRS-R)

Difference in ALS Functional Rating Scale - Revised (ALSFRS-R) score. The ALSFRS-R is an ordinal rating scale that assesses 12 functional activities. Each activity is scored between 0-4, with a total score ranging from 48 (normal function) to 0 (no function). (NCT01786603)
Timeframe: ALS Functional Rating Scale-Revised (ALSFRS-R) Difference from Baseline to Month 12

Interventionscore on a scale (Mean)
Rasagiline-1.00
Placebo-1.26

Change in Quality of Life

Participants completed the single-item ALSQOL (ALS Quality of Life) which asks participants to rank their global quality of life, considering all parts of their lives - physical, emotional, social, spiritual and financial - in the last 7 days and rate on a scale of 0 (very bad) to 10 (excellent). (NCT01786603)
Timeframe: Quality of Life Change from Baseline to Month 12

InterventionScore on a scale (Mean)
Rasagiline-0.09
Placebo-0.12

Change in Vital Capacity (VC)

Determine if decline in vital capacity is slower in participants taking 2 mg rasagiline than controls. (NCT01786603)
Timeframe: Vital Capacity Change from Baseline to Month 12

InterventionLiters (Mean)
Rasagiline-2.24
Placebo-2.48

Difference in Survival Status Between Study Groups

Determine if there is a difference in survival between participants on rasagiline than patients not on rasagiline (NCT01786603)
Timeframe: Survival status at Month 12

InterventionParticipants (Count of Participants)
Rasagiline55
Placebo19

Effect of Study Drug on Apoptosis Markers

Effect of rasagiline on the apoptosis markers (Annexin V stain) in participants with ALS. Assessed at baseline, month 6, and month 12; change from baseline to month 12 reported. Extra time point was not a pre-specified Primary or Secondary Outcome Measure. (NCT01786603)
Timeframe: Apoptosis Marker change from Baseline to Month 12

Interventionpercentage of change (Mean)
Rasagiline0.019
Placebo0.02

Effect of Study Drug on Oxidative Stress

Determine if oxygen radical antioxidant capacity is targeted by rasagiline in participants with ALS. Assessed at baseline, month 6, and month 12; change from baseline to month 12 reported. Extra time point was not a pre-specified Primary or Secondary Outcome Measure. (NCT01786603)
Timeframe: Oxidative Stress change from Baseline to Month 12

Interventionpmole/ml (Mean)
Rasagiline0.14
Placebo1.21

Number of Participants With Adverse Events

Determine if participants on rasagiline 2 mg had a different safety profile than patients not on rasagiline. Adverse event information to be collected from date of enrollment until end of study participation. (NCT01786603)
Timeframe: Adverse Events from Baseline to Month 12

InterventionParticipants (Count of Participants)
Rasagiline28
Placebo15

AUC0-t - Area Under the Plasma Concentration-time Curve From Time 0 to Last Observed Concentration

(NCT01532128)
Timeframe: pre-dose, and 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12, 16 and 24 h post-dose

,,
Interventionng.h/mL (Mean)
BIA 9-1067Rasagiline
Rasagiline 1 h After BIA 9-106721334.431
Rasagiline AloneNA4.323
Rasagiline Concomitant BIA 9-106719804.391

Cmax - Maximum Observed Plasma Concentration

(NCT01532128)
Timeframe: pre-dose, and 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12, 16 and 24 h post-dose

,,
Interventionng/mL (Mean)
BIA 9-1067Rasagiline
Rasagiline 1 h After BIA 9-10676726.058
Rasagiline AloneNA6152
Rasagiline Concomitant BIA 9-10676436.078

Tmax - Time of Occurrence of Cmax

(NCT01532128)
Timeframe: pre-dose, and 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12, 16 and 24 h post-dose

,,
Interventionhours (Median)
BIA 9-1067Rasagiline
Rasagiline 1 h After BIA 9-10672.000.50
Rasagiline AloneNA0.50
Rasagiline Concomitant BIA 9-10672.500.50

Change in ADAS-Cog 11 (Alzheimer's Disease Assessment Scale - Cognitive 11) Score

The ADAS-Cog 11 (Alzheimer's Disease Assessment Scale - Cognitive 11) is a psychometric instrument that evaluates memory, attention, reasoning, language, orientation, and praxis. A higher score indicates more impairment. Scores from the original portion of the test range from 0 (best) to 70 (worse). We used total ADAS-Cog 11 scores, which is a sum of individual subscales. We calculated the change by subtracting the ADAS Cog score at week 24 from baseline score. A positive change indicates cognitive worsening. (NCT02359552)
Timeframe: Mean change in scores from baseline to week 24

Interventionscore on a scale (Mean)
Placebo2.76
Rasagiline1.81

Change in ADCS-ADL (Alzheimer's Disease Cooperative Study-Activities of Daily Living) Score

Measure Description: The ADCS-ADL (Alzheimer's Disease Cooperative Study-Activities of Daily Living) is an activities-of-daily-living inventory developed by the ADCS to assess functional performance in participants with AD. Using a structured interview format, study partners are queried as to whether participants attempted each item in the inventory during the past 4 weeks and their level of performance. The ADCS-ADL provides a total score from 0-78, with a lower score indicating greater severity. We calculated change by subtracting scores on week 24 test from the baseline score. A negative score indicates worsening ability to complete ADLs. (NCT02359552)
Timeframe: Mean change in scores from baseline to week 24

Interventionscore on a scale (Mean)
Placebo-3.23
Rasagiline-3.75

Change in COWAT (Controlled Oral Word Association Test) Score

"Measure Description: Study participants are instructed, I want to see how many words you can say beginning with a certain letter in one minute. The study participant's responses are recorded on the worksheet. Study participants are then given an additional one minute for each of two different letters using similar instructions. The score is the total number of acceptable words for the three trials combined. A higher score represents better performance.~Responses are then judged for their acceptability (example for the use of proper nouns, numbers, repetitions and stem word with a different ending). The score is the total number of acceptable words for the three trials combined. A higher score represents better performance. We calculated change by subtracting week 24 scores from baseline scores. A negative score indicates worse performance." (NCT02359552)
Timeframe: Mean change in scores from baseline to week 24

Interventionscore on a scale (Mean)
Placebo-1.09
Rasagiline0.62

Change in Digit Span

Measure Description: The Digit Span consists of repetition of increasing long strings of digits presented at 1 per second as read by the examiner and repeated by the subject.The score is the maximum number of digits the patient can repeat until they fail twice in a row. The reverse digit span is identical to the forward digit span except that the patient repeats the presented digits in reverse order. The score is the maximum number of digits the patient can repeat in reverse order until they fail twice in a row. Each correct response is worth one point with a maximum total score of 28. A higher score is better. We calculated change by subtracting week 24 score from baseline score. A negative score indicates worse performance over the course of study. (NCT02359552)
Timeframe: Mean change in scores from baseline to week 24

Interventionscore on a scale (Mean)
Placebo-1.18
Rasagiline-0.29

Change in MMSE (Mini Mental Status Examination) Score

Measure Description: The MMSE (Mini Mental Status Examination) is a brief, frequently used screening instrument for AD drug studies. The MMSE evaluates orientation, memory, attention, concentration, naming, repetition, comprehension, and ability to create a sentence and to copy two overlapping pentagons. A lower score indicates more cognitive impairment. The highest score is 30, range is between 0 (severe impairment) and 30 (cognitively normal). We calculated the change in scores by subtracting week 24 score from baseline. A negative score indicates clinical worsening. (NCT02359552)
Timeframe: Mean change in scores from baseline to week 24

Interventionscore on a scale (Mean)
Placebo-1.14
Rasagiline-0.65

Change in NPI (Neuropsychiatric Inventory) Score

Measure Description: The behavioral outcome measure for this trial is the NPI (Neuropsychiatric Inventory). The NPI evaluates both the frequency and severity of 10 neuropsychiatric disturbances. Frequency assessments range from 1 (occasionally, less than once per week) to 4 (very frequently, once or more per day or continuously) as well as severity (1=mild, 2=moderate, 3=severe). The overall score is calculated by summing the severity and frequency of the subscale measures. The range of scores is 0-40. A score of 0 indicates no behavioral impairment and a score of 40 indicates severe behavioral impairment. We calculated change by subtracting Week 24 scores from baseline scores. A positive change indicates behavioral worsening. (NCT02359552)
Timeframe: Mean change in scores from baseline to week 24

Interventionscore on a scale (Mean)
Placebo2
Rasagiline0.2

Change in QoL-AD (Quality of Life - Alzheimer's Disease) Score

Measure Description: The QoL-AD (Quality of Life - Alzheimer's Disease) is a commonly used 13 item QoL scale that assesses items specific to QoL in patients with cognitive impairment. It is administered to the research partner with answers for the patient. Points are assigned to each item as follows: poor = 1, fair = 2, good = 3, excellent = 4.The total score is the sum of all 13 items. The range of score is from 0-52. We calculated the change by subtracting the scores on week 24 score from baseline. A negative value indicates worsening quality of life. (NCT02359552)
Timeframe: This assessment will be performed at the Baseline and Week 24 visits.

Interventionscore on a scale (Mean)
Placebo-1.95
Rasagiline1.11

Change in Regional Glucose Metabolism Between Week 24 and Baseline as Measured by 18F-2-fluoro-2-deoxy-D-glucose Positron Emission Tomography (FDG-PET).

The primary outcome measure is the change from baseline to week 24 in FDG-PET as measured by Standard Uptake Units Regional (SUVR) in several pre-specified brain regions including the medial temporal, lateral temporal, posterior cingulate - precuneus, inferior parietal, middle frontal, anterior cingulate, and striatum. The SUVR change was calculated by subtracting the value at 24 weeks from baseline values. Negative values indicate increased hypometabolism (i.e. worsening of cell function). (NCT02359552)
Timeframe: 24 weeks

,
InterventionSUVR (Mean)
Middle FrontalAnterior CingulateSuperior FrontalStriatumMedial TemporalLateral TemporalPost Cingulate - PrecuneusInferior Parietal
Placebo-0.032-0.020-0.016-0.024-0.015-0.020-0.017-0.025
Rasagiline-0.011-0.003-0.003-0.002-0.010-0.016-0.016-0.018

Research Highlights

Safety/Toxicity (32)

ArticleYear
Safety comparisons among monoamine oxidase inhibitors against Parkinson's disease using FDA adverse event reporting system.
Scientific reports, 11-06, Volume: 13, Issue: 1
2023
Effectiveness and safety of safinamide in the Toledo Movement Disorders Unit.
Revista de neurologia, 10-31, Volume: 77, Issue: S03
2023
Safety and Effectiveness of Rasagiline in Chinese Patients with Parkinson's Disease: A Prospective, Multicenter, Non-interventional Post-marketing Study.
Drug safety, Volume: 46, Issue: 7
2023
Comparative efficacy and safety of monoamine oxidase type B inhibitors plus channel blockers and monoamine oxidase type B inhibitors as adjuvant therapy to levodopa in the treatment of Parkinson's disease: a network meta-analysis of randomized controlled
European journal of neurology, Volume: 30, Issue: 4
2023
Effectiveness and safety of safinamide in routine clinical practice in a Belgian Parkinson's disease population: an open-label, levodopa add-on study.
Acta neurologica Belgica, Volume: 123, Issue: 3
2023
Overnight switch from rasagiline to safinamide in Parkinson's disease patients with motor fluctuations: a tolerability and safety study.
European journal of neurology, Volume: 28, Issue: 1
2021
Rasagiline and selegiline modulate mitochondrial homeostasis, intervene apoptosis system and mitigate α-synuclein cytotoxicity in disease-modifying therapy for Parkinson's disease.
Journal of neural transmission (Vienna, Austria : 1996), Volume: 127, Issue: 2
2020
Pharmacokinetics, Pharmacodynamics, and Safety of a Single Escalating Dose and Repeated Doses of Rasagiline Transdermal Patch in Healthy Chinese Subjects.
Clinical pharmacology in drug development, Volume: 9, Issue: 5
2020
Long-term safety and efficacy of adjunctive rasagiline in levodopa-treated Japanese patients with Parkinson's disease.
Journal of neural transmission (Vienna, Austria : 1996), Volume: 126, Issue: 3
2019
Aldehyde adducts inhibit 3,4-dihydroxyphenylacetaldehyde-induced α-synuclein aggregation and toxicity: Implication for Parkinson neuroprotective therapy.
European journal of pharmacology, Feb-15, Volume: 845
2019
Pharmacokinetics and safety of single and multiple doses of rasagiline in healthy Japanese and caucasian subjects.
Basic & clinical pharmacology & toxicology, Volume: 124, Issue: 3
2019
Safety and efficacy of rasagiline as an add-on therapy to riluzole in patients with amyotrophic lateral sclerosis: a randomised, double-blind, parallel-group, placebo-controlled, phase 2 trial.
The Lancet. Neurology, Volume: 17, Issue: 8
2018
Efficacy and safety of adjunctive rasagiline in Japanese Parkinson's disease patients with wearing-off phenomena: A phase 2/3, randomized, double-blind, placebo-controlled, multicenter study.
Parkinsonism & related disorders, Volume: 53
2018
Pharmacokinetics, Pharmacodynamics, and Safety of Rasagiline Transdermal Patch: A Preliminary Study in Healthy Chinese Subjects.
Clinical drug investigation, Volume: 38, Issue: 2
2018
Safety and efficacy of rasagiline in addition to levodopa for the treatment of idiopathic Parkinson's disease: a meta-analysis of randomised controlled trials.
European neurology, Volume: 73, Issue: 1-2
2015
Serotonin toxicity association with concomitant antidepressants and rasagiline treatment: retrospective study (STACCATO).
Pharmacotherapy, Volume: 34, Issue: 12
2014
Protective effect of rasagiline in aminoglycoside ototoxicity.
Neuroscience, Apr-18, Volume: 265
2014
Cardiac safety of rasagiline, a selective monoamine oxidase type B inhibitor for the treatment of Parkinson's disease: a thorough QT/QTc study.
International journal of clinical pharmacology and therapeutics, Volume: 52, Issue: 3
2014
Rasagiline meta-analysis: a spotlight on clinical safety and adverse events when treating Parkinson's disease.
Expert opinion on drug safety, Volume: 12, Issue: 4
2013
Efficacy and safety of rasagiline as an adjunct to levodopa treatment in Chinese patients with Parkinson's disease: a randomized, double-blind, parallel-controlled, multi-centre trial.
The international journal of neuropsychopharmacology, Volume: 16, Issue: 7
2013
Evaluation of the safety and tolerability of rasagiline in the treatment of the early stages of Parkinson's disease.
Current medical research and opinion, Volume: 29, Issue: 1
2013
Indirect comparisons of adverse events and dropout rates in early Parkinson's disease trials of pramipexole, ropinirole, and rasagiline.
The International journal of neuroscience, Volume: 122, Issue: 7
2012
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
PLoS computational biology, Volume: 7, Issue: 12
2011
Efficacy, safety and tolerability of rasagiline as adjunctive therapy in elderly patients with Parkinson's disease.
European journal of neurology, Volume: 19, Issue: 2
2012
Safety of rasagiline for the treatment of Parkinson's disease.
Expert opinion on drug safety, Volume: 10, Issue: 4
2011
Site-activated chelators derived from anti-Parkinson drug rasagiline as a potential safer and more effective approach to the treatment of Alzheimer's disease.
Neurochemical research, Volume: 35, Issue: 12
2010
TVP1022 and propargylamine protect neonatal rat ventricular myocytes against doxorubicin-induced and serum starvation-induced cardiotoxicity.
Journal of cardiovascular pharmacology, Volume: 52, Issue: 3
2008
Safety of rasagiline in elderly patients with Parkinson disease.
Neurology, May-09, Volume: 66, Issue: 9
2006
Tolerability, safety, pharmacodynamics, and pharmacokinetics of rasagiline: a potent, selective, and irreversible monoamine oxidase type B inhibitor.
Pharmacotherapy, Volume: 24, Issue: 10
2004
Monoamine oxidase-inhibition and MPTP-induced neurotoxicity in the non-human primate: comparison of rasagiline (TVP 1012) with selegiline.
Journal of neural transmission (Vienna, Austria : 1996), Volume: 108, Issue: 8-9
2001
Prevention of MPTP-induced neurotoxicity by AGN-1133 and AGN-1135, selective inhibitors of monoamine oxidase-B.
European journal of pharmacology, Oct-22, Volume: 116, Issue: 3
1985
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Long-term Use (10)

ArticleYear
Isradipine, an L-type calcium channel inhibitor, attenuates cue-associated methamphetamine-seeking in mice.
Brain research, 11-01, Volume: 1818
2023
Influence of DRD1 and DRD3 Polymorphisms in the Occurrence of Motor Effects in Patients with Sporadic Parkinson's Disease.
Neuromolecular medicine, Volume: 21, Issue: 3
2019
Rasagiline, an inhibitor of MAO-B, decreases colonic motility through elevating colonic dopamine content.
Neurogastroenterology and motility, Volume: 30, Issue: 11
2018
Efficacy of rasagiline and selegiline in Parkinson's disease: a head-to-head 3-year retrospective case-control study.
Journal of neurology, Volume: 264, Issue: 6
2017
Free-water and BOLD imaging changes in Parkinson's disease patients chronically treated with a MAO-B inhibitor.
Human brain mapping, Volume: 37, Issue: 8
2016
Molecular basis of neuroprotective activities of rasagiline and the anti-Alzheimer drug TV3326 [(N-propargyl-(3R)aminoindan-5-YL)-ethyl methyl carbamate].
Cellular and molecular neurobiology, Volume: 21, Issue: 6
2001
Rasagiline [N-propargyl-1R(+)-aminoindan], a selective and potent inhibitor of mitochondrial monoamine oxidase B.
British journal of pharmacology, Volume: 132, Issue: 2
2001
Mechanism underlying anti-apoptotic activity of a (-)deprenyl-related propargylamine, rasagiline.
Mechanisms of ageing and development, Jul-31, Volume: 116, Issue: 2-3
2000
Effect of long-term treatment with selective monoamine oxidase A and B inhibitors on dopamine release from rat striatum in vivo.
Journal of neurochemistry, Volume: 67, Issue: 4
1996
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Pharmacokinetics (13)

ArticleYear
Pharmacokinetics, Pharmacodynamics, and Safety of a Single Escalating Dose and Repeated Doses of Rasagiline Transdermal Patch in Healthy Chinese Subjects.
Clinical pharmacology in drug development, Volume: 9, Issue: 5
2020
Pharmacokinetics and safety of single and multiple doses of rasagiline in healthy Japanese and caucasian subjects.
Basic & clinical pharmacology & toxicology, Volume: 124, Issue: 3
2019
Pharmacokinetics, Pharmacodynamics, and Safety of Rasagiline Transdermal Patch: A Preliminary Study in Healthy Chinese Subjects.
Clinical drug investigation, Volume: 38, Issue: 2
2018
Simultaneous bioanalysis of rasagiline and its major metabolites in human plasma by LC-MS/MS: Application to a clinical pharmacokinetic study.
Journal of pharmaceutical and biomedical analysis, Jun-05, Volume: 125
2016
Pharmacokinetics of Rasagiline in Healthy Adult Chinese Volunteers with Various Genotypes: A Single-Center, Open-Label, Multiple-Dose Study.
Clinical drug investigation, Volume: 36, Issue: 5
2016
Pharmacokinetic interaction study between flavanones (hesperetin, naringenin) and rasagiline mesylate in wistar rats.
Drug development and industrial pharmacy, Volume: 42, Issue: 7
2016
Pharmacokinetic/pharmacodynamic evaluation of rasagiline mesylate for Parkinson's disease.
Expert opinion on drug metabolism & toxicology, Volume: 10, Issue: 10
2014
Comparative single-dose pharmacokinetics of rasagiline in minipigs after oral dosing or transdermal administration via a newly developed patch.
Xenobiotica; the fate of foreign compounds in biological systems, Volume: 43, Issue: 8
2013
LC method for determination of rasagiline mesylate in different plasma matrices and its application to oral pharmacokinetic study in rabbits.
Journal of chromatographic science, Volume: 51, Issue: 1
2013
TVP1022 attenuates cardiac remodeling and kidney dysfunction in experimental volume overload-induced congestive heart failure.
Circulation. Heart failure, Volume: 4, Issue: 4
2011
Rapid and sensitive liquid chromatography-tandem mass spectrometry: assay development, validation and application to a human pharmacokinetic study.
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences, Nov-15, Volume: 875, Issue: 2
2008
Validated LC-MS/MS method for quantitative determination of rasagiline in human plasma and its application to a pharmacokinetic study.
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences, Oct-01, Volume: 873, Issue: 2
2008
Tolerability, safety, pharmacodynamics, and pharmacokinetics of rasagiline: a potent, selective, and irreversible monoamine oxidase type B inhibitor.
Pharmacotherapy, Volume: 24, Issue: 10
2004
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioavailability (12)

ArticleYear
Preparation and
Archives of Razi Institute, Volume: 78, Issue: 3
2023
Thin film hydration versus modified spraying technique to fabricate intranasal spanlastic nanovesicles for rasagiline mesylate brain delivery: Characterization, statistical optimization, and in vivo pharmacokinetic evaluation.
Drug delivery and translational research, Volume: 13, Issue: 4
2023
Influence of chitosan thioglycolic acid conjugate in improving bioavailability of an antiparkinson drug; Rasagiline Mesylate from transdermal patch.
Drug development and industrial pharmacy, Volume: 47, Issue: 6
2021
Microemulsion-based gel for the transdermal delivery of rasagiline mesylate: In vitro and in vivo assessment for Parkinson's therapy.
European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V, Volume: 165
2021
Impact of rasagiline nanoparticles on brain targeting efficiency via gellan gum based transdermal patch: A nanotheranostic perspective for Parkinsonism.
International journal of biological macromolecules, Dec-01, Volume: 164
2020
Pharmacokinetic interaction study between flavanones (hesperetin, naringenin) and rasagiline mesylate in wistar rats.
Drug development and industrial pharmacy, Volume: 42, Issue: 7
2016
Brain targeted nanoparticulate drug delivery system of rasagiline via intranasal route.
Drug delivery, Volume: 23, Issue: 1
2016
Nasal in-situ gels for delivery of rasagiline mesylate: improvement in bioavailability and brain localization.
Drug delivery, Volume: 22, Issue: 7
2015
Comparative single-dose pharmacokinetics of rasagiline in minipigs after oral dosing or transdermal administration via a newly developed patch.
Xenobiotica; the fate of foreign compounds in biological systems, Volume: 43, Issue: 8
2013
Monoamine oxidase-B inhibition in the treatment of Parkinson's disease.
Pharmacotherapy, Volume: 27, Issue: 12 Pt 2
2007
Community and long-term care management of Parkinson's disease in the elderly: focus on monoamine oxidase type B inhibitors.
Drugs & aging, Volume: 24, Issue: 8
2007
Recent advances in Parkinson's disease therapy: use of monoamine oxidase inhibitors.
Expert review of neurotherapeutics, Volume: 5, Issue: 6
2005
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Dosage (27)

ArticleYear
Efficacy of rasagiline monotherapy for early Parkinson disease: A systematic review and meta-analysis of randomized controlled trials.
Journal of psychopharmacology (Oxford, England), Volume: 36, Issue: 6
2022
P2B001 (Extended Release Pramipexole and Rasagiline): A New Treatment Option in Development for Parkinson's Disease.
Advances in therapy, Volume: 39, Issue: 5
2022
Impact of rasagiline nanoparticles on brain targeting efficiency via gellan gum based transdermal patch: A nanotheranostic perspective for Parkinsonism.
International journal of biological macromolecules, Dec-01, Volume: 164
2020
Pharmacokinetics, Pharmacodynamics, and Safety of a Single Escalating Dose and Repeated Doses of Rasagiline Transdermal Patch in Healthy Chinese Subjects.
Clinical pharmacology in drug development, Volume: 9, Issue: 5
2020
Influence of DRD1 and DRD3 Polymorphisms in the Occurrence of Motor Effects in Patients with Sporadic Parkinson's Disease.
Neuromolecular medicine, Volume: 21, Issue: 3
2019
Monoamine oxidase-B inhibitors in the treatment of Parkinson's disease: clinical-pharmacological aspects.
Journal of neural transmission (Vienna, Austria : 1996), Volume: 125, Issue: 11
2018
Simultaneous determination of MAO-A and -B activity following first time intake of an irreversible MAO-B inhibitor in patients with Parkinson's disease.
Journal of neural transmission (Vienna, Austria : 1996), Volume: 124, Issue: 6
2017
Intensive rehabilitation treatment in early Parkinson's disease: a randomized pilot study with a 2-year follow-up.
Neurorehabilitation and neural repair, Volume: 29, Issue: 2
2015
Randomized, controlled trial of rasagiline as an add-on to dopamine agonists in Parkinson's disease.
Movement disorders : official journal of the Movement Disorder Society, Volume: 29, Issue: 8
2014
Comparative single-dose pharmacokinetics of rasagiline in minipigs after oral dosing or transdermal administration via a newly developed patch.
Xenobiotica; the fate of foreign compounds in biological systems, Volume: 43, Issue: 8
2013
LC method for determination of rasagiline mesylate in different plasma matrices and its application to oral pharmacokinetic study in rabbits.
Journal of chromatographic science, Volume: 51, Issue: 1
2013
Comparison of oral and transdermal administration of rasagiline mesylate on human melanoma tumor growth in vivo.
Cutaneous and ocular toxicology, Volume: 31, Issue: 4
2012
Rasagiline: a review of its use in the treatment of idiopathic Parkinson's disease.
Drugs, Mar-26, Volume: 72, Issue: 5
2012
Electropharmacograms of rasagiline, its metabolite aminoindan and selegiline in the freely moving rat.
Neuropsychobiology, Volume: 62, Issue: 4
2010
The role of rasagiline in the treatment of Parkinson's disease.
Clinical interventions in aging, May-25, Volume: 5
2010
Efficacy and tolerability of rasagiline in daily clinical use--a post-marketing observational study in patients with Parkinson's disease.
European journal of neurology, Volume: 17, Issue: 9
2010
Low dosage of rasagiline and epigallocatechin gallate synergistically restored the nigrostriatal axis in MPTP-induced parkinsonism.
Neuro-degenerative diseases, Volume: 7, Issue: 4
2010
Development and validation of a reverse phase liquid chromatography method for the quantification of rasagiline mesylate in biodegradable PLGA microspheres.
Journal of pharmaceutical and biomedical analysis, Jul-12, Volume: 49, Issue: 5
2009
Comprehensive review of rasagiline, a second-generation monoamine oxidase inhibitor, for the treatment of Parkinson's disease.
Clinical therapeutics, Volume: 29, Issue: 9
2007
Rasagiline: a review of its use in the management of Parkinson's disease.
Drugs, Volume: 67, Issue: 12
2007
Rasagiline (TVP-1012): a new selective monoamine oxidase inhibitor for Parkinson's disease.
The American journal of geriatric pharmacotherapy, Volume: 4, Issue: 4
2006
Rasagiline: A second-generation monoamine oxidase type-B inhibitor for the treatment of Parkinson's disease.
American journal of health-system pharmacy : AJHP : official journal of the American Society of Health-System Pharmacists, May-15, Volume: 63, Issue: 10
2006
Rasagiline improves quality of life in patients with early Parkinson's disease.
Movement disorders : official journal of the Movement Disorder Society, Volume: 21, Issue: 5
2006
Neuropharmacological, neuroprotective and amyloid precursor processing properties of selective MAO-B inhibitor antiparkinsonian drug, rasagiline.
Drugs of today (Barcelona, Spain : 1998), Volume: 41, Issue: 6
2005
A controlled trial of rasagiline in early Parkinson disease: the TEMPO Study.
Archives of neurology, Volume: 59, Issue: 12
2002
Rasagiline [N-propargyl-1R(+)-aminoindan], a selective and potent inhibitor of mitochondrial monoamine oxidase B.
British journal of pharmacology, Volume: 132, Issue: 2
2001
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Interactions (2)

ArticleYear
Effects of rasagiline combined with levodopa and benserazide hydrochloride on motor function and homocysteine and IGF-1 levels in elderly patients with Parkinson's disease.
BMC neurology, Oct-06, Volume: 23, Issue: 1
2023
Rasagiline alone and in combination with riluzole prolongs survival in an ALS mouse model.
Journal of neurology, Volume: 251, Issue: 9
2004
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]