Page last updated: 2024-09-23

lazabemide

Description

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

Cross-References

ID SourceID
PubMed CID71307
CHEMBL ID279390
SCHEMBL ID121998
MeSH IDM0165002

Synonyms (46)

Synonym
bdbm50029816
5-chloro-pyridine-2-carboxylic acid (2-amino-ethyl)-amide
lazabemide (usan/inn)
103878-84-8
D04681
lazabemide
n-(2-aminoethyl)-5-chloropicolinamide
2-pyridinecarboxamide, n-(2-aminoethyl)-5-chloro-
ro 19-6327/000
ccris 7301
ro-19-6327
ro-196327
CHEMBL279390 ,
n-(2-aminoethyl)-5-chloropyridine-2-carboxamide
n-(2-aminoethyl)-5-chloro-2-pyridinecarboxamide
A800836
AKOS006272560
420hd787n9 ,
unii-420hd787n9
lazabemide [usan:inn:ban]
n-(2-aminoethyl)-5-chloro-2-pyridinecarboxamide hydrate
lazabemide hydrate
ro 19-6327 hydrate
FT-0631029
gtpl6640
SCHEMBL121998
lazabemide [usan]
lazabemide [inn]
lazabemide [mi]
lazabemide [mart.]
ro-19-6327/000
lazabemide [who-dd]
JZXRLKWWVNUZRB-UHFFFAOYSA-N
CS-4008
DTXSID2048294
n-(2-aminoethyl)-5-chloro-2-pyridine carboxamide
HY-14201
AC-27411
n-(2-aminoethyl)-5-chloro-2-pyridinecarboxamide;n-(2-aminoethyl)-5-chloro-2-pyridinecarboxamide
Q6505756
BRD-K51486818-002-01-2
N17089
BCP21224
ro-19-6327;ro 19-6327;ro 196327
MS-23081
EN300-267479

Research Excerpts

Overview

ExcerptReference
"Lazabemide (Ro 19-6327) is a short-acting, reversible, highly selective inhibitor of monoamine oxidase type B, that, unlike selegiline (deprenyl), is not metabolized to active compounds."( , 1994)
"Lazabemide (RO19-6327) is a short-acting, reversible, highly selective inhibitor of monoamine oxidase type B which, unlike deprenyl, is not metabolized to active compounds."( , 1993)
"Lazabemide (Ro 19-6327) is a relatively short-acting, reversible, and selective type B monoamine oxidase inhibitor that is not metabolized to amphetamines or other active compounds. "( , 1996)

Treatment

ExcerptReference
"Lazabemide treatment was as well tolerated as placebo and was not attended by serious adverse experiences. "( , 1994)
"Lazabemide treatment was as well tolerated as placebo and was not attended by serious adverse experiences."( , 1993)

Protein Targets (5)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
phosphopantetheinyl transferaseBacillus subtilisPotency63.09570.141337.9142100.0000AID1490
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Amine oxidase [flavin-containing] BRattus norvegicus (Norway rat)IC50 (µMol)0.03000.00040.764912.5000AID126695
Amine oxidase [flavin-containing] BRattus norvegicus (Norway rat)Ki0.03810.00081.09276.0000AID1192621; AID1192622
Amine oxidase [flavin-containing] A Rattus norvegicus (Norway rat)IC50 (µMol)10.00000.00071.979812.5000AID125713
Amine oxidase [flavin-containing] A Rattus norvegicus (Norway rat)Ki0.07220.00190.55334.8000AID1192621
Amine oxidase [flavin-containing] AHomo sapiens (human)IC50 (µMol)80.00000.00002.37899.7700AID1571214
Amine oxidase [flavin-containing] AHomo sapiens (human)Ki4,075.00000.00192.379710.0000AID1413448; AID1708793
Amine oxidase [flavin-containing] BHomo sapiens (human)IC50 (µMol)0.07700.00001.89149.5700AID1152189; AID1158611; AID1192164; AID1194962; AID1261174; AID1278145; AID1297408; AID1373672; AID1409012; AID1432432; AID1484647; AID1498690; AID1512063; AID1514581; AID1571215; AID1624338; AID1896030; AID718026; AID751623; AID773445
Amine oxidase [flavin-containing] BHomo sapiens (human)Ki0.03420.00061.777110.0000AID1192621; AID1192622; AID1413449; AID1708794; AID254307
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Amine oxidase [flavin-containing] BHomo sapiens (human)EC50 (µMol)7.10001.20004.15007.1000AID1192632
Amine oxidase [flavin-containing] BHomo sapiens (human)Kd0.06600.00900.11930.2754AID1192631
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (15)

Processvia Protein(s)Taxonomy
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)
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (7)

Processvia Protein(s)Taxonomy
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)
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (6)

Processvia Protein(s)Taxonomy
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)
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (81)

Assay IDTitleYearJournalArticle
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.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1708793Inhibition of recombinant human MAO-A expressed in baculovirus infected BTI insect cells using p-tyramine as substrate incubated for 30 mins by Amplex red reagent based fluorescence analysis2021Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4
New 2-Pyrazoline and Hydrazone Derivatives as Potent and Selective Monoamine Oxidase A Inhibitors.
AID718026Inhibition of human recombinant MAO-B expressed in insect cell microsome assessed as 4-hydroxyquinoline formation using kynuramine as substrate after 20 mins by fluorescence spectrophotometry2012Bioorganic & medicinal chemistry, Dec-15, Volume: 20, Issue:24
Inhibition of monoamine oxidase by 8-[(phenylethyl)sulfanyl]caffeine analogues.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1571214Inhibition of MAOA (unknown origin) using kynuramine as substrate preincubated for 30 mins followed by substrate addition2018MedChemComm, Nov-01, Volume: 9, Issue:11
Selected aryl thiosemicarbazones as a new class of multi-targeted monoamine oxidase inhibitors.
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID1571216Selectivity index, ratio of IC50 for MAOA (unknown origin) to IC50 for MAOB (unknown origin)2018MedChemComm, Nov-01, Volume: 9, Issue:11
Selected aryl thiosemicarbazones as a new class of multi-targeted monoamine oxidase inhibitors.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID773445Reversible inhibition of recombinant human MAO-B assessed as inhibition of kynuramine conversion to fluorescent metabolite 4-hydroxyquinoline after 20 mins by fluorescence spectrophotometry2013Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
Inhibition of monoamine oxidase by 3,4-dihydro-2(1H)-quinolinone derivatives.
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID1373684Inhibition of human recombinant MAOB assessed as residual enzyme activity at 2 time IC50 pre-incubated for 30 mins followed by 0.06 mM benzylamine substrate addition2018Bioorganic & medicinal chemistry letters, 02-15, Volume: 28, Issue:4
Selective inhibition of monoamine oxidase A by hispidol.
AID1571215Inhibition of MAOB (unknown origin) using benzylamine as substrate preincubated for 30 mins followed by substrate addition2018MedChemComm, Nov-01, Volume: 9, Issue:11
Selected aryl thiosemicarbazones as a new class of multi-targeted monoamine oxidase inhibitors.
AID1708806Cytotoxicity against human HepG2 cells assessed as cell viability at 30 uM incubated for 2 hrs by MTT assay relative to control2021Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4
New 2-Pyrazoline and Hydrazone Derivatives as Potent and Selective Monoamine Oxidase A Inhibitors.
AID1192633Inhibition of human recombinant soluble MAO-B assessed as change in melting temperature at 100 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.
AID1413451Competitive inhibition of recombinant human MAO-A assessed as reduction in H2O2 production preincubated for 30 mins followed by p-tyramine substrate addition measured after 30 mins by Lineweaver-Burk plot analysis
AID1708794Inhibition of recombinant human MAO-B expressed in baculovirus infected BTI insect cells using p-tyramine as substrate incubated for 30 mins by Amplex red reagent based fluorescence analysis2021Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4
New 2-Pyrazoline and Hydrazone Derivatives as Potent and Selective Monoamine Oxidase A Inhibitors.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1152188Inhibition of recombinant human MAO-A using kynuramine as substrate assessed as 4-hydroxyquinoline production after 30 mins by fluorescence spectrophotometry analysis2014Bioorganic & medicinal chemistry letters, Jun-15, Volume: 24, Issue:12
α-Tetralone derivatives as inhibitors of monoamine oxidase.
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
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.
AID125713In vitro inhibitory activity against rat brain Monoamine oxidase A1995Journal of medicinal chemistry, Nov-24, Volume: 38, Issue:24
Selective and potent monoamine oxidase type B inhibitors: 2-substituted 5-aryltetrazole derivatives.
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.
AID1409012Inhibition of recombinant human MAO-B using kynuramine as substrate after 20 mins by fluorescence spectrophotometric analysis2018Bioorganic & medicinal chemistry, 11-01, Volume: 26, Issue:20
Synthesis and evaluation of 2-substituted 4(3H)-quinazolinone thioether derivatives as monoamine oxidase inhibitors.
AID1432432Inhibition of recombinant human MAO-B using benzylamine as substrate preincubated for 30 mins followed by substrate addition2017Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5
Selective inhibition of monoamine oxidase A by purpurin, an anthraquinone.
AID1278145Inhibition of recombinant human MAO-B after 20 mins using 50 uM kynuramine as substrate by fluorescence spectrophotometry2016Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4
Inhibition of monoamine oxidase by benzoxathiolone analogues.
AID1192630Reversible inhibition of MAO-B in rat whole brain homogenate assessed as recovered activity at 100 times IC50 incubated for 60 mins followed by 6 washes by Amplex Red 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.
AID1373685Reversible inhibition of human recombinant MAOB assessed as residual enzyme activity at 2 times IC50 pre-incubated with enzyme for 30 mins followed by dialysis with pH 7.2 sodium phosphate buffer for 6 hrs followed by 0.06 mM benzylamine substrate additio2018Bioorganic & medicinal chemistry letters, 02-15, Volume: 28, Issue:4
Selective inhibition of monoamine oxidase A by hispidol.
AID1708798Reversible inhibition of human MAO-B assessed as residual enzyme activity at 4 fold IC50 incubated for 15 mins and measured before dialysis relative to control2021Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4
New 2-Pyrazoline and Hydrazone Derivatives as Potent and Selective Monoamine Oxidase A Inhibitors.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID1413448Inhibition of recombinant human MAO-A assessed as reduction in H2O2 production preincubated for 30 mins followed by p-tyramine substrate addition measured after 30 mins by amplex red reagent based fluorescence assay
AID751623Inhibition of human recombinant monoamine oxidase-B assessed as kynuramine conversion to 6-hydroxyquinoline after 20 mins by fluorescence spectrophotometric analysis2013Bioorganic & medicinal chemistry letters, Mar-01, Volume: 23, Issue:5
Inhibition of monoamine oxidase by phthalide analogues.
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID1158611Inhibition of recombinant human MAO-B expressed in insect cells assessed as inhibition of oxidation of kynuramine to 4-hydroxyquinoline after 20 mins by fluorescence spectrophotometry2014European journal of medicinal chemistry, Jul-23, Volume: 82New insights into the biological properties of Crocus sativus L.: chemical modifications, human monoamine oxidases inhibition and molecular modeling studies.
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID1194962Inhibition of human recombinant MAOB using kynuramine substrate assessed as reduction in MAO-generated 4-hydroxyquinoline level by fluorescence spectrophotometry2015Bioorganic & medicinal chemistry letters, May-01, Volume: 25, Issue:9
The synthesis and evaluation of sesamol and benzodioxane derivatives as inhibitors of monoamine oxidase.
AID1624337Inhibition of human recombinant MAO-A expressed in baculovirus infected BTI insect cells using kynuramine as substrate after 20 mins by spectrophotometric analysis2019Bioorganic & medicinal chemistry letters, 03-15, Volume: 29, Issue:6
Osthenol, a prenylated coumarin, as a monoamine oxidase A inhibitor with high selectivity.
AID1297408Inhibition of human recombinant MAO-B using kynuramine as substrate incubated for 20 mins by fluorescence spectrophotometric analysis2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
An evaluation of synthetic indole derivatives as inhibitors of monoamine oxidase.
AID1192164Inhibition of human recombinant MAO-B assessed as kynuramine oxidation to 4-hydroxyquinoline formation by spectrofluorometric analysis2015Bioorganic & medicinal chemistry letters, Mar-15, Volume: 25, Issue:6
Inhibition of monoamine oxidase by indole-5,6-dicarbonitrile derivatives.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID1192163Inhibition of human recombinant MAO-A assessed as kynuramine oxidation to 4-hydroxyquinoline formation by spectrofluorometric analysis2015Bioorganic & medicinal chemistry letters, Mar-15, Volume: 25, Issue:6
Inhibition of monoamine oxidase by indole-5,6-dicarbonitrile derivatives.
AID1708797Reversible inhibition of human MAO-A assessed as residual enzyme activity at 4 fold IC50 incubated for 15 mins and measured before dialysis by dialysis method relative to control2021Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4
New 2-Pyrazoline and Hydrazone Derivatives as Potent and Selective Monoamine Oxidase A Inhibitors.
AID1192632Inhibition of human recombinant soluble MAO-B assessed as thermal shift 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.
AID1571227Reversible inhibition of MAOB (unknown origin) assessed as residual enzyme activity at 0.08 uM using benzylamine as substrate measured after 30 mins relative to control2018MedChemComm, Nov-01, Volume: 9, Issue:11
Selected aryl thiosemicarbazones as a new class of multi-targeted monoamine oxidase inhibitors.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID1399990Acute toxicity in po dosed rat2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
Design, synthesis and biological evaluation of lazabemide derivatives as inhibitors of monoamine oxidase.
AID1413450Selectivity index, ratio of Ki for recombinant human MAO-B to Ki for recombinant human MAO-A
AID1413449Inhibition of recombinant human MAO-B assessed as reduction in H2O2 production preincubated for 30 mins followed by p-tyramine substrate addition measured after 30 mins by amplex red reagent based fluorescence assay
AID1708796Reversible inhibition of human MAO-A assessed as residual enzyme activity at 4 fold IC50 incubated for 15 mins and measured 24 hrs post dialysis by dialysis method relative to control2021Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4
New 2-Pyrazoline and Hydrazone Derivatives as Potent and Selective Monoamine Oxidase A Inhibitors.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID1514581Inhibition of recombinant human MAOB expressed in insect cell microsomes using kynuramine as substrate measured after 20 mins by fluorescence spectrophotometry2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
Novel monoamine oxidase inhibitors based on the privileged 2-imidazoline molecular framework.
AID1624340Competitive inhibition of human recombinant MAO-A expressed in baculovirus infected BTI insect cells using kynuramine as substrate after 20 mins by Lineweaver-Burk plot analysis2019Bioorganic & medicinal chemistry letters, 03-15, Volume: 29, Issue:6
Osthenol, a prenylated coumarin, as a monoamine oxidase A inhibitor with high selectivity.
AID1152189Inhibition of recombinant human MAO-B using kynuramine as substrate assessed as 4-hydroxyquinoline production after 30 mins by fluorescence spectrophotometry analysis2014Bioorganic & medicinal chemistry letters, Jun-15, Volume: 24, Issue:12
α-Tetralone derivatives as inhibitors of monoamine oxidase.
AID1498690Inhibition of recombinant human MAO-B using benzylamine as substrate incubated for 30 mins by spectrophotometric method2018Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
Selective inhibition of monoamine oxidase A by chelerythrine, an isoquinoline alkaloid.
AID1192165Selectivity index, ratio of IC50 for human recombinant MAO-B to IC50 for human recombinant MAO-A2015Bioorganic & medicinal chemistry letters, Mar-15, Volume: 25, Issue:6
Inhibition of monoamine oxidase by indole-5,6-dicarbonitrile derivatives.
AID1261174Inhibition of human MAO-B expressed in baculovirus infected BT1 cells microsome fraction by fluorescence spectrometry2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Monoamine oxidase inhibitory activities of heterocyclic chalcones.
AID1708799Reversible inhibition of human MAO-B assessed as residual enzyme activity at 4 fold IC50 incubated for 15 mins and measured 24 hrs post dialysis relative to control2021Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4
New 2-Pyrazoline and Hydrazone Derivatives as Potent and Selective Monoamine Oxidase A Inhibitors.
AID1896030Inhibition of MAO-B (unknown origin)2021Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
The Repertoire of Small-Molecule PET Probes for Neuroinflammation Imaging: Challenges and Opportunities beyond TSPO.
AID1624338Inhibition of human recombinant MAO-B expressed in baculovirus infected BTI insect cells using benzylamine as substrate after 30 mins by spectrophotometric analysis2019Bioorganic & medicinal chemistry letters, 03-15, Volume: 29, Issue:6
Osthenol, a prenylated coumarin, as a monoamine oxidase A inhibitor with high selectivity.
AID127198Inhibition of mitochondrial Monoamine oxidase-B purified from bovine liver1993Journal of medicinal chemistry, Nov-26, Volume: 36, Issue:24
New analogues of N-(2-aminoethyl)-4-chlorobenzamide (Ro 16-6491). Some of the most potent monoamine oxidase-B inactivators.
AID1708795Selectivity index, ratio of Ki for inhibition of recombinant human MAO-A to Ki for inhibition of recombinant human MAO-B using p-tyramine as substrate2021Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4
New 2-Pyrazoline and Hydrazone Derivatives as Potent and Selective Monoamine Oxidase A Inhibitors.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
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.
AID1373672Inhibition of human recombinant MAOB using benzylamine as substrate preincubated for 30 mins followed by substrate addition2018Bioorganic & medicinal chemistry letters, 02-15, Volume: 28, Issue:4
Selective inhibition of monoamine oxidase A by hispidol.
AID1571228Reversible inhibition of MAOB (unknown origin) assessed as residual enzyme activity at 0.08 uM using benzylamine as substrate pre-incubated for 30 mins followed by dialysis with pH 7.2 sodium phosphate buffer relative to control2018MedChemComm, Nov-01, Volume: 9, Issue:11
Selected aryl thiosemicarbazones as a new class of multi-targeted monoamine oxidase inhibitors.
AID234092Selectivity for the B form was estimated by the IC50(MAO A)/IC50(MAO B) ratio1995Journal of medicinal chemistry, Nov-24, Volume: 38, Issue:24
Selective and potent monoamine oxidase type B inhibitors: 2-substituted 5-aryltetrazole derivatives.
AID1484647Inhibition of recombinant human MAO-B expressed in baculovirus infected BTI insect cell microsomes using kynuramine as substrate after 20 mins by fluorescence spectroscopy2017European journal of medicinal chemistry, Jul-28, Volume: 135The evaluation of 1,4-benzoquinones as inhibitors of human monoamine oxidase.
AID1708805Cytotoxicity against human HepG2 cells assessed as cell viability at 15 uM incubated for 2 hrs by MTT assay relative to control2021Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4
New 2-Pyrazoline and Hydrazone Derivatives as Potent and Selective Monoamine Oxidase A Inhibitors.
AID1413453Reversible inhibition of recombinant human MAO-A assessed as enzyme activity recovery at 5 time Ki value preincubated for 15 mins followed by dilution of enzyme-inhibitor mixture for 24 hrs and subsequent p-tyramine substrate addition by dialysis method
AID1512063Inhibition of human recombinant MAO-B expressed in insect cells microsomes assessed as inhibition of 4-hydroxyquinoline formation using kynuramine as substrate incubated for 20 mins by fluorescence spectrophotometry analysis2019Bioorganic & medicinal chemistry letters, 11-01, Volume: 29, Issue:21
1,3,4-Oxadiazol-2-ylbenzenesulfonamides as privileged structures for the inhibition of monoamine oxidase B.
AID126695In vitro inhibitory activity against rat brain Monoamine oxidase B1995Journal of medicinal chemistry, Nov-24, Volume: 38, Issue:24
Selective and potent monoamine oxidase type B inhibitors: 2-substituted 5-aryltetrazole derivatives.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1192629Reversible inhibition of MAO-B in rat whole brain homogenate assessed as recovered activity at 100 times IC50 incubated for 60 mins followed by 3 washes by Amplex Red 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.
AID1708804Cytotoxicity against human HepG2 cells assessed as cell viability at 7.5 uM incubated for 2 hrs by MTT assay relative to control2021Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4
New 2-Pyrazoline and Hydrazone Derivatives as Potent and Selective Monoamine Oxidase A Inhibitors.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID1345977Human Monoamine oxidase B (Catecholamine turnover)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.
AID1345977Human Monoamine oxidase B (Catecholamine turnover)1990Advances in neurology, , Volume: 53Ro 19-6327, a reversible and highly selective monoamine, oxidase B inhibitor: a novel tool to explore the MAO-B function in humans.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (108)

TimeframeStudies, This Drug (%)All Drugs %
pre-19903 (2.78)18.7374
1990's56 (51.85)18.2507
2000's19 (17.59)29.6817
2010's28 (25.93)24.3611
2020's2 (1.85)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 (%)
Trials11 (9.65%)5.53%
Reviews8 (7.02%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other95 (83.33%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research Highlights

Long-term Use (3)

ArticleYear
Monoamine oxidase B inhibitors for early Parkinson's disease.
The Cochrane database of systematic reviews, Jul-20, Issue: 3
2005
Lazabemide (Ro 19-6327), a reversible and highly sensitive MAO-B inhibitor: preclinical and clinical findings.
Journal of neural transmission. Supplementum, Volume: 41
1994
The effects of lifelong treatment with MAO inhibitors on amino acid levels in rat brain.
Journal of neural transmission. Parkinson's disease and dementia section, Volume: 2, Issue: 4
1990
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Pharmacokinetics (1)

ArticleYear
Pharmacokinetics and pharmacodynamics of single and multiple doses of the MAO-B inhibitor lazabemide in healthy subjects.
British journal of clinical pharmacology, Volume: 43, Issue: 1
1997
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioavailability (1)

ArticleYear
Pharmacological characterization of MRZ-8676, a novel negative allosteric modulator of subtype 5 metabotropic glutamate receptors (mGluR5): focus on L: -DOPA-induced dyskinesia.
Journal of neural transmission (Vienna, Austria : 1996), Volume: 118, Issue: 12
2011
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Dosage (5)

ArticleYear
Long-term effects of alpha-amino-3-hydroxy-5-methyl-4-isoxazole propionate and 6-nitro-7-sulphamoylbenzo(f)quinoxaline-2,3-dione in the rat basal ganglia: calcification, changes in glutamate receptors and glial reactions.
Neuroscience, Volume: 94, Issue: 1
1999
Pharmacokinetics and pharmacodynamics of single and multiple doses of the MAO-B inhibitor lazabemide in healthy subjects.
British journal of clinical pharmacology, Volume: 43, Issue: 1
1997
Effect of lazabemide on the progression of disability in early Parkinson's disease. The Parkinson Study Group.
Annals of neurology, Volume: 40, Issue: 1
1996
Mixed linear and non-linear disposition of lazabemide, a reversible and selective inhibitor of monoamine oxidase B.
British journal of clinical pharmacology, Volume: 37, Issue: 6
1994
Measurement of cerebral monoamine oxidase B activity using L-[11C]deprenyl and dynamic positron emission tomography.
Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism, Volume: 11, Issue: 4
1991
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]