Page last updated: 2024-12-05

isocarboxazid

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

Isocarboxazid is a non-selective, irreversible monoamine oxidase inhibitor (MAOI) used to treat depression. It is believed to work by inhibiting the breakdown of neurotransmitters such as serotonin, norepinephrine, and dopamine in the brain. Isocarboxazid has a complex synthesis involving multiple steps, and its effects can be significant, including potential interactions with certain foods and medications. It is studied to understand its therapeutic potential in treating depression and its impact on neurochemical pathways in the brain. Isocarboxazid's use has declined in recent years due to the availability of other, potentially safer antidepressants, but it remains a viable option for some individuals.'

Isocarboxazid: An MAO inhibitor that is effective in the treatment of major depression, dysthymic disorder, and atypical depression. It also is useful in the treatment of panic disorder and the phobic disorders. (From AMA, Drug Evaluations Annual, 1994, p311) [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID3759
CHEMBL ID1201168
CHEBI ID93635
SCHEMBL ID49562
MeSH IDM0011750

Synonyms (114)

Synonym
smr001233334
MLS002154005
BRD-K93332168-001-03-2
3-isoxazolecarboxylic acid, 2-(phenylmethyl)hydrazide
nsc169893
isocarboxazid
maraplan
bmih
mls003106729 ,
enerzer
isocarbonazid
n'-benzyl n-methyl-5-isoxazolecarboxylhydrazide-3
benazide
3-isoxazolecarboxylic acid, 2-benzylhydrazide
1-benzyl-2-(5-methyl-3-isoxazolylcarbonyl)hydrazine
ro 5-0831/1
isocarboxazide
ro 5-0831
marplan
wln: t5noj c1 evmm1r
isocarbossazide
5-methyl-3-isoxazolecarboxylic acid 2-benzylhydrazide
nsc-169893
isocarboxyzid
59-63-2
marplon
3-isoxazolecarboxylic acid, 5-methyl-, 2-(phenylmethyl)hydrazide
5-methyl-n'-(phenylmethyl)isoxazole-3-carbohydrazide
isocarbossazide [dcit]
ccris 9178
3-isoxazolecarboxylic acid, 5-methyl-, 2-benzylhydrazide
isocarboxazida [inn-spanish]
isocarboxazidum [inn-latin]
nsc 169893
1-benzyl-2-(5-methyl-3-isoxazolyl-carbonyl)hydrazine
isocarboxazide [inn-french]
einecs 200-438-4
brn 0201295
marplan (tn)
isocarboxazid (inn)
D02580
PRESTWICK2_000795
BSPBIO_000930
PRESTWICK3_000795
NCGC00016267-01
cas-59-63-2
AB00513923
DB01247
BPBIO1_001024
PRESTWICK1_000795
SPBIO_002869
PRESTWICK0_000795
NCGC00016267-02
CHEMBL1201168
ro-5-0831
HMS1570O12
n'-benzyl-5-methyl-1,2-oxazole-3-carbohydrazide
HMS2097O12
34237v843t ,
4-27-00-03999 (beilstein handbook reference)
isocarboxazid [usp:inn:ban]
unii-34237v843t
isocarboxazida
isocarboxazidum
tox21_110336
dtxsid4023171 ,
dtxcid003171
n'-benzyl-5-methylisoxazole-3-carbohydrazide
HMS2230E11
AKOS016003091
NCGC00016267-03
FT-0670438
isocarboxazid [orange book]
isocarboxazid [who-dd]
isocarboxazid [mi]
isocarboxazid [usp-rs]
isocarboxazid [mart.]
isocarboxazid [inn]
gtpl7204
HMS3369G18
CCG-220795
SCHEMBL49562
XKFPYPQQHFEXRZ-UHFFFAOYSA-N
n'-benzyl-5-methyl-3-isoxazolecarbohydrazide #
AC-24841
isocarboxazid (icd)
bdbm163692
SR-01000841192-2
SR-01000841192-3
sr-01000841192
5-methyl-n'-(phenylmethyl)-3-isoxazolecarbohydrazide
CHEBI:93635
isocarboxazid 5-methyl-3-isoxazole-carboxylic acid 2-benzylhydrazide, aldrichcpr
HMS3714O12
Q409595
HMS3887K05
59-63-2 (free base)
HY-13929
CS-0008613
NCGC00016267-06
A914188
MS-23317
isocarboxazid (200 mg)
isocarboxazid(200mg)
EN300-12578055
isocarboxazide (inn-french)
isocarboxazid (mart.)
isocarboxazidum (inn-latin)
isocarboxazida (inn-spanish)
isocarboxacid
n06af01
isocarboxazid (usp-rs)
isocarboxazid (usp:inn:ban)
Z2044793215

Research Excerpts

Overview

Isocarboxazid is an underutilized and potentially valuable agent for the treatment of depressed patients.

ExcerptReferenceRelevance
"Isocarboxazid appears to be an underutilized and potentially valuable agent for the treatment of depressed patients."( Side effects of isocarboxazid.
Zisook, S, 1984
)
1.33

Effects

ExcerptReferenceRelevance
"Isocarboxazide has been used as long-term treatment for a selected group of 20 depressive patients, of whom some 90% (17/19) were non-responders to treatment with tricyclic antidepressants. "( Long-term treatment of depression with isocarboxazide.
Larsen, JK; Rafaelsen, OJ, 1980
)
1.97

Treatment

ExcerptReferenceRelevance
"into isocarboxazide (Iso) pretreated mice, spontaneous motor activity (SMA) measured by photo-cell counters method increased markedly but SMA by wheel cage method decreased."( [Effects of beta-phenylethylamine derivatives on the central nervous system. (5) Changes in the volume of spontaneous movement in mice with intracerebral administration of tyramine].
Kisara, K; Sakurada, S; Shoji, T, 1975
)
0.71

Toxicity

ExcerptReferenceRelevance
"There have been numerous case reports of adverse reactions involving monoamine oxidase inhibitors (MAOIs), including reactions that developed when one MAOI was substituted for another."( Central nervous system toxicity after abrupt monoamine oxidase inhibitor switch: a case report.
Masiar, SJ; Safferman, AZ, 1992
)
0.28
"Three double-blind, placebo controlled studies found isocarboxazid (40-50 mg/day) to be efficacious and safe for the treatment of atypical depression."( Side effects of isocarboxazid.
Zisook, S, 1984
)
0.86
" An understanding of structure-activity relationships (SARs) of chemicals can make a significant contribution to the identification of potential toxic effects early in the drug development process and aid in avoiding such problems."( Developing structure-activity relationships for the prediction of hepatotoxicity.
Fisk, L; Greene, N; Naven, RT; Note, RR; Patel, ML; Pelletier, DJ, 2010
)
0.36

Bioavailability

ExcerptReferenceRelevance
" By measuring the brain function using computer period analysis of cerebral biopotentials, dose-efficacy relations were found (in the range of 25-75 mcg) which suggest the bioavailability of LHM at the CNS level."( Prediction of psychotropic properties of lisuride hydrogen maleate by quantitative pharmaco-electroencephalogram.
Akpinar, S; Herrmann, WM; Itil, TM, 1975
)
0.25
"The dissolution procedure serves as a quality control test to assure batch-to-batch uniformity and bioequivalence of a product once the bioavailability of the product has been established."( Influence of higher rates of agitation on release patterns of immediate-release drug products.
Dighe, S; Gurbarg, M; Noory, A; Shah, VP; Skelly, JP, 1992
)
0.28
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

ExcerptRelevanceReference
" Clinical adverse reactions tended to be mild and to respond to dosage decreases."( Side effects of isocarboxazid.
Zisook, S, 1984
)
0.61
" We proposed a systematic classification scheme using FDA-approved drug labeling to assess the DILI potential of drugs, which yielded a benchmark dataset with 287 drugs representing a wide range of therapeutic categories and daily dosage amounts."( FDA-approved drug labeling for the study of drug-induced liver injury.
Chen, M; Fang, H; Liu, Z; Shi, Q; Tong, W; Vijay, V, 2011
)
0.37
" Normal dosage isocarboxazide may be prescribed for all patients because isocarboxazide is not metabolized through the CYP2D6 enzyme complex like most other antidepressants."( [The use of the monoamine oxidase inhibitor isocarboxazide in treatment-resistant depression].
Brøsen, K; Krogh-Nielsen, L; Larsen, JK, 2015
)
1.03
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
benzenesAny benzenoid aromatic compound consisting of the benzene skeleton and its substituted derivatives.
[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 (11)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Beta-lactamaseEscherichia coli K-12Potency112.20200.044717.8581100.0000AID485294
USP1 protein, partialHomo sapiens (human)Potency44.66840.031637.5844354.8130AID504865
TDP1 proteinHomo sapiens (human)Potency7.30780.000811.382244.6684AID686978
estrogen nuclear receptor alphaHomo sapiens (human)Potency7.96010.000229.305416,493.5996AID743079; AID743080; AID743091
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency10.00000.035520.977089.1251AID504332
aryl hydrocarbon receptorHomo sapiens (human)Potency10.74110.000723.06741,258.9301AID743085; AID743122
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency11.35880.001723.839378.1014AID743083
chromobox protein homolog 1Homo sapiens (human)Potency89.12510.006026.168889.1251AID540317
lamin isoform A-delta10Homo sapiens (human)Potency3.16230.891312.067628.1838AID1487
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency63.09570.009610.525035.4813AID1479145
[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)
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (20)

Processvia Protein(s)Taxonomy
nucleotide-excision repairN-glycosylase/DNA lyaseHomo sapiens (human)
DNA damage responseN-glycosylase/DNA lyaseHomo sapiens (human)
negative regulation of double-strand break repair via single-strand annealingN-glycosylase/DNA lyaseHomo sapiens (human)
base-excision repairN-glycosylase/DNA lyaseHomo sapiens (human)
regulation of DNA-templated transcriptionN-glycosylase/DNA lyaseHomo sapiens (human)
response to oxidative stressN-glycosylase/DNA lyaseHomo sapiens (human)
response to radiationN-glycosylase/DNA lyaseHomo sapiens (human)
response to xenobiotic stimulusN-glycosylase/DNA lyaseHomo sapiens (human)
response to light stimulusN-glycosylase/DNA lyaseHomo sapiens (human)
response to estradiolN-glycosylase/DNA lyaseHomo sapiens (human)
cellular response to reactive oxygen speciesN-glycosylase/DNA lyaseHomo sapiens (human)
negative regulation of apoptotic processN-glycosylase/DNA lyaseHomo sapiens (human)
positive regulation of gene expression via chromosomal CpG island demethylationN-glycosylase/DNA lyaseHomo sapiens (human)
depurinationN-glycosylase/DNA lyaseHomo sapiens (human)
depyrimidinationN-glycosylase/DNA lyaseHomo sapiens (human)
response to ethanolN-glycosylase/DNA lyaseHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIN-glycosylase/DNA lyaseHomo sapiens (human)
response to folic acidN-glycosylase/DNA lyaseHomo sapiens (human)
cellular response to cadmium ionN-glycosylase/DNA lyaseHomo sapiens (human)
base-excision repair, AP site formationN-glycosylase/DNA lyaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (10)

Processvia Protein(s)Taxonomy
RNA polymerase II cis-regulatory region sequence-specific DNA bindingN-glycosylase/DNA lyaseHomo sapiens (human)
damaged DNA bindingN-glycosylase/DNA lyaseHomo sapiens (human)
endonuclease activityN-glycosylase/DNA lyaseHomo sapiens (human)
protein bindingN-glycosylase/DNA lyaseHomo sapiens (human)
microtubule bindingN-glycosylase/DNA lyaseHomo sapiens (human)
oxidized purine nucleobase lesion DNA N-glycosylase activityN-glycosylase/DNA lyaseHomo sapiens (human)
enzyme bindingN-glycosylase/DNA lyaseHomo sapiens (human)
oxidized purine DNA bindingN-glycosylase/DNA lyaseHomo sapiens (human)
8-oxo-7,8-dihydroguanine DNA N-glycosylase activityN-glycosylase/DNA lyaseHomo sapiens (human)
class I DNA-(apurinic or apyrimidinic site) endonuclease activityN-glycosylase/DNA lyaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (8)

Processvia Protein(s)Taxonomy
nucleusN-glycosylase/DNA lyaseHomo sapiens (human)
nucleoplasmN-glycosylase/DNA lyaseHomo sapiens (human)
mitochondrial matrixN-glycosylase/DNA lyaseHomo sapiens (human)
cytosolN-glycosylase/DNA lyaseHomo sapiens (human)
nuclear matrixN-glycosylase/DNA lyaseHomo sapiens (human)
nuclear speckN-glycosylase/DNA lyaseHomo sapiens (human)
protein-containing complexN-glycosylase/DNA lyaseHomo sapiens (human)
nucleusN-glycosylase/DNA lyaseHomo sapiens (human)
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (60)

Assay IDTitleYearJournalArticle
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
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).
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]
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).
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
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).
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]
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]
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
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).
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
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).
AID588209Literature-mined public compounds from Greene et al multi-species hepatotoxicity modelling dataset2010Chemical research in toxicology, Jul-19, Volume: 23, Issue:7
Developing structure-activity relationships for the prediction of hepatotoxicity.
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).
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).
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).
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).
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]
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
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).
AID1079945Animal toxicity known. [column 'TOXIC' in source]
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
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID625276FDA Liver Toxicity Knowledge Base Benchmark Dataset (LTKB-BD) drugs of most concern for DILI2011Drug discovery today, Aug, Volume: 16, Issue:15-16
FDA-approved drug labeling for the study of drug-induced liver injury.
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).
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).
AID588210Human drug-induced liver injury (DILI) modelling dataset from Ekins et al2010Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 38, Issue:12
A predictive ligand-based Bayesian model for human drug-induced liver injury.
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).
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.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
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).
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]
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID567091Drug absorption in human assessed as human intestinal absorption rate2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Prediction of drug intestinal absorption by new linear and non-linear QSPR.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
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.
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.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
AID1801344Fluorescence-based Assay from Article 10.1021/acschembio.5b00452: \\Small Molecule Inhibitors of 8-Oxoguanine DNA Glycosylase-1 (OGG1).\\2015ACS chemical biology, Oct-16, Volume: 10, Issue:10
Small Molecule Inhibitors of 8-Oxoguanine DNA Glycosylase-1 (OGG1).
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (353)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990302 (85.55)18.7374
1990's24 (6.80)18.2507
2000's4 (1.13)29.6817
2010's20 (5.67)24.3611
2020's3 (0.85)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 57.41

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

MetricThis Compound (vs All)
Research Demand Index57.41 (24.57)
Research Supply Index6.01 (2.92)
Research Growth Index4.40 (4.65)
Search Engine Demand Index96.26 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (57.41)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials30 (7.94%)5.53%
Reviews21 (5.56%)6.00%
Case Studies30 (7.94%)4.05%
Observational0 (0.00%)0.25%
Other297 (78.57%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (1)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
I2PETHV - Quantification and Localisation of Imidazoline2 Binding Sites in Healthy Volunteers Using [11C]BU99008 a Positron Emission Tomography Study [NCT02323217]Early Phase 120 participants (Actual)Interventional2015-01-31Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT02323217 (3) [back to overview]Determination of the Regional Density and Distribution of I2BS in Healthy Human Brain (1TCM Model)
NCT02323217 (3) [back to overview]Determination of the Regional Density and Distribution of I2BS in Healthy Human Brain (2TCM Model)
NCT02323217 (3) [back to overview]Determination of the Regional Density and Distribution of I2BS in Healthy Human Brain (MA Model)

Determination of the Regional Density and Distribution of I2BS in Healthy Human Brain (1TCM Model)

"The determination of the regional density and distribution of the I2BS in human brain of healthy volunteers. The output parameter used to determine this will be derived from the most appropriate PET pharmacokinetic model for this ligand in human e.g. Total Volume of Distribution (VT) or Binding Potential (BP).~Regional time-activity data were generated from arterial plasma input functions corrected for metabolites using the most appropriate model to derive the outcome measure VT (regional distribution volume). All image processing and kinetic analyses were performed in MIAKAT. The Akaike model selection criteria were used to determine the most appropriate model to describe these data.~The calculated criteria for the three main models are: one-tissue (1TCM) and two-tissue (2TCM) compartmental models, and multilinear analysis model (MA)." (NCT02323217)
Timeframe: 1 week

InterventionmL/cm^3 (Mean)
Whole BrainCerebellumBrain stemOccipital lobeInsulaFrontal lobeCingulateParietal lobeAmygdalaHippocampusStriatumThalamus
Healthy Volunteers44.539.362.738.663.341.658.339.289.868.4102.775.3

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Determination of the Regional Density and Distribution of I2BS in Healthy Human Brain (2TCM Model)

"The determination of the regional density and distribution of the I2BS in human brain of healthy volunteers. The output parameter used to determine this will be derived from the most appropriate PET pharmacokinetic model for this ligand in human e.g. Total Volume of Distribution (VT) or Binding Potential (BP).~Regional time-activity data were generated from arterial plasma input functions corrected for metabolites using the most appropriate model to derive the outcome measure VT (regional distribution volume). All image processing and kinetic analyses were performed in MIAKAT. The Akaike model selection criteria were used to determine the most appropriate model to describe these data.~The calculated criteria for the three main models are: one-tissue (1TCM) and two-tissue (2TCM) compartmental models, and multilinear analysis model (MA)." (NCT02323217)
Timeframe: 1 week

InterventionmL/cm^3 (Mean)
Whole BrainCerebellumBrain stemOccipital lobeInsulaFrontal lobeCingulateParietal lobeAmygdalaHippocampusStriatumThalamus
Healthy Volunteers48.841.966.442.767.745.762.243.694.677.7105.780.0

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Determination of the Regional Density and Distribution of I2BS in Healthy Human Brain (MA Model)

"The determination of the regional density and distribution of the I2BS in human brain of healthy volunteers. The output parameter used to determine this will be derived from the most appropriate PET pharmacokinetic model for this ligand in human e.g. Total Volume of Distribution (VT) or Binding Potential (BP).~Regional time-activity data were generated from arterial plasma input functions corrected for metabolites using the most appropriate model to derive the outcome measure VT (regional distribution volume). All image processing and kinetic analyses were performed in MIAKAT. The Akaike model selection criteria were used to determine the most appropriate model to describe these data.~The calculated criteria for the three main models are: one-tissue (1TCM) and two-tissue (2TCM) compartmental models, and multilinear analysis model (MA)." (NCT02323217)
Timeframe: 1 week

InterventionmL/cm^3 (Mean)
Whole BrainCerebellumBrain stemOccipital lobeInsulaFrontal lobeCingulateParietal lobeAmygdalaHippocampusStriatumThalamus
Healthy Volunteers44.839.663.238.863.942.058.839.591.169.1104.276.0

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