Page last updated: 2024-12-07

1-methyl-4-(2'-methylphenyl)-1,2,3,6-tetrahydropyridine

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

Description

1-methyl-4-(2'-methylphenyl)-1,2,3,6-tetrahydropyridine: more potent dopaminergic neurotoxic compound than MPTP in mice [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID91767
CHEMBL ID60303
CHEMBL ID536788
SCHEMBL ID1078756
MeSH IDM0140634

Synonyms (17)

Synonym
2'-methyl-mptp
m-mptp
1-methyl-4-(2'-methylphenyl)-1,2,3,6-tetrahydropyridine
2'-ch3-mptp
pyridine, 1,2,3,6-tetrahydro-1-methyl-4-(2-methylphenyl)-
CHEMBL60303
CHEMBL536788 ,
1-methyl-4-(2-methylphenyl)-3,6-dihydro-2h-pyridine
102417-86-7
unii-hgq85cv4u5
hgq85cv4u5 ,
bdbm50374545
SCHEMBL1078756
1,2,3,6-tetrahydro-1-methyl-4-(2-methylphenyl)pyridine
NCGC00485141-01
pyridine, 1,2,3,6-tetrahydro-1-methyl-4-(2-methy
DTXSID70877241

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
"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
" After 4 days of treatment, and as the dosage was gradually increased, the animals exhibited mild motor deficits."( 1-Methyl-4-(2'-methylphenyl)-1,2,3,6-tetrahydropyridine (2'-methyl-MPTP) is less neurotoxic than MPTP in the common marmoset.
Gibb, WR; Jackson, EA; Jenner, P; Marsden, CD; Nomoto, M; Rose, S, 1990
)
1.72
" Dose-response curves for chorea and dystonia revealed that the same dose of L-dopa (30 mg/kg) induced the highest score for both dyskinesias: however, the severity was much greater for chorea."( Characterisation of dyskinesias induced by L-dopa in MPTP-treated squirrel monkeys.
Boyce, S; Iversen, SD; Rupniak, NM; Steventon, MJ, 1990
)
0.28
"Unlike 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP), which produces consistent decreases in levels of striatal dopamine (DA) with considerably smaller and more variable effects on mouse brain levels of serotonin (5-HT) and norepinephrine (NE), a novel amine-substituted MPTP analogue, 1-methyl-4-(2'-aminophenyl)-1,2,3,6-tetrahydropyridine (2'-NH2-MPTP), administered in a standard mouse dosing paradigm for MPTP (20 mg/kg x 4) did not affect striatal DA but led to marked reductions (60-70%) in levels of 5-HT, 5-hydroxyindoleacetic acid (5-HIAA), and NE measured in frontal cortex and hippocampus 1 week after treatment."( Sustained depletion of cortical and hippocampal serotonin and norepinephrine but not striatal dopamine by 1-methyl-4-(2'-aminophenyl)-1,2,3,6-tetrahydropyridine (2'-NH2-MPTP): a comparative study with 2'-CH3-MPTP and MPTP.
Andrews, AM; Murphy, DL, 1993
)
0.29
" This dosing regimen causes substantial striatal dopamine depletion in mice."( 2'-NH(2)-MPTP [1-methyl-4-(2'-aminophenyl)-1,2,3,6-tetrahydropyridine] depletes serotonin and norepinephrine in rats: a comparison with 2'-CH(3)-MPTP [1-methyl-4-(2'-methylphenyl)-1,2,3,6-tetrahydropyridine].
Andrews, AM; Mazzola-Pomietto, P; Murphy, DL; Unger, EL, 2002
)
0.51
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (10)

Assay IDTitleYearJournalArticle
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.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID235548Selectivity Coefficient measured as ratio of Vmax/Km value of MAO-A to that of MAO-B1997Journal of medicinal chemistry, Jun-20, Volume: 40, Issue:13
Probing the active sites of monoamine oxidase A and B with 1,4-disubstituted tetrahydropyridine substrates and inactivators.
AID235549Selectivity Coefficient measured as ratio of Vmax/Km value of MAO-B to that of MAO-A1997Journal of medicinal chemistry, Jun-20, Volume: 40, Issue:13
Probing the active sites of monoamine oxidase A and B with 1,4-disubstituted tetrahydropyridine substrates and inactivators.
AID125694Tested for Kinetic data against the monoamine oxidase A catalyzed oxidation.1997Journal of medicinal chemistry, Jun-20, Volume: 40, Issue:13
Probing the active sites of monoamine oxidase A and B with 1,4-disubstituted tetrahydropyridine substrates and inactivators.
AID127348Binding affinity towards monoaminooxidase Relative to MPTP1993Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20
QSAR's from similarity matrices. Technique validation and application in the comparison of different similarity evaluation methods.
AID126526Tested for Kinetic data against the monoamine oxidase B catalyzed oxidation.1997Journal of medicinal chemistry, Jun-20, Volume: 40, Issue:13
Probing the active sites of monoamine oxidase A and B with 1,4-disubstituted tetrahydropyridine substrates and inactivators.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (73)

TimeframeStudies, This Drug (%)All Drugs %
pre-19907 (9.59)18.7374
1990's58 (79.45)18.2507
2000's4 (5.48)29.6817
2010's2 (2.74)24.3611
2020's2 (2.74)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 10.88

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 weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index10.88 (24.57)
Research Supply Index4.36 (2.92)
Research Growth Index5.24 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (10.88)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews3 (3.90%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other74 (96.10%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]