Page last updated: 2024-12-06

lifarizine

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

Description

lifarizine: sodium-calcium channel modulator; reduces ischemic brain damage [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID71336
CHEMBL ID122079
CHEBI ID177661
SCHEMBL ID94691
MeSH IDM0186042

Synonyms (26)

Synonym
CHEBI:177661
1-benzhydryl-4-[[5-methyl-2-(4-methylphenyl)-1h-imidazol-4-yl]methyl]piperazine
lifarizine
119514-66-8
lifarizine (usan/inn)
D04735
CHEMBL122079
rs-87476-000
rs 87476-000
lifarizine [usan:inn:ban]
unii-c3705i245k
1-(diphenylmethyl)-4-((5-methyl-2-p-tolylimidazol-4-yl)methyl)piperazine
piperazine, 1-(diphenylmethyl)-4-((5-methyl-2-(4-methylphenyl)-1h-imidazol-4-yl)methyl)-
c3705i245k ,
lifarizine [inn]
lifarizine [usan]
SCHEMBL94691
HTDFEXRUDGWNHA-UHFFFAOYSA-N
1-diphenylmethyl-4-[(2-(4-methylphenyl)-5-methyl-1h-imidazol-4-yl)methyl]piperazine
1-diphenylmethyl-4-[(2-(-4-methylphenyl)-5-methyl-1 h-imidazol-4-yl)methyl]piperazine
bdbm50473869
1-[di(phenyl)methyl]-4-[[5-methyl-2-(4-methylphenyl)-1h-imidazol-4-yl]methyl]piperazine
Q27275132
1-(diphenylmethyl)-4-{[5-methyl-2-(4-methylphenyl)-1h-imidazol-4-yl]methyl}piperazine
DTXSID80869632
AKOS040748748

Research Excerpts

Dosage Studied

ExcerptRelevanceReference
" Rats were dosed parenterally solely post-ischaemia (reperfusion) in a series of five studies covering a range of intra-arterial/intraperitoneal (i."( Reduction by lifarizine of the neuronal damage induced by cerebral ischaemia in rodents.
Alps, BJ; Armstrong, JM; Calder, C; McBean, DE; Wilson, AD, 1995
)
0.66
" The dosing regimen of lifarizine gave reduced damage in the hippocampal CA1 sub-field (4."( Neuroprotective efficacy of lifarizine (RS-87476) in a simplified rat survival model of 2 vessel occlusion.
Alps, BJ; Armstrong, JM; McBean, DE; Oswald, CB; Wilson, AD; Winters, V, 1995
)
0.9
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
diarylmethaneAny compound containing two aryl groups connected by a single C 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 (3)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Sodium channel protein type 1 subunit alphaRattus norvegicus (Norway rat)IC50 (µMol)0.49400.01001.14052.9390AID179553
Sodium channel protein type 2 subunit alphaRattus norvegicus (Norway rat)IC50 (µMol)0.49400.00401.14854.7300AID179553
Sodium channel protein type 3 subunit alphaRattus norvegicus (Norway rat)IC50 (µMol)0.49400.00600.86052.9390AID179553
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (4)

Assay IDTitleYearJournalArticle
AID179553Inhibitory effect against veratridine-induced glutamate release from rat brain slices2002Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17
Synthesis and structure-activity relationships of 6,7-benzomorphan derivatives as use-dependent sodium channel blockers for the treatment of stroke.
AID226365Displacement of [3H]-MK-801 from rat cerebral cortex glutamate NMDA receptor; ND is No Data.2002Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17
Synthesis and structure-activity relationships of 6,7-benzomorphan derivatives as use-dependent sodium channel blockers for the treatment of stroke.
AID184913Percent inhibition of veratridine-induced glutamate release in rat brain slices at 10000 nmol/L; ND is No Data.2002Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17
Synthesis and structure-activity relationships of 6,7-benzomorphan derivatives as use-dependent sodium channel blockers for the treatment of stroke.
AID226359Displacement of [3H]BTX from sodium channel of rat cerebral cortex synaptosomes2002Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17
Synthesis and structure-activity relationships of 6,7-benzomorphan derivatives as use-dependent sodium channel blockers for the treatment of stroke.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (18)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's16 (88.89)18.2507
2000's2 (11.11)29.6817
2010's0 (0.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (5.26%)5.53%
Reviews1 (5.26%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other17 (89.47%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]