Page last updated: 2024-11-12

l-826,141

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

Description

L-826,141: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9916436
CHEMBL ID323312
SCHEMBL ID185764
MeSH IDM0430794

Synonyms (19)

Synonym
l-826,141
2-{4-[1-(3,4-bis-difluoromethoxy-phenyl)-2-(3-methyl-1-oxy-pyridin-4-yl)-ethyl]-phenyl}-1,1,1,3,3,3-hexafluoro-propan-2-ol
bdbm50119355
4-{2-(3,4-bis-difluoromethoxy-phenyl)-2-[4-(2,2,2-trifluoro-1-hydroxy-1-trifluoromethyl-ethyl)-phenyl]-ethyl}-3-methyl-pyridin-1-ol anion
l-826141
CHEMBL323312 ,
SCHEMBL185764
benzenemethanol, 4-(1-(3,4-bis(difluoromethoxy)phenyl)-2-(3-methyl-1-oxido-4-pyridinyl)ethyl)-.alpha.,.alpha.-bis(trifluoromethyl)-
2JN104XMOK ,
491869-01-3
l 826141
unii-2jn104xmok
benzenemethanol, 4-(1-(3,4-bis(difluoromethoxy)phenyl)-2-(3-methyl-1-oxido-4-pyridinyl)ethyl)-alpha,alpha-bis(trifluoromethyl)-
4-(2-(3,4-bis(difluoromethoxy)phenyl)-2-(4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl)ethyl)-3-methylpyridine 1-oxide
Q27254832
2-[4-[1-[3,4-bis(difluoromethoxy)phenyl]-2-(3-methyl-1-oxidopyridin-1-ium-4-yl)ethyl]phenyl]-1,1,1,3,3,3-hexafluoropropan-2-ol
qjlfndiedqorep-uhfffaoysa-n
benzenemethanol, 4-[1-[3,4-bis(difluoromethoxy)phenyl]-2-(3-methyl-1-oxido-4-pyridinyl)ethyl]-alpha,alpha-bis(trifluoromethyl)-
PD162121

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
"A detailed SAR study directed toward the optimization of pharmacokinetic parameters for analogues of L-791,943 is reported."( Substituted 4-(2,2-diphenylethyl)pyridine-N-oxides as phosphodiesterase-4 inhibitors: SAR study directed toward the improvement of pharmacokinetic parameters.
Blouin, M; Brideau, C; Chauret, N; Ducharme, Y; Frenette, R; Friesen, RW; Girard, Y; Hamel, P; Jones, TR; Laliberté, F; Li, C; Masson, P; McAuliffe, M, 2002
)
0.31

Bioavailability

ExcerptReferenceRelevance
" The introduction of a soft metabolic site on this structure permitted the identification of L-826,141 as a potent phosphodiesterase type 4 (PDE4) inhibitor that is well absorbed and that presents a shorter half-life than L-791,943 in a variety of animal species."( Substituted 4-(2,2-diphenylethyl)pyridine-N-oxides as phosphodiesterase-4 inhibitors: SAR study directed toward the improvement of pharmacokinetic parameters.
Blouin, M; Brideau, C; Chauret, N; Ducharme, Y; Frenette, R; Friesen, RW; Girard, Y; Hamel, P; Jones, TR; Laliberté, F; Li, C; Masson, P; McAuliffe, M, 2002
)
0.53
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (2)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)IC50 (µMol)0.00550.00001.068010.0000AID157776; AID157778; AID363104
cAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)IC50 (µMol)0.00240.00001.146310.0000AID1619495
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (24)

Processvia Protein(s)Taxonomy
cAMP catabolic processcAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
signal transductioncAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
G protein-coupled receptor signaling pathwaycAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
sensory perception of smellcAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
regulation of protein kinase A signalingcAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
cellular response to xenobiotic stimuluscAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
regulation of adenylate cyclase-activating G protein-coupled receptor signaling pathwaycAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
cAMP-mediated signalingcAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
regulation of heart ratecAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
cAMP catabolic processcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
positive regulation of heart ratecAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
regulation of release of sequestered calcium ion into cytosol by sarcoplasmic reticulumcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
positive regulation of type II interferon productioncAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
positive regulation of interleukin-2 productioncAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
positive regulation of interleukin-5 productioncAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
negative regulation of peptidyl-serine phosphorylationcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
negative regulation of heart contractioncAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
T cell receptor signaling pathwaycAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
establishment of endothelial barriercAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
adrenergic receptor signaling pathwaycAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
regulation of cardiac muscle cell contractioncAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
negative regulation of adenylate cyclase-activating G protein-coupled receptor signaling pathwaycAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
regulation of cell communication by electrical coupling involved in cardiac conductioncAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
negative regulation of relaxation of cardiac musclecAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
regulation of calcium ion transmembrane transport via high voltage-gated calcium channelcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
cAMP-mediated signalingcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (14)

Processvia Protein(s)Taxonomy
3',5'-cyclic-AMP phosphodiesterase activitycAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
protein bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
cAMP bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
metal ion bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activitycAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
3',5'-cyclic-nucleotide phosphodiesterase activitycAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activitycAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
calcium channel regulator activitycAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
protein bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
enzyme bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
signaling receptor regulator activitycAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
cAMP bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
beta-2 adrenergic receptor bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
transmembrane transporter bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
metal ion bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
ATPase bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
scaffold protein bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
heterocyclic compound bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activitycAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (11)

Processvia Protein(s)Taxonomy
nucleoplasmcAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
cytosolcAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
plasma membranecAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
membranecAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
ruffle membranecAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
perinuclear region of cytoplasmcAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
perinuclear region of cytoplasmcAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
cytosolcAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
nucleuscAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)
centrosomecAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
cytosolcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
plasma membranecAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
apical plasma membranecAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
voltage-gated calcium channel complexcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
calcium channel complexcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
cytosolcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
nucleuscAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
perinuclear region of cytoplasmcAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (29)

Assay IDTitleYearJournalArticle
AID205167Inhibition of ascaris-induced bronchoconstriction in Anaesthetized squirrel monkey after treatment with 0.5 mg/kg peroral dose2002Bioorganic & medicinal chemistry letters, Oct-21, Volume: 12, Issue:20
Substituted 4-(2,2-diphenylethyl)pyridine-N-oxides as phosphodiesterase-4 inhibitors: SAR study directed toward the improvement of pharmacokinetic parameters.
AID205166Inhibition of ascaris-induced bronchoconstriction in Anaesthetized squirrel monkey after treatment with 3 mg/kg peroral dose2002Bioorganic & medicinal chemistry letters, Oct-21, Volume: 12, Issue:20
Substituted 4-(2,2-diphenylethyl)pyridine-N-oxides as phosphodiesterase-4 inhibitors: SAR study directed toward the improvement of pharmacokinetic parameters.
AID205169Inhibition of ascaris-induced bronchoconstriction in Anaesthetized squirrel monkey after treatment with 3 mg/kg peroral dose2002Bioorganic & medicinal chemistry letters, Oct-21, Volume: 12, Issue:20
Substituted 4-(2,2-diphenylethyl)pyridine-N-oxides as phosphodiesterase-4 inhibitors: SAR study directed toward the improvement of pharmacokinetic parameters.
AID363114Half life in squirrel monkey2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Recent advances on phosphodiesterase 4 inhibitors for the treatment of asthma and chronic obstructive pulmonary disease.
AID363116Oral bioavailability in rat at 3 mg/kg after 6 hrs2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Recent advances on phosphodiesterase 4 inhibitors for the treatment of asthma and chronic obstructive pulmonary disease.
AID363117Plasma concentration in rat at 3 mg/kg, po after 6 hrs2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Recent advances on phosphodiesterase 4 inhibitors for the treatment of asthma and chronic obstructive pulmonary disease.
AID92877Inhibition of LPS-induced TNF-alpha formation in human whole blood.2002Bioorganic & medicinal chemistry letters, Oct-21, Volume: 12, Issue:20
Substituted 4-(2,2-diphenylethyl)pyridine-N-oxides as phosphodiesterase-4 inhibitors: SAR study directed toward the improvement of pharmacokinetic parameters.
AID157778Inhibition of human Phosphodiesterase 4A isoform using construct representing the common region of spliced variants expressed as GST-fusion proteins in Sf9 cells.2002Bioorganic & medicinal chemistry letters, Oct-21, Volume: 12, Issue:20
Substituted 4-(2,2-diphenylethyl)pyridine-N-oxides as phosphodiesterase-4 inhibitors: SAR study directed toward the improvement of pharmacokinetic parameters.
AID77553Inhibition of the ovalbumin-induced bronchoconstriction in conscious guinea pigs after 0.5 hr pretreatment with 1 mg/kg administered intraperitoneally2002Bioorganic & medicinal chemistry letters, Oct-21, Volume: 12, Issue:20
Substituted 4-(2,2-diphenylethyl)pyridine-N-oxides as phosphodiesterase-4 inhibitors: SAR study directed toward the improvement of pharmacokinetic parameters.
AID363108Inhibition of ascaris-induced bronchoconstriction in sheep at 2 mg/kg, iv2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Recent advances on phosphodiesterase 4 inhibitors for the treatment of asthma and chronic obstructive pulmonary disease.
AID204424Inhibition of ascaris-induced bronchoconstriction in sheep after early treatment with 0.5 mg/kg peroral dose2002Bioorganic & medicinal chemistry letters, Oct-21, Volume: 12, Issue:20
Substituted 4-(2,2-diphenylethyl)pyridine-N-oxides as phosphodiesterase-4 inhibitors: SAR study directed toward the improvement of pharmacokinetic parameters.
AID71919Emetic effect in ferrets to maximum 30 mg/kg oral dose2002Bioorganic & medicinal chemistry letters, Oct-21, Volume: 12, Issue:20
Substituted 4-(2,2-diphenylethyl)pyridine-N-oxides as phosphodiesterase-4 inhibitors: SAR study directed toward the improvement of pharmacokinetic parameters.
AID157776Inhibitory activity against human PDE4A expressed isoform using construct representing the common region of spliced variants as GST-fusion protein in Sf9 cells.2003Bioorganic & medicinal chemistry letters, Feb-24, Volume: 13, Issue:4
Substituted aminopyridines as potent and selective phosphodiesterase-4 inhibitors.
AID205168Inhibition of ascaris-induced bronchoconstriction in Anaesthetized squirrel monkey after treatment with 1 mg/kg peroral dose2002Bioorganic & medicinal chemistry letters, Oct-21, Volume: 12, Issue:20
Substituted 4-(2,2-diphenylethyl)pyridine-N-oxides as phosphodiesterase-4 inhibitors: SAR study directed toward the improvement of pharmacokinetic parameters.
AID363113Half life in rat2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Recent advances on phosphodiesterase 4 inhibitors for the treatment of asthma and chronic obstructive pulmonary disease.
AID363115Half life in dog2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Recent advances on phosphodiesterase 4 inhibitors for the treatment of asthma and chronic obstructive pulmonary disease.
AID7764Half-life in Squirrel monkey2002Bioorganic & medicinal chemistry letters, Oct-21, Volume: 12, Issue:20
Substituted 4-(2,2-diphenylethyl)pyridine-N-oxides as phosphodiesterase-4 inhibitors: SAR study directed toward the improvement of pharmacokinetic parameters.
AID363106Inhibition of ovalbumin-induced bronchoconstriction in guinea pig at 1 mg/kg, ip2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Recent advances on phosphodiesterase 4 inhibitors for the treatment of asthma and chronic obstructive pulmonary disease.
AID12697Half-life in rat2002Bioorganic & medicinal chemistry letters, Oct-21, Volume: 12, Issue:20
Substituted 4-(2,2-diphenylethyl)pyridine-N-oxides as phosphodiesterase-4 inhibitors: SAR study directed toward the improvement of pharmacokinetic parameters.
AID13008Bioavailability upon oral administration of compound2002Bioorganic & medicinal chemistry letters, Oct-21, Volume: 12, Issue:20
Substituted 4-(2,2-diphenylethyl)pyridine-N-oxides as phosphodiesterase-4 inhibitors: SAR study directed toward the improvement of pharmacokinetic parameters.
AID205164Inhibition of ascaris-induced bronchoconstriction in Anaesthetized squirrel monkey after treatment with 0.5 mg/kg peroral dose2002Bioorganic & medicinal chemistry letters, Oct-21, Volume: 12, Issue:20
Substituted 4-(2,2-diphenylethyl)pyridine-N-oxides as phosphodiesterase-4 inhibitors: SAR study directed toward the improvement of pharmacokinetic parameters.
AID92859Inhibition of LPS-induced TNF-alpha production in human whole blood.2003Bioorganic & medicinal chemistry letters, Feb-24, Volume: 13, Issue:4
Substituted aminopyridines as potent and selective phosphodiesterase-4 inhibitors.
AID363112Inhibition of ascaris-induced bronchoconstriction in squirrel monkey at 0.5 mg/kg, po2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Recent advances on phosphodiesterase 4 inhibitors for the treatment of asthma and chronic obstructive pulmonary disease.
AID205165Inhibition of ascaris-induced bronchoconstriction in Anaesthetized squirrel monkey after treatment with 1 mg/kg peroral dose2002Bioorganic & medicinal chemistry letters, Oct-21, Volume: 12, Issue:20
Substituted 4-(2,2-diphenylethyl)pyridine-N-oxides as phosphodiesterase-4 inhibitors: SAR study directed toward the improvement of pharmacokinetic parameters.
AID363104Inhibition of GST-tagged PDE4A2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Recent advances on phosphodiesterase 4 inhibitors for the treatment of asthma and chronic obstructive pulmonary disease.
AID10296Half-life in Dog2002Bioorganic & medicinal chemistry letters, Oct-21, Volume: 12, Issue:20
Substituted 4-(2,2-diphenylethyl)pyridine-N-oxides as phosphodiesterase-4 inhibitors: SAR study directed toward the improvement of pharmacokinetic parameters.
AID363105Inhibition of TNFalpha release in human whole blood2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Recent advances on phosphodiesterase 4 inhibitors for the treatment of asthma and chronic obstructive pulmonary disease.
AID204425Inhibition of ascaris-induced bronchoconstriction in sheep after late treatment with 0.5 mg/kg peroral dose2002Bioorganic & medicinal chemistry letters, Oct-21, Volume: 12, Issue:20
Substituted 4-(2,2-diphenylethyl)pyridine-N-oxides as phosphodiesterase-4 inhibitors: SAR study directed toward the improvement of pharmacokinetic parameters.
AID71920Cmax in ferrets after 30mg/kg oral dose2002Bioorganic & medicinal chemistry letters, Oct-21, Volume: 12, Issue:20
Substituted 4-(2,2-diphenylethyl)pyridine-N-oxides as phosphodiesterase-4 inhibitors: SAR study directed toward the improvement of pharmacokinetic parameters.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (6)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's6 (100.00)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]

Market Indicators

Research Demand Index: 12.16

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 Index12.16 (24.57)
Research Supply Index2.20 (2.92)
Research Growth Index4.36 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.16)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (14.29%)5.53%
Reviews1 (14.29%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other5 (71.43%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]