Compounds > cipamfylline
Page last updated: 2024-09-23

cipamfylline

Description

cipamfylline: a PDE type-4 inhibitor [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID71356
CHEMBL ID356323
CHEBI ID177777
SCHEMBL ID26990
SCHEMBL ID8327157
MeSH IDM0440278

Synonyms (30)

Synonym
bdbm50040348
8-amino-1,3-bis-cyclopropylmethyl-3,7-dihydro-purine-2,6-dione
CHEBI:177777
8-amino-1,3-bis(cyclopropylmethyl)-7h-purine-2,6-dione
132210-43-6
D03516
cipamfylline (usan/inn)
cipamfylline
CHEMBL356323 ,
brl 61063
brl-61063
8-amino-1,3-bis(cyclopropylmethyl)xanthine
cipamfyllinum
brl61063
cipamfylline [usan:inn]
unii-afp56r140l
1h-purine-2,6-dione, 8-amino-1,3-bis(cyclopropylmethyl)-3,7-dihydro-
afp56r140l ,
MLS006010682
smr004701664
SCHEMBL26990
cipamfylline [usan]
cipamfylline [inn]
1,3-dicyclopropylmethyl-8-amino xanthine
8-amino-1,3-di(cyclopropylmethyl)xanthine
KSPYMJJKQMWWNB-UHFFFAOYSA-N
SCHEMBL8327157
DTXSID50157437
cipamfylline, >=98% (hplc)
Q1092675

Research Excerpts

Overview

ExcerptReference
"Cipamfylline is a new potent and selective inhibitor of PDE-4."( Gilbert, M; Griffiths, CE; Traulsen, J; Van Leent, EJ, 2002)

Drug Classes (1)

ClassDescription
oxopurine
[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 (9)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)IC50 (µMol)71.00000.00001.18439.6140AID158119
cGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)Ki7.50000.00071.07978.5000AID158122
cAMP-specific 3',5'-cyclic phosphodiesterase 4D Rattus norvegicus (Norway rat)IC50 (µMol)0.00600.00032.723210.0000AID160104
cAMP-specific 3',5'-cyclic phosphodiesterase 4CRattus norvegicus (Norway rat)IC50 (µMol)0.00600.00032.723210.0000AID160104
cAMP-specific 3',5'-cyclic phosphodiesterase 4BRattus norvegicus (Norway rat)IC50 (µMol)0.00600.00032.663810.0000AID160104
cAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)IC50 (µMol)1.75000.00001.068010.0000AID159502; AID695680
cAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)Ki21.00000.00041.43528.7600AID159505
cAMP-specific 3',5'-cyclic phosphodiesterase 4ARattus norvegicus (Norway rat)IC50 (µMol)0.00600.00032.723210.0000AID160104
cAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)IC50 (µMol)1.90000.00001.104010.0000AID159502
cAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)Ki21.00000.00041.16418.7600AID159505
cAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)IC50 (µMol)1.90000.00001.465110.0000AID159502
cAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)Ki21.00000.00040.12471.0000AID159505
cAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)IC50 (µMol)1.90000.00001.146310.0000AID159502
cAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)Ki21.00000.00041.52938.7600AID159505
[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)
cAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)EC50 (µMol)0.91000.01701.21593.4000AID695683
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (39)

Processvia Protein(s)Taxonomy
positive regulation of cardiac muscle hypertrophycGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
regulation of nitric oxide mediated signal transductioncGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
T cell proliferationcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
negative regulation of T cell proliferationcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cGMP catabolic processcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
oocyte developmentcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
negative regulation of cardiac muscle contractioncGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
relaxation of cardiac musclecGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
positive regulation of oocyte developmentcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cAMP-mediated signalingcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
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)
neutrophil homeostasiscAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
cAMP catabolic processcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
neutrophil chemotaxiscAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
positive regulation of type II interferon productioncAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
positive regulation of interleukin-2 productioncAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
T cell receptor signaling pathwaycAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
leukocyte migrationcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
cellular response to lipopolysaccharidecAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
cellular response to xenobiotic stimuluscAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
cellular response to epinephrine stimuluscAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
negative regulation of adenylate cyclase-activating adrenergic receptor signaling pathwaycAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
regulation of cardiac muscle cell contractioncAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
negative regulation of relaxation of cardiac musclecAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
regulation of calcium ion transmembrane transport via high voltage-gated calcium channelcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
cAMP-mediated signalingcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
cAMP catabolic processcAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)
cAMP-mediated signalingcAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo 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 (16)

Processvia Protein(s)Taxonomy
3',5'-cyclic-nucleotide phosphodiesterase activitycGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
protein bindingcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cGMP bindingcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
metal ion bindingcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activitycGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activitycGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
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-AMP phosphodiesterase activitycAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
calcium channel regulator activitycAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
protein bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
cAMP bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
gamma-tubulin bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
transmembrane transporter bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
metal ion bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activitycAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activitycAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)
metal ion bindingcAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activitycAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo 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 (20)

Processvia Protein(s)Taxonomy
cellular_componentcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
cytosolcGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)
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 4BHomo sapiens (human)
cytosolcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
synaptic vesiclecAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
postsynaptic densitycAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
Z disccAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
dendritic spinecAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
excitatory synapsecAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
gamma-tubulin complexcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
voltage-gated calcium channel complexcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
nucleuscAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
perinuclear region of cytoplasmcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
cytosolcAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)
extracellular spacecAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)
cytosolcAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)
ciliumcAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)
cytosolcAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)
nucleuscAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)
perinuclear region of cytoplasmcAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo 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 (13)

Assay IDTitleYearJournalArticle
AID159041Inhibition of Phosphodiesterase (PDE Ic) at 100 uM.1994Journal of medicinal chemistry, Feb-18, Volume: 37, Issue:4
Inhibition of cyclic nucleotide phosphodiesterase by derivatives of 1,3-bis(cyclopropylmethyl)xanthine.
AID31539Inhibition of adenosine binding to A1 receptor of rat brain homogenates1994Journal of medicinal chemistry, Feb-18, Volume: 37, Issue:4
Inhibition of cyclic nucleotide phosphodiesterase by derivatives of 1,3-bis(cyclopropylmethyl)xanthine.
AID695683Induction of SQSTM1-dependent intracellular redistribution of GFP-tagged PDE4A4 assessed as maximal accretion of enzyme into foci2011Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
Elucidation of a structural basis for the inhibitor-driven, p62 (SQSTM1)-dependent intracellular redistribution of cAMP phosphodiesterase-4A4 (PDE4A4).
AID158119Concentration required to inhibit 50% activity of phosphodiesterase VA isoenzyme at 100 uM1994Journal of medicinal chemistry, Feb-18, Volume: 37, Issue:4
Inhibition of cyclic nucleotide phosphodiesterase by derivatives of 1,3-bis(cyclopropylmethyl)xanthine.
AID159505Inhibition of cAMP hydrolysis by PDE41994Journal of medicinal chemistry, Feb-18, Volume: 37, Issue:4
Inhibition of cyclic nucleotide phosphodiesterase by derivatives of 1,3-bis(cyclopropylmethyl)xanthine.
AID159048Concentration required to inhibit 50% activity of phosphodiesterase II isoenzyme at 100 uM1994Journal of medicinal chemistry, Feb-18, Volume: 37, Issue:4
Inhibition of cyclic nucleotide phosphodiesterase by derivatives of 1,3-bis(cyclopropylmethyl)xanthine.
AID159039Concentration required to inhibit 50% activity of phosphodiesterase IB isoenzyme at 100 uM.1994Journal of medicinal chemistry, Feb-18, Volume: 37, Issue:4
Inhibition of cyclic nucleotide phosphodiesterase by derivatives of 1,3-bis(cyclopropylmethyl)xanthine.
AID1181904Toxicity in ferret assessed as emesis at 0.01 mg/kg, iv measured up to 2 hrs post dose2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Discovery and early clinical development of 2-{6-[2-(3,5-dichloro-4-pyridyl)acetyl]-2,3-dimethoxyphenoxy}-N-propylacetamide (LEO 29102), a soft-drug inhibitor of phosphodiesterase 4 for topical treatment of atopic dermatitis.
AID160104Inhibitory concentration on phosphodiesterase IV (PDE IV) for ability to displace [3H]rolipram from its high affinity binding site.1994Journal of medicinal chemistry, Feb-18, Volume: 37, Issue:4
Inhibition of cyclic nucleotide phosphodiesterase by derivatives of 1,3-bis(cyclopropylmethyl)xanthine.
AID695680Inhibition of full-length PDE4A4 using cAMP as substrate by two-step radiochemical assay2011Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
Elucidation of a structural basis for the inhibitor-driven, p62 (SQSTM1)-dependent intracellular redistribution of cAMP phosphodiesterase-4A4 (PDE4A4).
AID159502Concentration required to inhibit 50% activity of phosphodiesterase IV isoenzyme (at 100 uM).1994Journal of medicinal chemistry, Feb-18, Volume: 37, Issue:4
Inhibition of cyclic nucleotide phosphodiesterase by derivatives of 1,3-bis(cyclopropylmethyl)xanthine.
AID159193Concentration required to inhibit 50% activity of phosphodiesterase III isoenzyme at 100 uM1994Journal of medicinal chemistry, Feb-18, Volume: 37, Issue:4
Inhibition of cyclic nucleotide phosphodiesterase by derivatives of 1,3-bis(cyclopropylmethyl)xanthine.
AID158122Inhibition of cGMP hydrolysis by PDE 5A1994Journal of medicinal chemistry, Feb-18, Volume: 37, Issue:4
Inhibition of cyclic nucleotide phosphodiesterase by derivatives of 1,3-bis(cyclopropylmethyl)xanthine.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (11)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's5 (45.45)18.2507
2000's3 (27.27)29.6817
2010's3 (27.27)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 (%)
Trials2 (18.18%)5.53%
Reviews1 (9.09%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other8 (72.73%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceDescriptionRelationhip StrengthStudiesTrialsClassesRoles
my 5445[no description available]medium10pyridazines;
ring assembly
theophylline[no description available]medium10dimethylxanthineadenosine receptor antagonist;
anti-asthmatic drug;
anti-inflammatory agent;
bronchodilator agent;
drug metabolite;
EC 3.1.4.* (phosphoric diester hydrolase) inhibitor;
fungal metabolite;
human blood serum metabolite;
immunomodulator;
muscle relaxant;
vasodilator agent
zaprinast[no description available]medium10triazolopyrimidines
sk&f 96231[no description available]medium10
ibudilast[no description available]medium10pyrazolopyridine
4-(3-butoxy-4-methoxybenzyl)-2-imidazolidinone[no description available]medium10methoxybenzenes
rolipram[no description available]medium50pyrrolidin-2-onesantidepressant;
EC 3.1.4.* (phosphoric diester hydrolase) inhibitor
(+)-rolipram[no description available]medium10rolipram
rolipram[no description available]medium10rolipram
rs 14203[no description available]medium10
rs 25344[no description available]medium10
betamethasone valerate[no description available]medium3011beta-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(1),Delta(4)-steroid;
fluorinated steroid;
primary alpha-hydroxy ketone;
steroid ester		anti-inflammatory drug
betamethasone valerate[no description available]medium3111beta-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(1),Delta(4)-steroid;
fluorinated steroid;
primary alpha-hydroxy ketone;
steroid ester		anti-inflammatory drug
rp 73401[no description available]medium10aromatic ether;
benzamides;
chloropyridine;
monocarboxylic acid amide		anti-asthmatic drug;
anti-inflammatory agent;
bronchodilator agent;
phosphodiesterase IV inhibitor
ovalbumin[no description available]medium10
tacrolimus[no description available]medium10macrolide lactambacterial metabolite;
immunosuppressive agent
bromochloroacetic acid[no description available]medium112-bromocarboxylic acid;
monocarboxylic acid;
organochlorine compound
sodium dodecyl sulfate[no description available]medium11organic sodium saltdetergent;
protein denaturant
pentoxifylline[no description available]medium20oxopurine
adenosine[no description available]medium10adenosines;
purines D-ribonucleoside		analgesic;
anti-arrhythmia drug;
fundamental metabolite;
human metabolite;
vasodilator agent
denbufylline[no description available]medium20oxopurine
thromboxane a2[no description available]medium10epoxy monocarboxylic acid;
thromboxanes A		mouse metabolite
15-hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5,13-dienoic acid[no description available]medium10
1,3-dipropyl-8-cyclopentylxanthine[no description available]low00oxopurineadenosine A1 receptor antagonist;
EC 3.1.4.* (phosphoric diester hydrolase) inhibitor
enprofylline[no description available]low00oxopurineanti-arrhythmia drug;
anti-asthmatic drug;
bronchodilator agent;
non-steroidal anti-inflammatory drug
7-(2-chloroethyl)theophylline[no description available]low00oxopurine
etofylline[no description available]low00oxopurine
8-cyclopentyl-1,3-dimethylxanthine[no description available]low00oxopurine
dyphylline[no description available]low00oxopurine;
propane-1,2-diols		bronchodilator agent;
EC 3.1.4.* (phosphoric diester hydrolase) inhibitor;
muscle relaxant;
vasodilator agent
furafylline[no description available]low00oxopurine
propentofylline[no description available]low00oxopurine
proxyphylline[no description available]low00oxopurine
bamifylline[no description available]low00oxopurine
fenethylline[no description available]low00oxopurine
1,3,7-trimethyl-8-(phenylmethyl)purine-2,6-dione[no description available]low00oxopurine
reproterol[no description available]low00oxopurine
etamiphylline[no description available]low00oxopurine
etofylline clofibrate[no description available]low00oxopurine
doxofylline[no description available]low00oxopurineanti-asthmatic drug;
antitussive;
bronchodilator agent
rolofylline[no description available]low00oxopurine
7-methylxanthine[no description available]low00oxopurine;
purine alkaloid		human xenobiotic metabolite;
mouse metabolite;
plant metabolite
acefylline[no description available]low00oxopurine
1-methyluric acid[no description available]low00oxopurinehuman xenobiotic metabolite;
mouse metabolite
1,3-dimethyluric acid[no description available]low00oxopurinemetabolite
pentifylline[no description available]low00oxopurine
theodrenaline[no description available]low00oxopurine
1,3,7,9-tetramethyluric acid[no description available]low00oxopurine;
purine alkaloid		analgesic;
anti-inflammatory agent;
human xenobiotic metabolite;
plant metabolite
isoguanine[no description available]low00oxopurine
1,3,7-trimethylurate[no description available]low00oxopurinehuman blood serum metabolite;
human urinary metabolite;
human xenobiotic metabolite;
mouse metabolite
3,7-dimethyluric acid[no description available]low00oxopurinemetabolite;
mouse metabolite
1,7-dimethyluric acid[no description available]low00oxopurinehuman xenobiotic metabolite;
mouse metabolite
2,8-dihydroxyadenine[no description available]low006-aminopurines;
diol;
heteroaryl hydroxy compound;
oxopurine		human urinary metabolite;
mammalian metabolite;
mouse metabolite;
nephrotoxic agent
1,3-dipropyl-8-phenylxanthine[no description available]low00oxopurine
8-methoxymethyl-3-isobutyl-1-methylxanthine[no description available]low00oxopurine
5-hydroxyisourate[no description available]low00oxopurinehuman metabolite;
mouse metabolite
4-[(1,3-dimethyl-2,6-dioxo-7H-purin-8-yl)methylamino]benzoic acid[no description available]low00oxopurine
1',3'-dimethylspiro[1H-indole-3,8'-7,9-dihydropurine]-2,2',6'-trione[no description available]low00oxopurine
8-anilino-1,3-dimethyl-7H-purine-2,6-dione[no description available]low00oxopurine
2-[[3-methyl-7-(3-methylbutyl)-2,6-dioxo-8-purinyl]thio]propanoic acid methyl ester[no description available]low00oxopurine
7-[2-hydroxy-3-(2-methylphenoxy)propyl]-3-methyl-8-(propan-2-ylthio)purine-2,6-dione[no description available]low00oxopurine
3-methyl-7-pentyl-8-(2-phenylethylthio)purine-2,6-dione[no description available]low00oxopurine
2-(1,3-dimethyl-2,6-dioxo-7-purinyl)-N-(phenylmethyl)-N-(2-pyridinyl)acetamide[no description available]low00oxopurine
7-[(4-fluorophenyl)methyl]-1,3-dimethyl-8-[(2-oxo-2-thiophen-2-ylethyl)thio]purine-2,6-dione[no description available]low00oxopurine
8-(butan-2-ylthio)-7-[(4-chlorophenyl)methyl]-3-methylpurine-2,6-dione[no description available]low00oxopurine
3,7-dimethyl-1-(phenylmethyl)-8-[(phenylmethyl)amino]purine-2,6-dione[no description available]low00oxopurine
7-[(3-bromophenyl)methyl]-1,3-dimethyl-8-(2-methylpropylamino)purine-2,6-dione[no description available]low00oxopurine
8-(1,3-benzothiazol-2-ylthio)-3-methyl-7-pentylpurine-2,6-dione[no description available]low00oxopurine
7-(2-methoxyethyl)-3-methyl-8-(phenylthio)purine-2,6-dione[no description available]low00oxopurine
7-[2-(1,3-benzothiazol-2-ylthio)ethyl]-1,3-dimethyl-8-(3-methyl-1-piperidinyl)purine-2,6-dione[no description available]low00oxopurine
8-(2,5-dimethylphenoxy)-1,3-dimethyl-7-prop-2-enylpurine-2,6-dione[no description available]low00oxopurine
3-methyl-7-(phenylmethyl)-8-(propan-2-ylthio)purine-2,6-dione[no description available]low00oxopurine
3-methyl-7-[(4-methylphenyl)methyl]-8-[2-(1-piperidinyl)ethylthio]purine-2,6-dione[no description available]low00oxopurine
7-[(2-chloro-6-fluorophenyl)methyl]-1,3-dimethyl-8-(1-piperidinylmethyl)purine-2,6-dione[no description available]low00oxopurine
2-[(7-ethyl-1,3-dimethyl-2,6-dioxo-8-purinyl)thio]-N-(6-methyl-2-pyridinyl)acetamide[no description available]low00oxopurine
8-(3-ethoxypropylamino)-1,3-dimethyl-7H-purine-2,6-dione[no description available]low00oxopurine
1,3-dimethyl-8-[methyl-(phenylmethyl)amino]-7-[2-(2-pyrimidinylthio)ethyl]purine-2,6-dione[no description available]low00oxopurine
3,5-dimethyl-4-isoxazolecarboxylic acid (3-butyl-2,6-dioxo-7-propyl-8-purinyl)methyl ester[no description available]low00oxopurine
7-(3-methoxypropyl)-3-(phenylmethyl)-8-(3-thiophenyl)purine-2,6-dione[no description available]low00oxopurine
6-thiouric acid[no description available]low00oxopurine
1,3-dimethyl-8-[2-(1-pyrrolidinyl)ethylthio]-6-sulfanylidene-7H-purin-2-one[no description available]low00oxopurine
3-methyl-7-(2-phenylethyl)-8-(propylamino)purine-2,6-dione[no description available]low00oxopurine
8-[(1-ethyl-3-piperidinyl)thio]-1,3-dimethyl-6-sulfanylidene-7H-purin-2-one[no description available]low00oxopurine
3-butyl-8-(2-fluorophenyl)-7-(phenylmethyl)purine-2,6-dione[no description available]low00oxopurine
4-[[7-[(4-fluorophenyl)methyl]-1,3-dimethyl-2,6-dioxo-8-purinyl]methyl]-1-piperazinecarboxylic acid ethyl ester[no description available]low00oxopurine
1,3-dimethyl-8-[[methyl-(phenylmethyl)amino]methyl]-7-(2-methylpropyl)purine-2,6-dione[no description available]low00oxopurine
8-[[4-[2-furanyl(oxo)methyl]-1-piperazinyl]methyl]-1,3-dimethyl-7-propylpurine-2,6-dione[no description available]low00oxopurine
4-[7-(2-methoxyethyl)-2,6-dioxo-3-(phenylmethyl)-8-purinyl]benzonitrile[no description available]low00oxopurine
2-(1,3-dimethyl-2,6-dioxo-7-purinyl)-N'-[2-(2-ethoxyphenoxy)-1-oxoethyl]acetohydrazide[no description available]low00oxopurine
2-(1,3-dimethyl-2,6-dioxo-7-purinyl)-N-[3-[(4-methoxyphenyl)sulfamoyl]-4-methylphenyl]acetamide[no description available]low00oxopurine
8-(4-methoxyphenyl)-7-methyl-3-(phenylmethyl)purine-2,6-dione[no description available]low00oxopurine
8-[[4-[2-furanyl(oxo)methyl]-1-piperazinyl]methyl]-1,3-dimethyl-7-[(2-methylphenyl)methyl]purine-2,6-dione[no description available]low00oxopurine
1,3-dimethyl-8-(3-methyl-1-piperidinyl)-7-[2-[(5-methyl-1,3,4-thiadiazol-2-yl)thio]ethyl]purine-2,6-dione[no description available]low00oxopurine
7-[(2-chloro-6-fluorophenyl)methyl]-1,3-dimethyl-8-[(3-methyl-1-piperidinyl)methyl]purine-2,6-dione[no description available]low00oxopurine
istradefylline[no description available]low00oxopurine
psb 1115[no description available]low00oxopurine
8-hydroxyadenine[no description available]low006-aminopurines;
heteroaryl hydroxy compound;
nucleobase analogue;
oxopurine		bacterial metabolite;
human metabolite
cafedrine[no description available]low00oxopurine
mrs 1754[no description available]low00oxopurine
psb 36[no description available]low00oxopurine
entecavir[no description available]low002-aminopurines;
oxopurine;
primary alcohol;
secondary alcohol		antiviral drug;
EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor
acyclovir[no description available]low002-aminopurines;
oxopurine		antimetabolite;
antiviral drug
guanine[no description available]low002-aminopurines;
oxopurine;
purine nucleobase		algal metabolite;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
hypoxanthine[no description available]low00nucleobase analogue;
oxopurine;
purine nucleobase		fundamental metabolite
ganciclovir[no description available]low002-aminopurines;
oxopurine		antiinfective agent;
antiviral drug
8-hydroxyguanine[no description available]low00oxopurine
7-ethylguanine[no description available]low00oxopurine
8-nitroguanine[no description available]low00oxopurine
8-oxyguanine[no description available]low002-aminopurines;
oxopurine
9-carboxymethoxymethylguanine[no description available]low00oxopurine
ConditionIndicatedRelationship StrengthStudiesTrials
Anterior Circulation Transient Ischemic Attack0low10
Brain Stem Ischemia, Transient0low10
Brain Stem Transient Ischemic Attack0low10
Brain TIA0low10
Brainstem Ischemia, Transient0low10
Brainstem Transient Ischemic Attack0low10
Carotid Circulation Transient Ischemic Attack0low10
Cerebral Ischemia, Transient0low10
Crescendo Transient Ischemic Attacks0low10
Dermatitis, Atopic0medium31
Dermatitis, Irritant0medium11
Dermatitis, Primary Irritant0medium11
Disease Models, Animal0low20
Eczema, Atopic0medium31
Eczema, Infantile0medium31
Endotoxin Shock0low10
Erythema0medium11
Hemorrhage, Subarachnoid0low10
Irritant Dermatitis0medium11
Ischemic Attack, Transient0low10
Neurodermatitis, Atopic0medium31
Neurodermatitis, Disseminated0medium31
Perinatal Subarachnoid Hemorrhage0low10
Posterior Circulation Transient Ischemic Attack0low10
Recrudescence0medium11
Recurrence0medium11
Relapse0medium11
SAH (Subarachnoid Hemorrhage)0low10
Septic Shock0low10
Shock, Endotoxic0low10
Shock, Septic0low10
Shock, Toxic0low10
Subarachnoid Hemorrhage0low10
Subarachnoid Hemorrhage, Aneurysmal0low10
Subarachnoid Hemorrhage, Intracranial0low10
Subarachnoid Hemorrhage, Spontaneous0low10
TIA (Transient Ischemic Attack)0low10
Toxic Shock0low10
Toxic Shock Syndrome0low10
Transient Ischemic Attack0low10
Transient Ischemic Attack, Anterior Circulation0low10
Transient Ischemic Attack, Brain Stem0low10
Transient Ischemic Attack, Brainstem0low10
Transient Ischemic Attack, Carotid Circulation0low10
Transient Ischemic Attack, Posterior Circulation0low10
Transient Ischemic Attack, Vertebrobasilar Circulation0low10
Transient Ischemic Attacks, Crescendo0low10
Vertebrobasilar Circulation Transient Ischemic Attack0low10

Research Highlights

Dosage (1)

ArticleYear
Effect of TNF alpha production inhibitors BRL 61063 and pentoxifylline on the response of rats to poly I:C.
Toxicology, Jan-06, Volume: 95, Issue: 1-3		1995
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]