Page last updated: 2024-11-04

tofisopam

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

Description

tofisopam: structure; dextofisopam is the R-enantiomer of tofisopam & antidiarrheal [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID5502
CHEMBL ID404216
CHEBI ID32241
SCHEMBL ID43522
SCHEMBL ID8086894
MeSH IDM0059701
PubMed CID23663407
CHEMBL ID66552
CHEBI ID76198
SCHEMBL ID383675
MeSH IDM0059701

Synonyms (112)

Synonym
LS-14948
1-[3,4-bis(methyloxy)phenyl]-5-ethyl-4-methyl-7,8-bis(methyloxy)-5h-2,3-benzodiazepine
tofisopam
tofisopam, >=98% (hplc), solid
1-(3,4-dimethoxyphenyl)-5-ethyl-7,8-dimethoxy-4-methyl-5h-2,3-benzodiazepine
tofizopam
tofisopamum [inn-latin]
egyt 341
einecs 244-922-3
5h-2,3-benzodiazepine, 1-(3,4-dimethoxyphenyl)-5-ethyl-7,8-dimethoxy-4-methyl-
grandaxin
tofisopam [inn:dcf:jan]
NCGC00165912-01
tofisopam (jp17/inn)
emandaxin (tn)
D01254
22345-47-7
NCGC00165912-02
emandaxin
CHEMBL404216
cas-22345-47-7
dtxcid303681
dtxsid3023681 ,
tox21_112269
ccris 8738
unii-uzc80hau42
uzc80hau42 ,
tofisopamum
seriel
FT-0638212
7,8-dimethoxy-1-(3,4-dimethoxyphenyl)-5-ethyl-4-methyl-5h-2,3-benzodiazepine
(+/-)-1-(3,4-dimethoxyphenyl)-5-ethyl-7,8-dimethoxy-4-methyl-5h-2,3-benzodiazepine
tofisopam [jan]
tofisopam [inn]
tofisopam [mi]
tofisopam [mart.]
tofisopam [who-dd]
DB08811
SCHEMBL43522
SCHEMBL8086894
1-(3,4-dimethoxyphenyl)-4-methyl-5-ethyl-7,8-dimethoxy-5h-2,3-benzodiazepine
T3509
tofisopam (patented in japan)
Q-201839
AC-24288
AKOS025401672
CHEBI:32241
5h-2,3-benzodiazepine, 1-(3,4-dimethoxyphenyl)-5-ethyl-7,8-dimethoxy-4-methyl-1-(3,4-dimethoxyphenyl)-4-methyl-5-ethyl-7,8-dimethoxy-5h-2,3-benzodiazepine; 7,8-dimethoxy-1-(3,4-dimethoxyphenyl)-5-ethyl-4-methyl-5h-2,3-benzodiazepine; egyt 341; grandaxin;
1-(3,4-dimethoxyphenyl)-5-ethyl-7,8-dimethoxy-4-methyl-5h-benzo[d][1,2]diazepine
BCP09600
Q945537
BRD-A69095630-001-01-1
(1z,3z)-1-(3,4-dimethoxyphenyl)-5-ethyl-7,8-dimethoxy-4-methyl-5h-benzo[d][1,2]diazepine
SB17495
SB17496
benzodiazepine; egyt 341; grandaxin; nodeprine; seriel
NCGC00165912-03
A878592
HY-A0165
HMS3393D12
cs-600g
lp-x
cs-600
lx-a
sodium 2-(4-(2-oxocyclopentylmethyl)phenyl)propionate dihydrate
loxoprofen sodium salt
benzeneacetic acid, alpha-methyl-4-((2-oxocyclopentyl)methyl)-, sodium salt, dihydrate
alpha-methyl-4-((2-oxocyclopentyl)methyl)benzeneacetate sodium salt dihydrate
MLS001401445
smr000469165
sodium loxoprofen
HMS2051D12
chebi:76198 ,
CHEMBL66552 ,
sodium 2-[4-[(2-oxocyclopentyl)methyl]phenyl]propionate
sodium 2-(4-((2-oxocyclopentyl)methyl)phenyl)propanoate
A839900
ndc2m7399s ,
unii-ndc2m7399s
HMS2233J14
AKOS015994737
c15h17nao3
CCG-101024
FT-0630879
HMS3370C11
sodium 2-(4-((2-oxocyclopentyl)methyl)(phenyl)propionate
benzeneacetic acid, .alpha.-methyl-4-((2-oxocyclopentyl)methyl)-, sodium salt (1:1)
loxoprofen sodium [who-dd]
loxoprofen sodium salt [mi]
loxoprofen sodium hydrate [jan]
NC00274
sodium 2-{4-[(2-oxocyclopentyl)methyl]phenyl}propanoate
KS-5040
SCHEMBL383675
Q-201325
2-[4-[(2-oxocyclopentyl)methyl]phenyl]propionic acid sodium salt
L0252
AKOS025392177
2-{4-[(2-oxocyclopentyl)methyl]phenyl}propanoate sodium salt
mfcd00941425
loxoprofen (sodium)
CS-0013894
HY-B0578A
WORCCYVLMMTGFR-UHFFFAOYSA-M
Q27145804
sodium;2-[4-[(2-oxocyclopentyl)methyl]phenyl]propanoate
AMY8901
CCG-267132
sodium2-(4-((2-oxocyclopentyl)methyl)phenyl)propanoate
BL164648
?-methyl-4-[(2-oxocyclopentyl)methyl]benzeneacetic acid sodium salt; cs 600; loxonin; sodium 2-[4-[(2-oxocyclopentyl)methyl]phenyl]propionate; sodium loxoprofen
losoprofen sodium

Research Excerpts

Overview

Tofisopam (Grandaxin) is a derivative of benzodiazepines. It is marketed for the treatment of anxiety in some European countries.

ExcerptReferenceRelevance
"Tofisopam is a member of the 2,3-benzodiazepine compound family which is marketed for the treatment of anxiety in some European countries. "( The atypical anxiolytic drug, tofisopam, selectively blocks phosphodiesterase isoenzymes and is active in the mouse model of negative symptoms of psychosis.
Rundfeldt, C; Socała, K; Wlaź, P, 2010
)
2.09
"Tofisopam (Grandaxin) is a derivative of benzodiazepines."( [A case in which tofisopam was effective for treatment of paroxysmal supraventricular tachycardia].
Kato, R; Ooi, K; Ueno, K, 2003
)
1.38
"Tofisopam is an anxiolytic agent of the BZD group, chemically 1(3-4 dimethoxyphenyl)-4methyl-5-ethyl-7,8 dimethoxy-5H-2,3-benzodiazepine. "( [Effect of tofisopam on CYP3A4 enzyme activity on human recombinant 3A4 supersome].
Bajnógel, J; Drabant, S; Egyed, A; Klebovich, I; Tömlo, J; Tóth, M, 2005
)
2.16
"Tofisopam is a new agent marketed in Europe as a minor tranquilizer. "( Comparative efficacy of tofisopam and placebo.
Finnerty, RJ; Goldberg, HL, 1979
)
2.01

Effects

Tofisopam also has mixed dopamine agonist and antagonist-like properties in several in vivo and in vitro tests in animals.

ExcerptReferenceRelevance
"Tofisopam has also mixed dopamine agonist and antagonist like properties."( [Pharmacologic effects of tofizopam (Grandaxin)].
Petócz, L, 1993
)
1.01
"Tofisopam also has mixed dopamine agonist and antagonist-like properties in several in vivo and in vitro tests in animals."( Is tofisopam an atypical anxiolytic?
File, SE; Pellow, S, 1986
)
1.61

Pharmacokinetics

ExcerptReferenceRelevance
" A high sensitive gas chromatography nitrogen phosphorous detection (GC-NPD) bioanalytical method was developed and validated for the purpose of pharmacokinetic study of tofisopam."( Gas chromatography nitrogen phosphorous detection (GC-NPD) assay of tofisopam in human plasma for pharmacokinetic evaluation.
Bereczki, A; Drabant, S; Grézal, G; Klebovich, I; Lakner, G; Nemes, KB; Tömlo, J; Tóth, M; Varga, B, 2006
)
0.76

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
" Although loxoprofen exhibits strong anti-inflammatory and analgesic activities with relatively low ulcerogenicity, its relatively low bioavailability makes it not an ideal drug candidate for intravenous injection."( HR1405-01, a Safe intravenous NSAID with superior anti-inflammatory and analgesic activities in preclinical trials.
Chen, X; Ding, B; Lv, T; Mao, D; Min, T; Ye, H; Zhang, C, 2022
)
0.72

Dosage Studied

ExcerptRelevanceReference
" A dosage of 25 mg/kg was ineffective."( Antidepressant-like effect of tofisopam in mice: A behavioural, molecular docking and MD simulation study.
Can, ÖD; Evren, AE; Kandemir, Ü; Turan Yücel, N, 2022
)
1.01
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (4)

RoleDescription
non-steroidal anti-inflammatory drugAn anti-inflammatory drug that is not a steroid. In addition to anti-inflammatory actions, non-steroidal anti-inflammatory drugs have analgesic, antipyretic, and platelet-inhibitory actions. They act by blocking the synthesis of prostaglandins by inhibiting cyclooxygenase, which converts arachidonic acid to cyclic endoperoxides, precursors of prostaglandins.
non-narcotic analgesicA drug that has principally analgesic, antipyretic and anti-inflammatory actions. Non-narcotic analgesics do not bind to opioid receptors.
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitorA compound or agent that combines with cyclooxygenases (EC 1.14.99.1) and thereby prevents its substrate-enzyme combination with arachidonic acid and the formation of icosanoids, prostaglandins, and thromboxanes.
antipyreticA drug that prevents or reduces fever by lowering the body temperature from a raised state. An antipyretic will not affect the normal body temperature if one does not have fever. Antipyretics cause the hypothalamus to override an interleukin-induced increase in temperature. The body will then work to lower the temperature and the result is a reduction in fever.
[role 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]

Drug Classes (2)

ClassDescription
organic molecular entityAny molecular entity that contains carbon.
organic sodium salt
[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 (15)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
glp-1 receptor, partialHomo sapiens (human)Potency10.00000.01846.806014.1254AID624172
TDP1 proteinHomo sapiens (human)Potency30.05340.000811.382244.6684AID686978; AID686979
AR proteinHomo sapiens (human)Potency31.79900.000221.22318,912.5098AID743035; AID743040
pregnane X nuclear receptorHomo sapiens (human)Potency1.00000.005428.02631,258.9301AID1346985
estrogen nuclear receptor alphaHomo sapiens (human)Potency23.89110.000229.305416,493.5996AID743075
DNA polymerase kappa isoform 1Homo sapiens (human)Potency29.93490.031622.3146100.0000AID588579
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency7.20800.005612.367736.1254AID624032
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency24.65590.011917.942071.5630AID651632; AID720516
Ataxin-2Homo sapiens (human)Potency23.71010.011912.222168.7989AID651632
importin subunit beta-1 isoform 1Homo sapiens (human)Potency6.51315.804836.130665.1308AID540253
snurportin-1Homo sapiens (human)Potency6.51315.804836.130665.1308AID540253
GTP-binding nuclear protein Ran isoform 1Homo sapiens (human)Potency6.51315.804816.996225.9290AID540253
[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)
cAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)IC50 (µMol)0.90000.00001.146310.0000AID1619495
Prostaglandin G/H synthase 1Homo sapiens (human)IC50 (µMol)24.00000.00021.557410.0000AID612057
Prostaglandin G/H synthase 2Homo sapiens (human)IC50 (µMol)10.00000.00010.995010.0000AID612058
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (96)

Processvia Protein(s)Taxonomy
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)
cell population proliferationATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of B cell proliferationATPase family AAA domain-containing protein 5Homo sapiens (human)
nuclear DNA replicationATPase family AAA domain-containing protein 5Homo sapiens (human)
signal transduction in response to DNA damageATPase family AAA domain-containing protein 5Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorATPase family AAA domain-containing protein 5Homo sapiens (human)
isotype switchingATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of DNA replicationATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of isotype switching to IgG isotypesATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA clamp unloadingATPase family AAA domain-containing protein 5Homo sapiens (human)
regulation of mitotic cell cycle phase transitionATPase family AAA domain-containing protein 5Homo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of cell cycle G2/M phase transitionATPase family AAA domain-containing protein 5Homo sapiens (human)
negative regulation of receptor internalizationAtaxin-2Homo sapiens (human)
regulation of translationAtaxin-2Homo sapiens (human)
RNA metabolic processAtaxin-2Homo sapiens (human)
P-body assemblyAtaxin-2Homo sapiens (human)
stress granule assemblyAtaxin-2Homo sapiens (human)
RNA transportAtaxin-2Homo sapiens (human)
prostaglandin biosynthetic processProstaglandin G/H synthase 1Homo sapiens (human)
response to oxidative stressProstaglandin G/H synthase 1Homo sapiens (human)
regulation of blood pressureProstaglandin G/H synthase 1Homo sapiens (human)
cyclooxygenase pathwayProstaglandin G/H synthase 1Homo sapiens (human)
regulation of cell population proliferationProstaglandin G/H synthase 1Homo sapiens (human)
cellular oxidant detoxificationProstaglandin G/H synthase 1Homo sapiens (human)
prostaglandin biosynthetic processProstaglandin G/H synthase 2Homo sapiens (human)
angiogenesisProstaglandin G/H synthase 2Homo sapiens (human)
response to oxidative stressProstaglandin G/H synthase 2Homo sapiens (human)
embryo implantationProstaglandin G/H synthase 2Homo sapiens (human)
learningProstaglandin G/H synthase 2Homo sapiens (human)
memoryProstaglandin G/H synthase 2Homo sapiens (human)
regulation of blood pressureProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of cell population proliferationProstaglandin G/H synthase 2Homo sapiens (human)
response to xenobiotic stimulusProstaglandin G/H synthase 2Homo sapiens (human)
response to nematodeProstaglandin G/H synthase 2Homo sapiens (human)
response to fructoseProstaglandin G/H synthase 2Homo sapiens (human)
response to manganese ionProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of vascular endothelial growth factor productionProstaglandin G/H synthase 2Homo sapiens (human)
cyclooxygenase pathwayProstaglandin G/H synthase 2Homo sapiens (human)
bone mineralizationProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of prostaglandin biosynthetic processProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of fever generationProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of synaptic plasticityProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of synaptic transmission, dopaminergicProstaglandin G/H synthase 2Homo sapiens (human)
prostaglandin secretionProstaglandin G/H synthase 2Homo sapiens (human)
response to estradiolProstaglandin G/H synthase 2Homo sapiens (human)
response to lipopolysaccharideProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of peptidyl-serine phosphorylationProstaglandin G/H synthase 2Homo sapiens (human)
response to vitamin DProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to heatProstaglandin G/H synthase 2Homo sapiens (human)
response to tumor necrosis factorProstaglandin G/H synthase 2Homo sapiens (human)
maintenance of blood-brain barrierProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of protein import into nucleusProstaglandin G/H synthase 2Homo sapiens (human)
hair cycleProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of apoptotic processProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of nitric oxide biosynthetic processProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of cell cycleProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of vasoconstrictionProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of smooth muscle contractionProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of smooth muscle contractionProstaglandin G/H synthase 2Homo sapiens (human)
decidualizationProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of smooth muscle cell proliferationProstaglandin G/H synthase 2Homo sapiens (human)
regulation of inflammatory responseProstaglandin G/H synthase 2Homo sapiens (human)
brown fat cell differentiationProstaglandin G/H synthase 2Homo sapiens (human)
response to glucocorticoidProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of calcium ion transportProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of synaptic transmission, glutamatergicProstaglandin G/H synthase 2Homo sapiens (human)
response to fatty acidProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to mechanical stimulusProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to lead ionProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to ATPProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to hypoxiaProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to non-ionic osmotic stressProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to fluid shear stressProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of transforming growth factor beta productionProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of cell migration involved in sprouting angiogenesisProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of fibroblast growth factor productionProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of brown fat cell differentiationProstaglandin G/H synthase 2Homo sapiens (human)
positive regulation of platelet-derived growth factor productionProstaglandin G/H synthase 2Homo sapiens (human)
cellular oxidant detoxificationProstaglandin G/H synthase 2Homo sapiens (human)
regulation of neuroinflammatory responseProstaglandin G/H synthase 2Homo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathway in response to osmotic stressProstaglandin G/H synthase 2Homo sapiens (human)
cellular response to homocysteineProstaglandin G/H synthase 2Homo sapiens (human)
response to angiotensinProstaglandin G/H synthase 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (26)

Processvia Protein(s)Taxonomy
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)
protein bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
ATP bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
ATP hydrolysis activityATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA clamp unloader activityATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
RNA bindingAtaxin-2Homo sapiens (human)
epidermal growth factor receptor bindingAtaxin-2Homo sapiens (human)
protein bindingAtaxin-2Homo sapiens (human)
mRNA bindingAtaxin-2Homo sapiens (human)
peroxidase activityProstaglandin G/H synthase 1Homo sapiens (human)
prostaglandin-endoperoxide synthase activityProstaglandin G/H synthase 1Homo sapiens (human)
protein bindingProstaglandin G/H synthase 1Homo sapiens (human)
heme bindingProstaglandin G/H synthase 1Homo sapiens (human)
metal ion bindingProstaglandin G/H synthase 1Homo sapiens (human)
oxidoreductase activity, acting on single donors with incorporation of molecular oxygen, incorporation of two atoms of oxygenProstaglandin G/H synthase 1Homo sapiens (human)
peroxidase activityProstaglandin G/H synthase 2Homo sapiens (human)
prostaglandin-endoperoxide synthase activityProstaglandin G/H synthase 2Homo sapiens (human)
protein bindingProstaglandin G/H synthase 2Homo sapiens (human)
enzyme bindingProstaglandin G/H synthase 2Homo sapiens (human)
heme bindingProstaglandin G/H synthase 2Homo sapiens (human)
protein homodimerization activityProstaglandin G/H synthase 2Homo sapiens (human)
metal ion bindingProstaglandin G/H synthase 2Homo sapiens (human)
oxidoreductase activity, acting on single donors with incorporation of molecular oxygen, incorporation of two atoms of oxygenProstaglandin G/H synthase 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (26)

Processvia Protein(s)Taxonomy
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)
Elg1 RFC-like complexATPase family AAA domain-containing protein 5Homo sapiens (human)
nucleusATPase family AAA domain-containing protein 5Homo sapiens (human)
cytoplasmAtaxin-2Homo sapiens (human)
Golgi apparatusAtaxin-2Homo sapiens (human)
trans-Golgi networkAtaxin-2Homo sapiens (human)
cytosolAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
membraneAtaxin-2Homo sapiens (human)
perinuclear region of cytoplasmAtaxin-2Homo sapiens (human)
ribonucleoprotein complexAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
photoreceptor outer segmentProstaglandin G/H synthase 1Homo sapiens (human)
cytoplasmProstaglandin G/H synthase 1Homo sapiens (human)
endoplasmic reticulum membraneProstaglandin G/H synthase 1Homo sapiens (human)
Golgi apparatusProstaglandin G/H synthase 1Homo sapiens (human)
intracellular membrane-bounded organelleProstaglandin G/H synthase 1Homo sapiens (human)
extracellular exosomeProstaglandin G/H synthase 1Homo sapiens (human)
cytoplasmProstaglandin G/H synthase 1Homo sapiens (human)
neuron projectionProstaglandin G/H synthase 1Homo sapiens (human)
nuclear inner membraneProstaglandin G/H synthase 2Homo sapiens (human)
nuclear outer membraneProstaglandin G/H synthase 2Homo sapiens (human)
cytoplasmProstaglandin G/H synthase 2Homo sapiens (human)
endoplasmic reticulumProstaglandin G/H synthase 2Homo sapiens (human)
endoplasmic reticulum lumenProstaglandin G/H synthase 2Homo sapiens (human)
endoplasmic reticulum membraneProstaglandin G/H synthase 2Homo sapiens (human)
caveolaProstaglandin G/H synthase 2Homo sapiens (human)
neuron projectionProstaglandin G/H synthase 2Homo sapiens (human)
protein-containing complexProstaglandin G/H synthase 2Homo sapiens (human)
neuron projectionProstaglandin G/H synthase 2Homo sapiens (human)
cytoplasmProstaglandin G/H synthase 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (43)

Assay IDTitleYearJournalArticle
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.
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.
AID628755Inhibition of bovine aortic PDE3 using cAMP as substrate in presence of rolipram2011Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21
New PDE4 inhibitors based on pharmacophoric similarity between papaverine and tofisopam.
AID628754Inhibition of bovine aortic endothelial cells PDE2 using cAMP as substrate in presence of cGMP2011Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21
New PDE4 inhibitors based on pharmacophoric similarity between papaverine and tofisopam.
AID628753Inhibition of bovine aortic PDE1 using calmodulin activated cGMP as substrate2011Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21
New PDE4 inhibitors based on pharmacophoric similarity between papaverine and tofisopam.
AID311932Inhibition of ASM in human H4 cells assessed as residual activity at 10 uM2008Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2
Identification of new functional inhibitors of acid sphingomyelinase using a structure-property-activity relation model.
AID628752Inhibition of bovine aortic PDE4 using cAMP as substrate in presence of cGMP2011Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21
New PDE4 inhibitors based on pharmacophoric similarity between papaverine and tofisopam.
AID1745845Primary 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.
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.
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID179638Antiinflammatory activity on peroral administration against adjuvant arthritis in rat.1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Synthesis and antiinflammatory activity of [(cycloalkylmethyl)phenyl]acetic acids and related compounds.
AID537750Inhibition of COX1 in human whole blood assessed as TXB2 biosynthesis after 24 hrs by EIA2010Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21
Properties and synthesis of 2-{2-fluoro (or bromo)-4-[(2-oxocyclopentyl)methyl]phenyl}propanoic acid: nonsteroidal anti-inflammatory drugs with low membrane permeabilizing and gastric lesion-producing activities.
AID537752Selectivity ratio of IC50 for human COX1-derived TXB2 biosynthesis to IC50 for human COX2-derived PGE2 biosynthesis2010Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21
Properties and synthesis of 2-{2-fluoro (or bromo)-4-[(2-oxocyclopentyl)methyl]phenyl}propanoic acid: nonsteroidal anti-inflammatory drugs with low membrane permeabilizing and gastric lesion-producing activities.
AID537756Antiinflammatory activity against Wistar rat assessed as decrease in gastric level of PGE2 at 40 to 50 mg/kg, po2010Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21
Properties and synthesis of 2-{2-fluoro (or bromo)-4-[(2-oxocyclopentyl)methyl]phenyl}propanoic acid: nonsteroidal anti-inflammatory drugs with low membrane permeabilizing and gastric lesion-producing activities.
AID179451Analgesic activity on peroral administration against Scald induced pain in rat paw1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Synthesis and antiinflammatory activity of [(cycloalkylmethyl)phenyl]acetic acids and related compounds.
AID76665Antipyretic activity on peroral administration against LPS-induced fever in guinea pig.1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Synthesis and antiinflammatory activity of [(cycloalkylmethyl)phenyl]acetic acids and related compounds.
AID612063Reduction in PGE2 levels in fasted Wistar rat stomach at 40 to 50 mg/kg, po measured after 8 hrs2011Bioorganic & medicinal chemistry, Jun-01, Volume: 19, Issue:11
Synthesis and biological evaluation of loxoprofen derivatives.
AID537751Inhibition of COX2 in human whole blood assessed as PGE2 biosynthesis after 24 hrs by EIA2010Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21
Properties and synthesis of 2-{2-fluoro (or bromo)-4-[(2-oxocyclopentyl)methyl]phenyl}propanoic acid: nonsteroidal anti-inflammatory drugs with low membrane permeabilizing and gastric lesion-producing activities.
AID612061Ulcerogenicity in fasted Wistar rat assessed as damage in gastric mucosa at 40 to 50 mg/kg, po measured after 8 hrs2011Bioorganic & medicinal chemistry, Jun-01, Volume: 19, Issue:11
Synthesis and biological evaluation of loxoprofen derivatives.
AID178496Antiinflammatory activity on peroral administration in rat determined by Randall-Slelitto test1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Synthesis and antiinflammatory activity of [(cycloalkylmethyl)phenyl]acetic acids and related compounds.
AID537759Antiinflammatory activity in rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, po administered 1 hr before carrageenan challenge measured after 3 to 6 hrs2010Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21
Properties and synthesis of 2-{2-fluoro (or bromo)-4-[(2-oxocyclopentyl)methyl]phenyl}propanoic acid: nonsteroidal anti-inflammatory drugs with low membrane permeabilizing and gastric lesion-producing activities.
AID177772Analgesic activity on peroral administration against Bradykinin induced pain in rat paw1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Synthesis and antiinflammatory activity of [(cycloalkylmethyl)phenyl]acetic acids and related compounds.
AID612065Antiinflammatory activity in Wistar rat assessed as inhibition of carrageenan-induced foot-pad edema at 10 mg/kg, po administered 1 hr before carrageenan challenge measured after 3 to 6 hrs by plethysmometer2011Bioorganic & medicinal chemistry, Jun-01, Volume: 19, Issue:11
Synthesis and biological evaluation of loxoprofen derivatives.
AID537753Toxicity in Wistar rat assessed as gastric lesion at 40 to 50 mg/kg, po2010Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21
Properties and synthesis of 2-{2-fluoro (or bromo)-4-[(2-oxocyclopentyl)methyl]phenyl}propanoic acid: nonsteroidal anti-inflammatory drugs with low membrane permeabilizing and gastric lesion-producing activities.
AID182814Gastric lesion activity on peroral administration in rat.1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Synthesis and antiinflammatory activity of [(cycloalkylmethyl)phenyl]acetic acids and related compounds.
AID612059Membrane permeabilization activity assessed as release of calcein from liposomes after 10 mins by fluorescence assay2011Bioorganic & medicinal chemistry, Jun-01, Volume: 19, Issue:11
Synthesis and biological evaluation of loxoprofen derivatives.
AID537762Membrane permeabilization activity in calcein-loaded liposome assessed as calcein release at 0.1 to 1 M by fluorescence assay2010Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21
Properties and synthesis of 2-{2-fluoro (or bromo)-4-[(2-oxocyclopentyl)methyl]phenyl}propanoic acid: nonsteroidal anti-inflammatory drugs with low membrane permeabilizing and gastric lesion-producing activities.
AID612148Inhibition of PGE2 production in carrageenan-induced Wistar rat foot-pad at 10 mg/kg, po administered 1 hr before carrageenan challenge by EIA2011Bioorganic & medicinal chemistry, Jun-01, Volume: 19, Issue:11
Synthesis and biological evaluation of loxoprofen derivatives.
AID612060Selectivity ratio of IC50 for human COX-1 to IC50 for human COX-22011Bioorganic & medicinal chemistry, Jun-01, Volume: 19, Issue:11
Synthesis and biological evaluation of loxoprofen derivatives.
AID612057Inhibition of human whole blood COX-1 assessed as production of TXB2 after 24 hrs by EIA2011Bioorganic & medicinal chemistry, Jun-01, Volume: 19, Issue:11
Synthesis and biological evaluation of loxoprofen derivatives.
AID612058Inhibition of human whole blood COX-2 assessed as production of PGE2 after 24 hrs by EIA2011Bioorganic & medicinal chemistry, Jun-01, Volume: 19, Issue:11
Synthesis and biological evaluation of loxoprofen derivatives.
AID182609Antiinflammatory activity on peroral administration against carrageenan paw edema1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Synthesis and antiinflammatory activity of [(cycloalkylmethyl)phenyl]acetic acids and related compounds.
AID1906163Effect on metabolic conversion rate in rat liver homogenate measured up to 240 mins by HPLC analysis2022European journal of medicinal chemistry, May-05, Volume: 235HR1405-01, a Safe intravenous NSAID with superior anti-inflammatory and analgesic activities in preclinical trials.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (99)

TimeframeStudies, This Drug (%)All Drugs %
pre-199042 (42.42)18.7374
1990's14 (14.14)18.2507
2000's21 (21.21)29.6817
2010's14 (14.14)24.3611
2020's8 (8.08)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 69.29

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 Index69.29 (24.57)
Research Supply Index4.82 (2.92)
Research Growth Index4.44 (4.65)
Search Engine Demand Index117.85 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (69.29)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials19 (18.27%)5.53%
Trials0 (0.00%)5.53%
Reviews10 (9.62%)6.00%
Reviews0 (0.00%)6.00%
Case Studies2 (1.92%)4.05%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Observational0 (0.00%)0.25%
Other73 (70.19%)84.16%
Other8 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (2)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Double-Blind, Randomized, Placebo-Controlled Phase 2b Study of 100, 200, and 300 mg BID Dextofisopam in Female Outpatients With Irritable Bowel Syndrome [NCT00486876]Phase 2324 participants (Actual)Interventional2007-06-30Completed
Open-Label, Inpatient Study of Levotofisopam 50 mg TID Administered for 7 Days to Men and Postmenopausal Women With Hyperuricemia and Gout [NCT01519687]Phase 220 participants (Anticipated)Interventional2012-01-31Recruiting
[information is prepared from clinicaltrials.gov, extracted Sep-2024]