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(-)-6-(3-(3-cyclopropyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone
-
IC50: 0.1195 mM, PDE7
(2E)-9,10-dimethoxy-3-methyl-2-[(2,4,6-trimethylphenyl)imino]-2,3,6,7-tetrahydro-4H-pyrimido[6,1-a]isoquinolin-4-one
-
(2R,3R)-3-(6-amino-9H-purin-9-yl)nonan-2-ol
-
IC50: 0.31 mM, PDE4
(2Z)-9,10-dimethoxy-3-methyl-2-[(2,4,6-trimethylphenyl)imino]-2,3,6,7-tetrahydro-4H-pyrimido[6,1-a]isoquinolin-4-one
-
IC50: 0.00043 mM, PDE4
(4aS,8aR)-4-(3,4-dimethoxyphenyl)-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
-
-
1,10-phenanthroline
-
0.3 mM, more than 95% inhibition
1-(2,4-dichlorobenzyl)-7-(2-oxopropyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
-
-
1-(2-methylbenzyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
-
-
1-(2-methylbenzyl)-7-(2-oxopropyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
-
-
1-(3-chlorobenzyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
-
-
1-(3-chlorobenzyl)-7-(2-oxopropyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
-
-
1-(3-methylbenzyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
-
-
1-(4-chlorobenzyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
-
-
1-(4-chlorobenzyl)-7-(2-oxopropyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
-
-
1-(4-methylbenzyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
-
-
1-(4-methylbenzyl)-7-(2-oxopropyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
-
-
1-benzyl-7-(2-oxopropyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione
-
-
10-(3-pyrrolidin-1-ylpropyl)-2-(trifluoromethyl)-10H-phenoxazine
-
-
10-(4'-N-morpholinobutyl)-2-chlorophenoxazine
-
-
10-(4'-N-morpholinobutyl)-2-trifluoromethylphenoxazine
-
-
10-(4'-N-piperidinobutyl)-2-chlorophenoxazine
-
-
10-(4'-N-piperidinobutyl)-2-trifluoromethylphenoxazine
-
-
10-(4'-N-pyrrolidinobutyl)-2-chlorophenoxazine
-
-
10-(4'-N-pyrrolidinobutyl)-2-trifluoromethylphenoxazine
-
increase of Km value in presence of inhibitor
10-[3'-[(beta-hydroxyethyl)-piperazino]propyl]-2-trifluoromethylphenoxazine
-
-
10-[30-[(beta-hydroxy ethyl)-piperazino]propyl]-2-chlorophenoxazine
-
-
10-[4'-(N-diethylamino)-butyl]-2-chlorophenoxazine
-
-
10-[4'-(N-diethylamino)butyl]-2-trifluoromethylphenoxazine
-
-
10-[4'-[(beta-hydroxy ethyl)-piperazino]butyl]-2-trifluoro-methylphenoxazine
-
-
10-[4'-[(beta-hydroxy-ethyl)piperazino]butyl]-2-chlorophenoxazine
-
-
2-cyclohexyl-2-methyl-N1-[3-(2-oxo-1,2-dihydro-6-quinolyl,oxy)propyl]-1-hydrazinecarboxamide
-
IC50: 0.0203 mM, PDE7; IC50: 0.0453 mM, PDE4
3-(1-methyl-7-oxo-3-propyl-4,7-dihydro-1H-pyrazolo[4,3-d]pyrimidin-5-yl)-N-[2-(1-methylpyrrolidin-2-yl)ethyl]-4-propoxybenzenesulfonamide
-
-
3-(6-aminopurin-9-yl)nonan-2-ol hydrochloride
-
3-isobutyl-1-methyl-xanthine
3-isobutyl-1-methylxanthine
3-isobutyl-methylxanthine
-
inhibitor of all PDE isoforms except PDE8
3-isobuytl-1-methylxanthine
-
4-(3,4-dimethoxy-phenyl)-4a,5,8,8a-tetrahydro-2H-phthalazin-1-one
-
PDE4 inhibitor, potent inhibitor of isoform PDE4D3
4-(3,4-dimethoxyphenyl)-2-{5-[(2-{5-[2-(2-fluoro-5-methoxyphenyl)ethyl]tetrahydrofuran-2-yl}ethyl)amino]pentyl}-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
-
the dual PDE4 inhibitor/selective serotonin reuptake inhibitor shows potent and selective serotonin reuptake inhibition
4-(3-Butoxy-4-methoxybenzyl)-2-imidazolidinone
4-[(2-chloro-4-nitrophenyl)thio]-pyridine
-
4-[(3-butoxy-4-methoxyphenyl)methyl]-2-imidazolidinone
-
competitive
4-[8-(3-nitrophenyl)-[1,7]naphthyridin-6-yl]benzoic acid
i.e. NVP; i.e. NVP; i.e. NVP
6-(3,4-dimethoxyphenyl)-2-[4-(morpholinomethyl)benzyl]-4,5-dihydropyridazin-3(2H)-one
-
-
6-(3-(3-cyclooctyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone
-
IC50: 0.0513 mM, PDE7; IC50: 0.1008 mM, PDE4
8-(4-chlorophenyl)thioguanosine 3',5'-cyclic monophosphate
-
-
8-bromoguanosine 3',5'-cyclic monophosphate
-
-
8-methoxymethyl-isobutylmethylxanthine
-
inhibits activated PDE1 and PDE2 isoforms as well as PDE4 and PDE5
alpha-alpha'-dipyridyl
treatment of CpdA with the Fe2+-specific chelator alpha-alpha'-dipyridyl results in a nearly complete loss of activity
apigenin-7-O-glucoside
-
-
apremilast
-
CC-10004, i.e. (S)-N-[2-[1-(3-ethoxy-4-methoxyphenyl)-2-methanesulfonylethyl]-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl]acetamide, oral phosphodiesterase-4 inhibitor, apremilast shows no marked selectivity among PDE4 isozymes
AWD 12-281
-
selective PDE4 inhibitor
ayanin
-
i.e. quercetin-3,7,4'-O-trimethylether, non-selective phosphodiesterase 1-4 inhibitor
Biochanin A
-
IC50: 0.0085 mM, more selectively inhibits PDE4 than PDE1 or PDE2
BRL-50481
-
PDE7 inhibitor
cGMP
-
5% inhibition at 0.1 mM
chamomile
-
inhibits cAMP-PDE activity
CI-1044
-
i.e. (R)-N-[9-amino-3,4,6,7-tetrahydro-4-oxo-1-phenylpyrrolo[3,2,1-j,k][1,4] benzodiazepin-3-yl]-3-pyridinecarboxamide, selective inhibitor of PDE4, administration of 160 mg/kg of CI-1044 causes perivascular and interstitial inflammation, with infiltrates of admixed neutrophils and macrophages but without evidence of vascular necrosis, PDE4 inhibitor CI-1044 induces changes of vascular tone that could lead to histological alterations in the mesenteric area
cilostazol
-
IC50: 0.0214 mM, PDE7; IC50: 0.088 mM, PDE4
cis-(+)-4-(3,4-dimethoxyphenyl)-2-[4-(morpholinomethyl)benzyl]-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
-
-
cis-(+)-4-(3,4-dimethoxyphenyl)-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
-
-
cis-(+/-)-4-(3,4-dimethoxyphenyl)-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
-
-
cis-(-)-4-(3,4-dimethoxyphenyl)-2-[4-(morpholinomethyl)benzyl]-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
-
-
cis-(-)-4-(3,4-dimethoxyphenyl)-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
-
-
cis-2-[(E)-4-(1H-imidazol-1-yl)but-2-enyl]-4-(3,4-dimethoxyphenyl)-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
-
-
cis-2-[2-[2-(1H-imidazol-1-yl)ethoxy]ethyl]-4-(3,4-dimethoxyphenyl)-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
-
-
cis-2-[4-(1,4-dioxa-8-azaspiro[4.5]decan-8-ylmethyl)-benzyl]-4-(3,4-dimethoxyphenyl)-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
-
-
cis-2-[4-[(1H-imidazol-1-yl)methyl]benzyl]-4-(3,4-dimethoxyphenyl)-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
-
-
cis-4-(3,4-dimethoxyphenyl)-2-[2-(morpholinomethyl)benzyl]-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
-
-
cis-4-(3,4-dimethoxyphenyl)-2-[3-(morpholinomethyl)benzyl]-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
-
-
cis-4-(3,4-dimethoxyphenyl)-2-[4-(morpholinomethyl)benzyl]-4a,5,6,7,8,8a-hexahydrophthalazin-1(2H)-one
-
-
cis-4-(3,4-dimethoxyphenyl)-2-[4-(morpholinomethyl)benzyl]-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
-
-
cis-4-(3,4-dimethoxyphenyl)-2-[4-(piperidin-1-ylmethyl)benzyl]-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
-
-
cis-4-(3,4-dimethoxyphenyl)-2-[4-[(4-methylpiperazin-1-yl)methyl]benzyl]-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
-
-
cis-4-(3,4-dimethoxyphenyl)-2-[4-[(4-oxopiperidin-1-yl)-methyl]benzyl]-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
-
-
cis-4-(3,4-dimethoxyphenyl)-2-[4-[(dimethylamino)-methyl]benzyl]-4a,5,8,8a-tetrahydrophthalazin-1(2H)-one
-
-
cis-5-(3,4-dimethoxyphenyl)-3-[4-(morpholinomethyl)benzyl]-3,4-diazabicyclo[4.1.0]hept-4-en-2-one
-
-
cis-5-(3,4-dimethoxyphenyl)-3-[4-(morpholinomethyl)benzyl]-3,4-diazabicyclo[4.2.0]oct-4-en-2-one hydrochloride
-
-
DC-TA 46
-
the inhibitor affects memory retention in a visible/hidden-platform water maze task. This memory impairment can be correlated to the decrease of cAMP nucleotide, due to the induction of a PDE4D cAMP-specific PDE isoform
dexamethasone
-
dexmethasone at 0.1 mg/kg inhibits the activity of PDE4
dioclein
-
dioclein is at least 11times more potent in inhibiting calmodulin-activated PDE1 than other PDE types. Among PDE1-PDE5, dioclein is at least 19fold more selective for the activated PDE1 isoform compared to PDE3
diosmetin
-
IC50: 0.0202 mM, PDE4
erythro-9-(2-hydroxy-3-nonyl)-adenine hydrochloride
-
erythro-9-(2-hydroxy-3-nonyl)adenine
erythro-9-[3-(2-hydroxynonyl)]-adenine
-
erythro-9-[3-(2-hydroxynonyl)]adenine
-
0.1 mM, 12% inhibition, wild-type enzyme
ethaverine
-
IC50: 0.008 mM
ethyl 2-([4-(3-carbamoylpiperazin-1-yl)-6-[4-(dimethylamino)piperidin-1-yl]pyrimidin-2-yl]amino)-4-methyl-1,3-thiazole-5-carboxylate
-
-
ethyl 2-([4-[(3,4-dimethoxybenzyl)amino]-6-(piperazin-1-yl)pyrimidin-2-yl]amino)-4-methyl-1,3-thiazole-5-carboxylate
-
-
ethyl 2-([4-[4-(dimethylamino)piperidin-1-yl]-6-(4-hydroxypiperidin-1-yl)pyrimidin-2-yl]amino)-4-methyl-1,3-thiazole-5-carboxylate
-
-
ethyl 2-([4-[4-(dimethylamino)piperidin-1-yl]-6-(4-methylpiperazin-1-yl)pyrimidin-2-yl]amino)-4-methyl-1,3-thiazole-5-carboxylate
-
-
ethyl 2-([4-[4-(dimethylamino)piperidin-1-yl]-6-(morpholin-4-yl)pyrimidin-2-yl]amino)-4-methyl-1,3-thiazole-5-carboxylate
-
-
ethyl 2-([4-[4-(dimethylamino)piperidin-1-yl]-6-[3-(hydroxymethyl)piperidin-1-yl]pyrimidin-2-yl]amino)-4-methyl-1,3-thiazole-5-carboxylate
-
-
ethyl 2-([7-ethyl-6-[(4-sulfamoylbenzyl)amino]-7H-purin-2-yl]amino)-4-methyl-1,3-thiazole-5-carboxylate
-
-
ethyl 2-[[4,6-bis(4-hydroxypiperidin-1-yl)pyrimidin-2-yl]amino]-4-methyl-1,3-thiazole-5-carboxylate
-
-
ethyl 2-[[4-[4-[2-(dimethylamino)ethyl]piperazin-1-yl]-6-(4-methylpiperazin-1-yl)pyrimidin-2-yl]amino]-4-methyl-1,3-thiazole-5-carboxylate
-
-
ethyl 3,5-dimethyl-1-phenyl-1H-pyrazole-4-carboxylate
-
IC50: 0.00027 mM, PDE4D; IC50: 0.00031 mM, PDE4B
ethyl 3,5-dimethyl-1-quinolin-8-yl-1H-pyrazole-4-carboxylate
-
IC50: 0.017 mM, PDE4B; IC50: 0.019 mM, PDE4D
ethyl 3,5-dimethyl-1H-pyrazole-4-carboxylate
-
IC50: 0.015 mM, PDE4B; IC50: 0.019 mM, PDE4D
ethyl 3-(4-chlorophenyl)-1-phenyl-1H-pyrazole-4-carboxylate
-
IC50: 0.00088 mM, PDE4D; IC50: 0.0015 mM, PDE4B
ethyl 3-methyl-5-(4-methylphenyl)-1H-pyrazole-4-carboxylate
-
IC50: 0.06 mM, PDE4B; IC50: 0.082 mM, PDE4D
ethyl 4-methyl-2-([4-(4-methylpiperazin-1-yl)-6-[methyl(3,4,5-trimethoxybenzyl)amino]pyrimidin-2-yl]amino)-1,3-thiazole-5-carboxylate
-
-
ethyl 4-methyl-2-([4-(methylamino)-6-[(4-sulfamoylbenzyl)amino]pyrimidin-2-yl]amino)-1,3-thiazole-5-carboxylate
-
-
ethyl 4-methyl-2-([4-(piperazin-1-yl)-6-[(4-sulfamoylbenzyl)amino]pyrimidin-2-yl]amino)-1,3-thiazole-5-carboxylate
-
-
ethyl 4-methyl-2-([4-[(4-sulfamoylbenzyl)amino]pyrimidin-2-yl]amino)-1,3-thiazole-5-carboxylate
-
-
ethyl 4-methyl-2-([4-[methyl(3,4,5-trimethoxybenzyl)amino]-6-(piperazin-1-yl)pyrimidin-2-yl]amino)-1,3-thiazole-5-carboxylate
-
-
ethyl 4-methyl-2-[[4-(piperazin-1-yl)-7-(3,4,5-trimethoxybenzyl)-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidin-2-yl]amino]-1,3-thiazole-5-carboxylate
-
-
ethyl 5-amino-1-(4a,5,6,7,8,9a-hexahydro[1]benzothieno[2,3-d]pyrimidin-4-yl)-1H-pyrazole-4-carboxylate
-
IC50: 0.025 mM, PDE4B; IC50: 0.05 mM, PDE4D
genistein
-
IC50: 0.0095 mM, PDE4
hesperetin
-
IC50: 0.0282 mM, PDE4
IBMX
non-selective PDE inhibitor
imperatorin
-
potent PFE4 inhibitor, imperatorin is significantly more active against PDE4B than PDE4A
IR-284
-
dual PDE4/PDE7 inhibitor
L-826,141
-
PDE4-selective inhibitor
luteolin-7-glucoside
-
IC50: 0.043 mM, PDB4, dual inhibition of PDE2 and PDE4
luteolin-7-O-glucoside
-
-
methylisobutylxanthine
-
-
myricetin
-
IC50: 0.0389 mM, PDE4
N-[(5S)-5-[2-(3-fluorophenyl)acetamido]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
N-[2-(5-chloro-2-nitrophenylthio)phenyl]acetamide
10% inhibition at 0.01 mM; 11% inhibition at 0.01 mM; lead compound for Parkinson's disease treatment
N-[3-(1H-imidazol-1-yl)propyl]-2-[cis-4-(3,4-dimethoxyphenyl)-1-oxo-4a,5,8,8a-tetrahydrophthalazin-2(1H)-yl]acetamide
-
-
O-phospho-L-serine
-
PdeA and PdeB show 59% and 73% residual activity, respectively, for 3',5'-cAMP hydrolysis at 5 mM phosphoserine
O-phospho-L-tyrosine
-
PdeA and PdeB show 44% and 52% residual activity, respectively, for 3',5'-cAMP hydrolysis at 5 mM phosphotyrosine
orthovanadate
-
PdeA and PdeB show 26% and 29% residual activity, respectively, for 3',5'-cAMP hydrolysis at 1 mM orthovanadate
patuletin-7-O-glucoside
-
-
PF-04957325
-
a selective PDE8 inhibitor
prunetin
-
IC50: 0.0114 mM, PDE4
quazinone
-
0.1 mM, 26% inhibition, wild-type enzyme
quercetin-3,5,7,3',4'-O-pentaacetate
-
-
quercetin-3,5,7,3',4'-O-pentamethylether
-
-
quercetin-3,7,4'-O-trimethylether
-
ayanin
quercetin-3-O-methyl-5,7,3',4'-O-tetraacetate
-
-
quercetin-3-O-methylether
-
-
quinazolinamine
-
IC50: 0.34 mM, PDE4
Ro-20-1724
-
inhibition of PDE4, resulting in increased intacelular cAMP
RP-73401
-
IC50: 0.0000016 mM, PDE4
RS-25344
-
phosphorylation of PDE-4D3 increases the sensitivity of the enzyme to inhibition by RS-25344 about 100fold
RS-33793
-
phosphorylation of PDE-4D3 increases the sensitivity of the enzyme to inhibition by RS-33793 about 330fold
XAP2
-
noncompetitive inhibition, aryl-hydrocarbon receptor-interacting protein XAP2 inhibits PDE4A5 activity by XAP2 does not require any intermediate proteins. XAP2 inhibits PDE4A5 and not other PDE4 isoforms
-
Zl-n-91
-
selective PDE4 inhibitor, Zl-n-91 at 0.03, 0.3 or 3 mg/kg dose dependently inhibits PDE4 activity
3-isobutyl-1-methyl-xanthine
-
-
3-isobutyl-1-methyl-xanthine
-
-
3-isobutyl-1-methyl-xanthine
-
3-isobutyl-1-methylxanthine
-
IC50: 0.007 mM, PDE7
3-isobutyl-1-methylxanthine
-
the inhibitor binds to a subpocket that comprises key residues Ile336, Phe340, Gln369 and Phe372 of PDE54D2. This subpocket may be a common site for binding nonselective inhibitors
3-isobutyl-1-methylxanthine
-
-
3-isobutyl-1-methylxanthine
-
3-isobutyl-1-methylxanthine
nonselective inhibitor, the PDE8A1 catalytic domain is insensitive to 3-isobutyl-1-methylxanthine inhibition
3-isobutyl-1-methylxanthine
-
3-isobutyl-1-methylxanthine
-
-
3-isobutyl-1-methylxanthine
-
-
3-isobutyl-1-methylxanthine
-
3-isobutyl-1-methylxanthine
-
3-isobutyl-1-methylxanthine
-
4-(3-Butoxy-4-methoxybenzyl)-2-imidazolidinone
-
Ro20-1724
4-(3-Butoxy-4-methoxybenzyl)-2-imidazolidinone
-
Ro-20-1724
Caffeine
-
-
Caffeine
-
50 mM, 30% inhibition of soluble enzyme
carboxyamidotriazole
-
non-selective inhibition
carboxyamidotriazole
-
non-selective inhibition
cilomilast
-
Cilostamide
-
IC50: 0.022 mM, PDE7; IC50: 0.0888 mM, PDE4
Cilostamide
-
inhibitor of isoform PDE3
Cilostamide
-
IC50: 0.099 mM, PDE4
dipyridamole
-
-
dipyridamole
-
inhibits PDE8 at high concentrations
dipyridamole
-
IC50: 0.013 mM
EDTA
-
0.3 mM, more than 95% inhibition
EDTA
-
PdeA and PdeB show 39% residual activity, respectively, for 3',5'-cAMP hydrolysis at 0.1 mM EDTA
erythro-9-(2-hydroxy-3-nonyl)adenine
-
7.4% inhibition at 0.1 mM
erythro-9-(2-hydroxy-3-nonyl)adenine
-
a PDE2 selective inhibitor
erythro-9-(2-hydroxy-3-nonyl)adenine
i.e. EHNA
etazolate
-
etazolate
-
IC50: 0.025 mM
IC86340
-
-
-
isobutylmethylxanthine
0.1 mM, 14% inhibition; 0.1 mM, 32% inhibition
isobutylmethylxanthine
-
a non-specific PDE inhibitor
luteolin
-
IC50: 0.0191 mM, PDE4
Milrinone
-
IC50: 0.0175 mM, PDE4; IC50: 0.0583 mM, PDE7
Milrinone
-
42% inhibition at 0.1 mM
Milrinone
0.1 mM, 93% inhibition
papaverine
-
inhibitor of isoform PDE10
papaverine
-
IC50: 0.03 mM
quercetin
-
IC50: 0.0099 mM, PDE4
Ro 20-1724
0.1 mM, 12% inhibition; 0.1 mM, 4% inhibition
Ro 20-1724
-
selective PDE4 inhibitor
Ro20-1724
-
roflumilast
-
roflumilast is approximately 10fold more potent than rolipram
roflumilast
-
PDE4-selective inhibitor
rolipram
-
IC50: 0.00045 mM, PDE4
rolipram
-
inhibitor of isoform PDE4
rolipram
-
18% inhibition at 0.1 mM
rolipram
-
inhibition of PDE4, resulting in increased intacelular cAMP
rolipram
-
competitive inhibitor of the cytosol enzyme but as a partial competitive inhibitor of the particulate enzyme. Particulate PDE-46 shows a 60fold higher affinity for rolipram than cytosolic PDE-46
rolipram
-
specific PDE4 inhibitor, complete inhibition at 0.01 mM rolipram
rolipram
-
PDE4 inhibition by rolipram can promote regression of malignant brain tumors when administered as an adjunct to established therapies
rolipram
PDE4 is specifically inhibited by rolipram; PDE4 is specifically inhibited by rolipram; PDE4 is specifically inhibited by rolipram; PDE4 is specifically inhibited by rolipram
rolipram
-
a selective inhibitor of PDE4
rolipram
0.1 mM, 4% inhibition; 0.1 mM, 7% inhibition
rolipram
-
isozyme PDE4A is only partially inhibited by 0.02 mM rolipram, whereas PDE4B is completely inhibited at this concentration
rolipram
-
PDE4 inhibitor
rolipram
-
PDE4-selective inhibitor
rolipram
-
PDE4 inhibitor
rolipram
-
the inhibitor affects memory retention in a visible/hidden-platform water maze task. This memory impairment can be correlated to the decrease of cAMP nucleotide, due to the induction of a PDE4D cAMP-specific PDE isoform
rolipram
i.e. 4-[3-(cyclopentoxyl)-4-methoxyphenyl]-2-pyrrolidinone
rolipram
-
rolipram at 0.3 mg/kg inhibits the activity of PDE4
rolipram
-
Ro 20-1724, a PDE4 selective inhibitor
SB 207499
-
SCH 351591
-
SCH51866
-
-
sildenafil
-
IC50: 3190 nM, PDE4
sildenafil
-
0.1 mM, 29% inhibition, wild-type enzyme
sildenafil
-
IC50: 0.001 mM
tadalafil
-
IC50: above 10000 nM, PDE4
theophylline
weak inhibitor
theophylline
-
non-selective inhibitor of phosphodiesterases
trequinsin
-
IC50: 0.0025 mM
vardenafil
-
IC50: 2055 nM, PDE4; IC50: 4600 nM, PDE4
vardenafil
-
PDE5 inhibitor
vinpocetine
-
inhibitor of activated isoform PDE4
vinpocetine
-
0.1 mM, 34% inhibition
zaprinast
-
10% inhibition at 0.05 mM
zaprinast
0.1 mM, 67% inhibition; 0.1 mM, 72% inhibition
zardaverine
weak inhibitor
Zn2+
-
more than 90% inhibition at 0.05 mM Zn2+ in the presence of 0.1 mM EDTA, inhibition can be greatly relieved with EDTA at 0.30 mM
Zn2+
-
the 3',5'-phosphodiesterase enzyme activities of PdeA and PdeB are reduced to 24% and 28%, respectively, by 0.05 mM Zn2+ at pH 8.0 in 50 mM Tris-HCl buffer
additional information
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the major enzyme activity (isoform PDE8) is insensitive towards 3-isobutyl-methylxanthine
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not inhibited by quercetin-3,7,3',4'-O-tetramethylether
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IC 50 for sildenafil and tadalafil is above 10000 nM, PDE7; IC50 for sildenafil is above 100000 nM and IC50 for tadalafil and vardenafil is above 10000 nM, PDE8
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treatment with oxidant t-butylhydroperoxide results in release of significant amounts of interleukin-8, which is prevented by inhibition of enzyme isoforms PDE1 and PDE4
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the enzyme is insensitive (up to 100 mM) to a variety of PDE inhibitors including rolipram, zaprinast, vinpocetine, SKF-94120, and IBMX
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the enzyme is insensitive (up to 100 mM) to a variety of PDE inhibitors including rolipram, zaprinast, vinpocetine, SKF-94120, and IBMX
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EHNA, milrinone, rolipram, and zaprinast, which are PDE2, PDE3, and PDE4 inhibitors, respectively, do not inhibit the PDE7B activity up to concentrations of 0.100 mM
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zaprinast, rolipram, and milrinone do not significantly inhibit PDE7B
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zaprinast, rolipram, and milrinone do not significantly inhibit PDE7B
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no inhibition by siguazodan or zaprinast
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no inhibition by siguazodan or zaprinast
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not affected by Ca2+, Fe2+, Mn2+, HSCH2CH2OH, methanol, and dimethylsulfoxide
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not inhibited by alpha-bisabolol, caffeic acid, ferulic acid, quinic acid, rutin, chlorogenic acid, herniarin, and umbelliferone
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the oxidant t-butylhydroperoxide signifcantly increases the cytosolic calcium concentration. Inhibition of both isoforms PDE1 and PDE4 completely prevent the t-butylhydroperoxide stimulated TNF-alpha release
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zaprinast, rolipram, and milrinone do not significantly inhibit PDE7B
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zaprinast, rolipram, and milrinone do not significantly inhibit PDE7B
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unlike other cAMP-specific PDEs, PDE8s are insensitive to a common nonselective PDE inhibitor, 3-isobutyl-1-methylxanthine (IBMX), but ca be inhibited by a high concentration of dipyridamole
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he 3',5'-phosphodiesterase activities of PdeA and PdeB are not inhibited by theophylline, 3-isobuthyl-1-methylxanthine, and beta-glycerophosphate
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removal of the last 35 amino acids of an N-terminal 80-residue highly conserved region (UCR2) results in a 6fold increase in PDE activity, providing evidence that this part of the molecule acts as an intramolecular inhibitor
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not inhibited by cilostamide
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not inhibitory: 3-isobutyl-1-methylxanthine, papaverine, theophylline; TcrPDEA1 is resistant to the typical phosphodiesterase inhibitors, such as IBMX, papaverine and theophylline
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not inhibitory: 3-isobutyl-1-methylxanthine, papaverine, theophylline; TcrPDEA1 is resistant to the typical phosphodiesterase inhibitors, such as IBMX, papaverine and theophylline
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