3.1.4.17 (-)-6-(3-(3-cyclopropyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone IC50: 0.0001 mM, PDE3A; IC50: 0.00028 mM, PDE3B 8657 3.1.4.17 (2R,3R)-3-(6-amino-9H-purin-9-yl)nonan-2-ol IC50: 0.0043 mM, PDE2 24063 3.1.4.17 (2S,3R)-3-(7-amino-3H-imidazo[4,5-b]pyridin-3-yl)nonan-2-ol - 83466 3.1.4.17 (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: 0.000006 mM, PDE3; IC50: 0.0012 mM, PDE2; IC50: 0.015 mM, PDE1 7669 3.1.4.17 (6aS,9aR)-3-benzyl-2-(biphenyl-4-ylmethyl)-5-methyl-5,6a,7,8,9,9a-hexahydrocyclopenta[4,5]imidazo[2,1-b]purin-4(3H)-one comparison of inhibitory effect on several recombinant human PDE isoforms. Effective PDE1 inhibitor in cellular context 138232 3.1.4.17 (Rp)-guanosine-3',5'-cyclic-S-(4-bromo-2,3-dioxobutyl)monophosphorothioate time-dependent and irreversible inactivation of PDE3A 71569 3.1.4.17 (S)-N-(2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-(4-(trifluoromethyl)-1H-imidazol-1-yl)-pyrazolo[1,5-a]pyrimidine-3-carboxamide - 230720 3.1.4.17 (S)-N-(2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-6-methyl-5-(4-methyl-1H-1,2,3-triazol-1-yl)-pyrazolo[1,5-a]pyrimidine-3-carboxamide - 230721 3.1.4.17 1-(2-chlorophenyl)-4-methyl-8-[(morpholin-4-yl)methyl][1,2,4]triazolo[4,3-a]quinoxaline compound shows good combined potency, acceptable brain uptake and high selectivity for both PDE2 and PDE10 enzymes. In microdosing experiment in rats, the compound shows preferential distribution in brain areas 230467 3.1.4.17 1-(2-methylbenzyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione - 24659 3.1.4.17 1-(2-methylbenzyl)-7-(2-oxopropyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione - 24664 3.1.4.17 1-(3-chlorobenzyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione - 24657 3.1.4.17 1-(3-chlorobenzyl)-7-(2-oxopropyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione - 24662 3.1.4.17 1-(3-methylbenzyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione - 24660 3.1.4.17 1-(4-chlorobenzyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione - 24658 3.1.4.17 1-(4-chlorobenzyl)-7-(2-oxopropyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione - 24663 3.1.4.17 1-(4-methylbenzyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione - 24661 3.1.4.17 1-(4-methylbenzyl)-7-(2-oxopropyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione - 24665 3.1.4.17 1-benzyl-7-(2-oxopropyl)-3-propyl-3,7-dihydro-1H-purine-2,6-dione - 24666 3.1.4.17 2-cyclohexyl-2-methyl-N1-[3-(2-oxo-1,2-dihydro-6-quinolyl,oxy)propyl]-1-hydrazinecarboxamide IC50: 0.00000034 mM, PDE3A, highly selective PDE3 inhibitor; IC50: 0.0000019 mM, PDE3B; IC50: 0.0.0209 mM, PDE2; IC50: 0.1129 mM, PDE1 4966 3.1.4.17 2-[1-(2,4-dichlorobenzyl)-2-methyl-5-(methylmercapto)-1H-indol-3-yl] ethanaminium chloride IC50: 0.005 mM, PDE1; IC50: 0.037 mM, PDE2 232730 3.1.4.17 2-[[4-[4-pyridin-4-yl-1-(2,2, 2-trifluoroethyl)pyrazol-3-yl]phenoxy]methyl]quinoline succinic acid potent inhibitor 38301 3.1.4.17 2-[[4-[4-pyridin-4-yl-1-(2,2, 2-trifluoroethyl)pyrazol-3-yl]phenoxy]methyl]quinoline succinic acid selective PDE10A inhibitor, inhibition of striatal PDE10A activity increases the responsiveness of medium-sized spiny projection neurons to depolarising stimuli 38301 3.1.4.17 3',5'-cGMP - 1633 3.1.4.17 3'-benzyl-2'-(biphenyl-4-ylmethyl)-5'-methyl-3'H-spiro[cyclopentane-1,7'-imidazo[2,1-b]purin]-4'(5'H)-one comparison of inhibitory effect on several recombinant human PDE isoforms. Effective PDE1 inhibitor in cellular context 138231 3.1.4.17 3-isobutyl-1-methyl-1H-purine-2,6(3H,7H)-dione IC50: 0.0402 mM 13943 3.1.4.17 3-isobutyl-1-methyl-1H-purine-2,6(3H,7H)-dione IC50: 0.068 mM 13943 3.1.4.17 3-isobutyl-1-methyl-1H-purine-2,6(3H,7H)-dione IC50: 0.02654 mM, PDE4A4 13943 3.1.4.17 3-isobutyl-1-methylxanthine - 1157 3.1.4.17 3-isobutyl-1-methylxanthine marked differences in inhibition for isozymes 1157 3.1.4.17 3-isobutyl-1-methylxanthine broad-spectrum PDE inhibitor; broad-spectrum PDE inhibitor; broad-spectrum PDE inhibitor 1157 3.1.4.17 3-isobutyl-8-(methoxymethyl)-1-methyl-3,9-dihydro-1H-purine-2,6-dione i.e. 8MM-IBMX, comparison of inhibitory effect on several recombinant human PDE isoforms 138229 3.1.4.17 4-(3-Butoxy-4-methoxybenzyl)-2-imidazolidinone Ro20-1724 15544 3.1.4.17 5-(1-(difluoromethyl)-1H-pyrazol-4-yl)-N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)phenyl)propyl)-pyrazolo[1,5-a]pyrimidine-3-carboxamide - 231516 3.1.4.17 5-(2-propoxyphenyl)-2,3-dihydro-7H-[1,2,3]triazolo[4,5-d]pyrimidin-7-one - 24062 3.1.4.17 5-(3-cyclopentyloxy-4-methoxy-phenyl)-pyrrolidin-2-one 50% inhibition at about 0.1 mM 117585 3.1.4.17 5-methyl-2-[4-(trifluoromethyl)benzyl]-5,6a,7,8,9,9a-hexahydrocyclopenta[4,5]imidazo[2,1-b]purin-4(1H)-one i.e. SCH51866, comparison of inhibitory effect on several recombinant human PDE isoforms. Effective PDE1 inhibitor in cellular context 138230 3.1.4.17 6-(3-(3-cyclooctyl-3-((1R,2R)-2-hydroxycyclohexyl)ureido)-propoxy)-2(1H)-quinolinone IC50: 0.00000032 mM, PDE3A, highly selective PDE3 inhibitor; IC50: 0.0000015 mM, PDE3B; IC50: 0.0429 mM, PDE1; IC50: 0.0523 mM, PDE2 5003 3.1.4.17 6-methyl-N-[(1R)-1-[4-(trifluoromethoxy)phenyl]propyl]pyrazolo[1,5-a]pyrimidine-3-carboxamide - 231663 3.1.4.17 8-hydroxyquinoline 2 mM, 28% residual activity 321 3.1.4.17 8-methoxymethyl(-3-isobutyl-1-)methylxanthine - 47785 3.1.4.17 8-methoxymethyl-3-isobutyl-1-methylxanthine - 33701 3.1.4.17 8-methoxymethyl-3-isobutyl-1-methylxanthine 0.02 mM selectively inhibits PDE1; 0.02 mM selectively inhibits PDE1 33701 3.1.4.17 8-methoxymethyl-isobutylmethylxanthine inhibits activated PDE1 and PDE2 isoforms as well as PDE4 and PDE5, is 3times more potent in inhibiting PDE5 than PDE1 15113 3.1.4.17 adenine at 2.5 mM, strong 144 3.1.4.17 adenosine at 2.5 mM, strong 122 3.1.4.17 adenosine - 122 3.1.4.17 ADP at 2.5 mM, strong 13 3.1.4.17 ADP 1 mM, 56% residual activity 13 3.1.4.17 Al3+ strongly inhibitory at 2.5 mM 264 3.1.4.17 Al3+ - 264 3.1.4.17 Al3+ at 2.5 mM 264 3.1.4.17 amantadine brain 60 kDa isozyme 16839 3.1.4.17 AMP at 2.5 mM, strong 30 3.1.4.17 AMP 1 mM, 15% residual activity 30 3.1.4.17 amrinone IC50: 0.0167 mM, PDE3A; IC50: 0.0312 mM, PDE3B 13050 3.1.4.17 angiotensin III - 2543 3.1.4.17 apigenin IC50: 0.0105 mM, PDB3; IC50: 0.0167 mM, PDB2; IC50: 0.0254 mM, PDB1 515 3.1.4.17 ATP at 2.5 mM, strong 4 3.1.4.17 ATP 1 mM, 46% residual activity 4 3.1.4.17 Ba2+ - 111 3.1.4.17 BAY 60-7550 - 36986 3.1.4.17 BAY 60-7550 PDE2 inhibitor 36986 3.1.4.17 BAY60-7550 inhibition of isoform PDE2, results in increase in basal cGMP levels after application to thalamic neurons 138815 3.1.4.17 Biochanin A IC50: 0.0279 mM, PDE2; IC50: 0.0291 mM, PDE1 1435 3.1.4.17 Ca2+ micromolar concentrations 15 3.1.4.17 Ca2+ - 15 3.1.4.17 Ca2+ 2 mM, 69% residual activity 15 3.1.4.17 Caffeine noncompetitive, dog heart 882 3.1.4.17 Caffeine - 882 3.1.4.17 Calmidazolium soluble but not particulate form 3621 3.1.4.17 cAMP particulate enzyme 268 3.1.4.17 cAMP - 268 3.1.4.17 cAMP IC50: 1200 nM, PDE11A4 268 3.1.4.17 cGMP - 342 3.1.4.17 cGMP IC50: 0.000075 mM, PDE3A; IC50: 0.00032 mM, PDE3B 342 3.1.4.17 cGMP IC50: 560 nM, PDE11A4 342 3.1.4.17 cGMP competitive inhibitor of PDE3A acting directly at the catalytic site 342 3.1.4.17 cGMP the hydrolysis of cGMP by PDE3 inhibits the hydrolysis of cAMP 342 3.1.4.17 Chloropromazine soluble but not particulate form 6497 3.1.4.17 Cilostamide - 2477 3.1.4.17 Cilostamide 50 mM, inhibits growth of acinar epithelial cells by 63% 2477 3.1.4.17 Cilostamide IC50: 0.000027 mM, PDE3A; IC50: 0.00005 mM, PDE3B; IC50: 0.0125 mM, PDE2 2477 3.1.4.17 Cilostamide IC50: 0.00013 mM, PDE3; IC50: 0.048 mM, PDE2; IC50: 0.221 mM, PDE1 2477 3.1.4.17 cilostazol IC50: 0.0002 mM, PDE3A; IC50: 0.00038 mM, PDE3B; IC50: 0.0452 mM, PDE2 4160 3.1.4.17 cilostazol - 4160 3.1.4.17 cilostazol a PDE3 inhibitor 4160 3.1.4.17 Co2+ inhibits at concentrations higher than optimal 23 3.1.4.17 Co2+ inhibits at higher concentrations 23 3.1.4.17 Co2+ - 23 3.1.4.17 Co2+ PdeA and PdeB are inhibited (20-30%) at 0.25 mM Co2+ 23 3.1.4.17 cortisol - 919 3.1.4.17 Cu2+ - 19 3.1.4.17 Cu2+ 2 mM, 27% residual activity 19 3.1.4.17 daidzein IC50: 0.0286 mM, PDE3 848 3.1.4.17 dibutyryl cyclic AMP 94% inhibition at 2.5 mM 29934 3.1.4.17 dibutyryl cyclic AMP - 29934 3.1.4.17 dioclein potent selective and calmodulin-independent inhibitor of PDE1, competitive inhibitor for cGMP hydrolysis by PDE1 in basal-activated (1 mM EGTA) and calmodulin-activated (18 nM calmodulin with 0.01 mM CaCl2) states. Dioclein is at least 11times more potent in inhibiting calmodulin-activated PDE1 than other PDE types. Among PDE1-PDE5, dioclein is at least 11fold more selective for the activated PDE1 isoform compared to basal PDE2 (70fold), activated PDE2 (26fold), PDE3 (19fold), PDE4 (11fold), and PDE5 (16fold) 4184 3.1.4.17 dioclein dioclein is at least 11times more potent in inhibiting calmodulin-activated PDE1 than other PDE types. Among PDE1-PDE5, dioclein is at least 11fold more selective for the activated PDE1 isoform compared to basal PDE2 (70fold), activated PDE2 (26fold) 4184 3.1.4.17 dioclein - 4184 3.1.4.17 diosmetin IC50: 0.0048 mM, PDB2; IC50: 0.0144 mM, PDB1 4707 3.1.4.17 dipyridamole - 1192 3.1.4.17 dipyridamole 50% inhibition at about 0.0002-0.00055 mM 1192 3.1.4.17 dipyridamole 50% inhibition at 0.00082 mM; 50% inhibition at 0.0018 mM 1192 3.1.4.17 dipyridamole IC50: 0.00078 mM 1192 3.1.4.17 dipyridamole IC50: 0.0069 mM 1192 3.1.4.17 dipyridamole IC50: 840 nM, PDE11A4 1192 3.1.4.17 dipyridamole IC50: 0.00034 mM, PDE4A4 1192 3.1.4.17 dipyridamole inhibits with micromolar potency 1192 3.1.4.17 dipyridamole 1 mM, 71% residual activity 1192 3.1.4.17 E4021 50% inhibition at about 0.0005-0.001 mM 7548 3.1.4.17 EDTA complete loss of activity for mutants H23A, H169A, H207A 21 3.1.4.17 EDTA PdeA and PdeB show 39% relative activity in the hydrolysis of 3',5'-cAMP in the presence of 0.05 mM EDTA 21 3.1.4.17 EDTA 2 mM, 44% residual activity 21 3.1.4.17 EHNA a selective PDE2 inhibitor 37320 3.1.4.17 eriodictyol IC50: 0.0525 mM, PDB3 2485 3.1.4.17 erythro-9-(2-hydroxy-3-nonyl)-adenine IC50: 0.0092 mM, PDE2 11514 3.1.4.17 erythro-9-(2-hydroxy-3-nonyl)adenine 50% inhibition at about 0.1 mM 2020 3.1.4.17 erythro-9-(2-hydroxy-3-nonyl)adenine IC50: 0.00061 mM for wild-type enzyme 2020 3.1.4.17 erythro-9-(2-hydroxy-3-nonyl)adenine inhibition of isoform PDE2, results in increase in basal cGMP levels after application to thalamic neurons 2020 3.1.4.17 etazolate IC50: 0.0007 mM 5805 3.1.4.17 ethylene glycol bis(beta-aminoethyl ether)-N,N'-tetraacetic acid soluble but not particulate form 44119 3.1.4.17 FAD - 20 3.1.4.17 Fe2+ strongly inhibitory at 2.5 mM 25 3.1.4.17 Fe2+ - 25 3.1.4.17 Fe2+ at 2.5 mM 25 3.1.4.17 Fe2+ strong inhibition at 1 mM 25 3.1.4.17 Fe3+ strongly inhibitory at 2.5 mM 70 3.1.4.17 Fe3+ - 70 3.1.4.17 Fe3+ at 2.5 mM 70 3.1.4.17 felodipine - 53907 3.1.4.17 GDP 1 mM, 41% residual activity 53 3.1.4.17 genistein IC50: 0.0017 mM, PDB2; IC50: 0.0129 mM, PDB3; IC50: 0.0168 mM, PDB1 377 3.1.4.17 GMP 1 mM, 31% residual activity 162 3.1.4.17 GTP 1 mM, 44% residual activity 37 3.1.4.17 IBMX - 6114 3.1.4.17 isobutylmethylxanthine 50% inhibition at about 0.05 mM 7213 3.1.4.17 isobutylmethylxanthine inhibits with micromolar potency 7213 3.1.4.17 linoleic acid - 428 3.1.4.17 luteolin IC50: 0.0101 mM, PDB3; IC50: 0.0133 mM, PDB2; IC50: 0.0215 mM, PDB1 436 3.1.4.17 luteolin-7-glucoside IC50: 0.0351 mM, PDB2 12809 3.1.4.17 methylxanthines - 103046 3.1.4.17 Mg2+ inhibits at concentrations higher than optimal 6 3.1.4.17 Mg2+ inhibits at higher amounts 6 3.1.4.17 Milrinone 0.2627 mM, PDE1; IC50: 0.0001 mM, PDE3B; IC50: 0.00045 mM, PDE3A 3352 3.1.4.17 Milrinone 50% inhibition at about 0.1 mM 3352 3.1.4.17 Milrinone - 3352 3.1.4.17 Mn2+ inhibits at concentrations higher than optimal 11 3.1.4.17 Mn2+ - 11 3.1.4.17 Mn2+ PdeA and PdeB are inhibited (20-30%) at 0.25 mM Mn2+ 11 3.1.4.17 additional information inhibition by monoclonal antibodies 2 3.1.4.17 additional information - 2 3.1.4.17 additional information not inhibitory: EDTA up to 2.5 mM 2 3.1.4.17 additional information IC50 for vardenafil, sildenafil and tadalafil is above 10000 nM, PDE2 2 3.1.4.17 additional information 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 2 3.1.4.17 additional information the oxidant t-butylhydroperoxide signifcantly increases the cytosolic calcium concentration, which is prevented by inhibition of enzyme isoform PDE1. Inhibition of both isoforms PDE1 and PDE4 completely prevent the t-butylhydroperoxide stimulated TNF-alpha release 2 3.1.4.17 additional information NAD+ is not an inhibitor of PDE3A 2 3.1.4.17 additional information not inhibited by rolipram and sildenafil 2 3.1.4.17 additional information PdeA and PdeB are not stimulated by 3-isobuthyl-1-methylxanthine, theophylline, beta-glycerophosphate, Ca2+, Mg2+, Fe2+, and Fe3+ 2 3.1.4.17 additional information the broad-spectrum phosphodiesterase inhibitor 3-isobutyl-1-methylxanthine, IBMX, has no effect on the activity of PdeE at 1 mM. No inhibition by theophylline at 1 mM, beta-glycerophosphate at 0.1 mM, and by orthovanadate 2 3.1.4.17 MP-10 - 147236 3.1.4.17 myricetin IC50: 0.0124 mM, PDB3; IC50: 0.0128 mM, PDB2; IC50: 0.0249 mM, PDB1 484 3.1.4.17 N-((1S)-1-(3-fluoro-4-(trifluoromethoxy)phenyl)-2-methoxyethyl)-7-methoxy-2-oxo-2,3-dihydropyrido[2,3-b]pyrazine-4(1H)-carboxamide TAK-915 231918 3.1.4.17 N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-(1H-pyrazol-1-yl)pyrazolo[1,5-a]pyrimidine-3-carboxamide - 231919 3.1.4.17 N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-(2-methylpyridin-4-yl)pyrazolo[1,5-a]-pyrimidine-3-carboxamide - 231920 3.1.4.17 N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-(3-methyl-1H-1,2,4-triazol-1-yl)pyrazolo-[1,5-a]pyrimidine-3-carboxamide - 231921 3.1.4.17 N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-(4-methyl-1H-1,2,3-triazol-1-yl)pyrazolo-[1,5-a]pyrimidine-3-carboxamide - 231922 3.1.4.17 N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-(4-methyl-1H-imidazol-1-yl)pyrazolo [1,5-a]pyrimidine-3-carboxamide - 231923 3.1.4.17 N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-(6-methylpyridin-3-yl)pyrazolo[1,5-a]-pyrimidine-3-carboxamide - 231924 3.1.4.17 N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-(pyridin-2-yl)pyrazolo[1,5-a]pyrimidine-3-carboxamide - 231925 3.1.4.17 N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-(tetrahydro-2H-pyran-4-yl)pyrazolo[1,5-a]-pyrimidine-3-carboxamide - 231926 3.1.4.17 N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)-phenyl)propyl)-5-isopropylpyrazolo[1,5-a]pyrimidine-3-carboxamide - 231927 3.1.4.17 N-((1S)-2-hydroxy-2-methyl-1-(4-(trifluoromethoxy)phenyl)propyl)-6-methyl-5-(3-methyl-1H-1,2,4-triazol-1-yl)pyrazolo[1,5-a]pyrimidine-3-carboxamide - 231928 3.1.4.17 N-(6-Aminohexyl)-5-chloro-1-naphthalenesulfonamide soluble but not particulate form 6558 3.1.4.17 N-[(1S)-2-hydroxy-2-methyl-1-[4-(trifluoromethoxy)phenyl]propyl]-6-methylpyrazolo[1,5-a]pyrimidine-3-carboxamide - 232068 3.1.4.17 N-[(1S)-2-hydroxy-2-methyl-1-[4-(trifluoromethoxy)phenyl]propyl]pyrazolo[1,5-a]pyrimidine-3-carboxamide - 232069 3.1.4.17 N-[1-(4-methoxyphenyl)propyl]pyrazolo[1,5-a]pyrimidine-3-carboxamide - 232084 3.1.4.17 N-[1-[3-fluoro-4-(trifluoromethoxy)phenyl]-2-hydroxy-2-methylpropyl]-2-oxo-2,3-dihydropyrido[2,3-b]pyrazine-4(1H)-carboxamide - 232085 3.1.4.17 N-[1-[4-(trifluoromethoxy)phenyl]propyl]pyrazolo[1,5-a]pyrimidine-3-carboxamide - 232086 3.1.4.17 NAD+ - 7 3.1.4.17 NADH 1 mM, 76% residual activity 8 3.1.4.17 NADP+ - 10 3.1.4.17 NADPH 1 mM, 25% residual activity 5 3.1.4.17 NaF 1 mM, 79% residual activity 235 3.1.4.17 Ni2+ - 38 3.1.4.17 nicardipine weak inhibitor 9371 3.1.4.17 nicardipine - 9371 3.1.4.17 nimodipine - 7349 3.1.4.17 orthovanadate PdeA shows 26% relative activity and PdeB shows 29% relative activity in the hydrolysis of 3',5'-cAMP in the presence of 0.05 mM orthovanadate 1328 3.1.4.17 papaverine - 1540 3.1.4.17 papaverine IC50: 0.025 mM 1540 3.1.4.17 papaverine competitive inhibitor 1540 3.1.4.17 papaverine selective PDE10A inhibitor 1540 3.1.4.17 Pb2+ at 2.5 mM 139 3.1.4.17 phosphate PdeA and PdeB enzyme activities are strongly inhibited by 0.1 M sodium phosphate buffer (pH 6.0 and 7.0), the PdeB activity is more strongly inhibited by 0.1 M phosphate than is PdeA activity 16 3.1.4.17 phosphoserine PdeA shows 59% relative activity and PdeB shows 73% relative activity in the hydrolysis of 3',5'-cAMP in the presence of 0.05 mM phosphoserine 9243 3.1.4.17 phosphotyrosine PdeA shows 44% relative activity and PdeB shows 52% relative activity in the hydrolysis of 3',5'-cAMP in the presence of 0.05 mM phosphotyrosine 2579 3.1.4.17 PQ-10 - 147235 3.1.4.17 quercetin IC50: 0.0056 mM, PDB3; IC50: 0.0179 mM, PDB2; IC50: 0.0278 mM, PDB1 137 3.1.4.17 quercetin - 137 3.1.4.17 quercetin-3,5,7,3',4'-O-pentaacetate - 25914 3.1.4.17 quercetin-3,5,7,3',4'-O-pentamethylether - 14444 3.1.4.17 quercetin-3,7,3',4'-O-tetramethylether - 71568 3.1.4.17 quercetin-3,7,4'-O-trimethylether ayanin 25915 3.1.4.17 quercetin-3-O-methyl-5,7,3',4'-O-tetraacetate - 14445 3.1.4.17 quercetin-3-O-methylether - 11932 3.1.4.17 quinazolinamine IC50: 0.01 mM, PDE3; IC50: 0.23 mM, PDE1; IC50: 0.241 mM, PDE2 7670 3.1.4.17 rolipram - 757 3.1.4.17 rolipram weak inhibitor 757 3.1.4.17 rolipram IC50: 0.15 mM for wild-type enzyme 757 3.1.4.17 RP-73401 IC50: 0.05 mM, PDE3; IC50: 0.067 mM, PDE2; IC50: 0.13 mM, PDE1 7549 3.1.4.17 sarilesin - 117586 3.1.4.17 sildenafil IC50: IC50: 0.00012 mM, PDE11; IC50: IC50: 0.0013 mM, PDE1 615 3.1.4.17 sildenafil IC50: 1725 nM, PDE11; IC50: 350 nM, PDE1 615 3.1.4.17 sildenafil IC50: 3800 nM, 1000fold selectivity for PDE5A1 compared to PDE11A4. This drug (PDE5 inhibitor in treatment of erectile dysfunction) is very unlikely to crossreact with PDE11A4 in patients taking the prescribed dosage of this medication 615 3.1.4.17 sildenafil IC50: 0.00315 mM, PDE4A4 615 3.1.4.17 sildenafil - 615 3.1.4.17 sildenafil viagra, potent selective PDE5 inhibitor 615 3.1.4.17 SKF 94120 weak inhibitor 103647 3.1.4.17 tadalafil IC50: 67 nM, PDE11; IC50: above 10000 nM, PDE1 1339 3.1.4.17 tadalafil partially inhibits PDE11 1339 3.1.4.17 tadalafil PDE11 inhibition has impacts on sperm quality. Reasonable caution should by suggested in patients taking the prescribed dosages of tadalafil, a PDE5 inhibitor which could crossreact with human PDE11A splicing variants 1339 3.1.4.17 tadalafil IC50: 73 nM, 40fold selectivity for PDE5A1 compared to PDE11A4. This drug (PDE5 inhibitor in treatment of erectile dysfunction) is very unlikely to crossreact with PDE11A4 in patients taking the prescribed dosage of this medication 1339 3.1.4.17 tadalafil - 1339 3.1.4.17 TAK-915 i.e. 2 N-((1S)-1-(3-fluoro-4-(trifluoromethoxy)phenyl)-2-methoxyethyl)-7-methoxy-2-oxo-2,3-dihydropyrido[2,3-b]pyrazine-4(1H)-carboxamide 232752 3.1.4.17 theophylline - 1221 3.1.4.17 theophylline 1 mM, 70% residual activity 1221 3.1.4.17 TP-10 - 147237 3.1.4.17 trequinsin IC50: 0.0039 mM 11346 3.1.4.17 Trifluoperazine - 977 3.1.4.17 vardenafil IC50: 121 nM, PDE1; IC50: 308 nM, PDE11 1227 3.1.4.17 vardenafil IC50: 840 nM, 9300fold selectivity for PDE5A1 compared to PDE11A4. This drug (PDE5 inhibitor in treatment of erectile dysfunction) is very unlikely to crossreact with PDE11A4 in patients taking the prescribed dosage of this medication 1227 3.1.4.17 vardenafil - 1227 3.1.4.17 vinpocetine - 3865 3.1.4.17 vinpocetine IC50: 0.0232 mM, PDE1 3865 3.1.4.17 vinpocetine 50% inhibition at about 0.06-0.09 mM 3865 3.1.4.17 vinpocetine IC50: 0.0223 3865 3.1.4.17 vinpocetine comparison of inhibitory effect on several recombinant human PDE isoforms 3865 3.1.4.17 vinpocetine inhibitor of activated PDE1 3865 3.1.4.17 zaprinast - 1223 3.1.4.17 zaprinast weak inhibitor 1223 3.1.4.17 zaprinast 50% inhibition at about 0.016-0.02 mM 1223 3.1.4.17 zaprinast 50% inhibition at 0.005 mM; 50% inhibition at 0.028 mM 1223 3.1.4.17 zaprinast IC50: 0.0016 mM, PDE11; IC50: 0.071 mM, PDE1 1223 3.1.4.17 zaprinast IC50: 0.00816 mM, PDE4A4 1223 3.1.4.17 Zn2+ strongly inhibitory at 2.5 mM 14 3.1.4.17 Zn2+ - 14 3.1.4.17 Zn2+ at 2.5 mM 14 3.1.4.17 Zn2+ PdeA and PdeB are potently inhibited in the hydrolysis of 3',5'-cAMP by 0.05 mM Zn2+ with 24% and 28% of remaining activity 14 3.1.4.17 Zn2+ strong inhibition at 1 mM 14