Page last updated: 2024-09-04

cilomilast and roflumilast

cilomilast has been researched along with roflumilast in 39 studies

Compound Research Comparison

Studies
(cilomilast)
Trials
(cilomilast)
Recent Studies (post-2010)
(cilomilast)
Studies
(roflumilast)
Trials
(roflumilast)
Recent Studies (post-2010) (roflumilast)
162134256690425

Protein Interaction Comparison

ProteinTaxonomycilomilast (IC50)roflumilast (IC50)
Chain A, cAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)0.0008
Chain A, cAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)0.0008
Chain A, cAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)0.0008
Chain A, cAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)0.0008
Chain A, cAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)0.0008
Chain A, cAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)0.0008
Chain A, cAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)0.0008
Chain A, cAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)0.0008
Chain A, cAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)0.0008
Chain A, cAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)0.0008
Chain A, cAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)0.0008
Chain B, cAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)0.0008
Chain A, cGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)0.0008
Chain A, cGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)0.0008
Chain A, cAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)0.0058
Chain A, cAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)0.0058
Chain A, cAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)0.0058
Chain A, cAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)0.0058
Chain A, cAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)0.0058
Chain A, cAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)0.0058
Chain A, cAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)0.0058
cGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)0.0008
High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8AHomo sapiens (human)0.0008
cGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)0.0008
cAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)0.0005
Sodium-dependent serotonin transporterRattus norvegicus (Norway rat)0.0003
Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)0.0008
cAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)0.025
cAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)0.0008
cAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)0.0475
cGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)0.0008
Beta-2 adrenergic receptorCavia porcellus (domestic guinea pig)0.001
Dual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11AHomo sapiens (human)0.0008
cAMP-specific 3',5'-cyclic phosphodiesterase 7BHomo sapiens (human)0.0008
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10AHomo sapiens (human)0.0008

Research

Studies (39)

TimeframeStudies, this research(%)All Research%
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's18 (46.15)29.6817
2010's16 (41.03)24.3611
2020's5 (12.82)2.80

Authors

AuthorsStudies
Artis, DR; Bollag, G; Card, GL; England, BP; Fong, D; Gillette, S; Ibrahim, PN; Kim, SH; Lee, B; Luu, C; Milburn, MV; Powell, B; Schlessinger, J; Suzuki, Y; Tabrizizad, M; Zhang, KY1
Hughes, RA; Manallack, DT; Thompson, PE1
Barlow, DJ; Ehrman, TM; Hylands, PJ1
Huang, L; Jiang, HL; Lai, KF; Li, XS; Luo, ZH; Shan, WJ; Zhou, Q1
Egerland, U; Gewald, R; Grunwald, C1
Huang, L; Lai, K; Li, X; Shan, W; Xie, J; Zhou, Q1
de Esch, IJ; de Graaf, C; Jansen, C; Kanev, GK; Kooistra, AJ; Leurs, R1
Chen, W; Dong, G; Feng, C; Gu, Z; Li, H; Li, J; Li, M; Liu, H; Tang, W; Xu, Y; Zhang, R; Zhang, X; Zhu, F1
He, J; Ke, H; Peng, T; Qi, B; Shi, J1
Balliano, TL; Barbosa, G; Carvalho, VF; da Silva, BA; de Souza, ET; Lima, LM; Martins, IRR; Martins, MA; Medeiros, MM; Moraes Junior, MO; Nunes, IKDC; Silva, PMR; Silva, SWD1
He, Y; Hou, R; Hou, S; Liao, C; Xie, Z; Yan, G1
Fitzgerald, M; Sturton, G1
Giembycz, MA1
Draheim, R; Egerland, U; Rundfeldt, C1
Dai, YR; Xia, XD; Xu, ZJ1
Vignola, AM1
Banner, KH; Trevethick, MA1
Hanania, NA; Soto, FJ1
Cortijo, J; Morcillo, EJ; Sanz, MJ1
Beume, R; Bundschuh, DS; Marx, D; Wohlsen, A; Wollin, L1
Fan Chung, K1
Abraham, WM; Claveau, D; Dias, R; Dubé, D; Gallant, M; Girard, Y; Goetghebeur, P; Huang, Z; Jones, T; Lacombe, P; Laliberte, F; Liu, S; Macdonald, D; Mancini, JA; Ng, K; Nicholson, DW; Otu, F; Styhler, A; Turner, MJ; Young, RN; Zhang, L1
Chaves, J; Lerner, A; Makkinje, A; Meyers, JA; Taverna, J1
Cui, X; Wang, D1
Harada, D; Ikeda, Y; Kobayashi, K; Manabe, H; Nosaka, Y1
Tatlicioğlu, T1
Ball, D; Barnette, MS; Capper-Spudich, EA; Davis, TG; Ferrari, L; Knowles, RG; Kou, JP; Lucas, FS; Nials, AT; Peterson, JJ; Podolin, PL; Solanke, YE; Williamson, RA; Wiseman, J; Wren, P1
Diamant, Z; Spina, D1
Iwata, M; Kobayashi, M; Kubo, S; Ohtsu, Y; Shimizu, Y; Takahashi, K1
Black, PN; Chong, J; Leung, B; Poole, P1
Hirano, Y; Kobayashi, M; Kobayashi, S; Kubo, S; Shimizu, Y; Takahashi, K1
Iwata, M; Kobayashi, M; Kubo, S; Miyata, K; Shimizu, Y; Takahashi, K1
Krug, O; Schänzer, W; Thevis, M1
Barg, M; Geerts, A; Quednau, R; Tersteegen, A; Wunder, F1
Chong, J; Leung, B; Poole, P2
Goto, T; Maeda, H; Nakamura, S; Suzuki, O; Yoshino, T1
Fortescue, R; Janjua, S; Poole, P1
Aguiar, JA; Ask, K; Cao, Q; Doxey, AC; Hirota, JA; Hou, V; Huff, RD; Inman, MD; Kim, Y; Miller, MS; Revill, S; Tiessen, N1

Reviews

18 review(s) available for cilomilast and roflumilast

ArticleYear
The next generation of phosphodiesterase inhibitors: structural clues to ligand and substrate selectivity of phosphodiesterases.
    Journal of medicinal chemistry, 2005, May-19, Volume: 48, Issue:10

    Topics: Animals; Binding Sites; Crystallography, X-Ray; Cyclic AMP; Cyclic GMP; Drug Design; Humans; Models, Molecular; Molecular Structure; Phosphodiesterase Inhibitors; Quantitative Structure-Activity Relationship; Xanthines

2005
Advances in the Development of Phosphodiesterase-4 Inhibitors.
    Journal of medicinal chemistry, 2020, 10-08, Volume: 63, Issue:19

    Topics: Animals; Cyclic Nucleotide Phosphodiesterases, Type 4; Drug Development; Drug Discovery; Humans; Molecular Structure; Phosphodiesterase 4 Inhibitors; Protein Conformation; Quinolones; Vomiting

2020
Zinc enzymes in medicinal chemistry.
    European journal of medicinal chemistry, 2021, Dec-15, Volume: 226

    Topics: Chemistry, Pharmaceutical; Enzyme Inhibitors; Enzymes; Humans; Models, Molecular; Zinc

2021
Phosphodiesterase 4 inhibitors for the treatment of COPD.
    Chest, 2002, Volume: 121, Issue:5 Suppl

    Topics: Aminopyridines; Animals; Benzamides; Bronchodilator Agents; Carboxylic Acids; Clinical Trials, Phase I as Topic; Clinical Trials, Phase II as Topic; Cyclohexanecarboxylic Acids; Cyclopropanes; Humans; Nitriles; Phosphodiesterase Inhibitors; Pulmonary Disease, Chronic Obstructive

2002
Development status of second generation PDE4 inhibitors for asthma and COPD: the story so far.
    Monaldi archives for chest disease = Archivio Monaldi per le malattie del torace, 2002, Volume: 57, Issue:1

    Topics: Aminopyridines; Asthma; Benzamides; Bronchodilator Agents; Carboxylic Acids; Cyclohexanecarboxylic Acids; Cyclopropanes; Drug Interactions; Humans; Nitriles; Phosphodiesterase Inhibitors; Pulmonary Disease, Chronic Obstructive

2002
[Phosphosdiesterase 4 inhibitors in the treatment of pulmonary diseases].
    Zhonghua jie he he hu xi za zhi = Zhonghua jiehe he huxi zazhi = Chinese journal of tuberculosis and respiratory diseases, 2004, Volume: 27, Issue:1

    Topics: 3',5'-Cyclic-AMP Phosphodiesterases; Aminopyridines; Asthma; Benzamides; Bronchodilator Agents; Carboxylic Acids; Cyclic Nucleotide Phosphodiesterases, Type 4; Cyclohexanecarboxylic Acids; Cyclopropanes; Humans; Lung Diseases; Nitriles; Phosphodiesterase Inhibitors; Pulmonary Disease, Chronic Obstructive; Pyridines

2004
PDE4 inhibitors in COPD--a more selective approach to treatment.
    Respiratory medicine, 2004, Volume: 98, Issue:6

    Topics: 3',5'-Cyclic-AMP Phosphodiesterases; Aminopyridines; Benzamides; Bronchodilator Agents; Carboxylic Acids; Cyclic Nucleotide Phosphodiesterases, Type 4; Cyclohexanecarboxylic Acids; Cyclopropanes; Humans; Nitriles; Phosphodiesterase Inhibitors; Pneumonia; Pulmonary Disease, Chronic Obstructive; Rolipram; Theophylline; Treatment Outcome

2004
PDE4 inhibition: a novel approach for the treatment of inflammatory bowel disease.
    Trends in pharmacological sciences, 2004, Volume: 25, Issue:8

    Topics: 3',5'-Cyclic-AMP Phosphodiesterases; Aminopyridines; Animals; Anti-Inflammatory Agents; Benzamides; Bronchodilator Agents; Carboxylic Acids; Cyclic Nucleotide Phosphodiesterases, Type 4; Cyclohexanecarboxylic Acids; Cyclopropanes; Enzyme Inhibitors; Humans; Inflammatory Bowel Diseases; Nitriles

2004
Selective phosphodiesterase-4 inhibitors in chronic obstructive lung disease.
    Current opinion in pulmonary medicine, 2005, Volume: 11, Issue:2

    Topics: 3',5'-Cyclic-AMP Phosphodiesterases; Amides; Aminopyridines; Benzamides; Carboxylic Acids; Cyclic Nucleotide Phosphodiesterases, Type 4; Cyclohexanecarboxylic Acids; Cyclopropanes; Humans; Indoles; Inflammation; Lung; Nitriles; Nucleotides, Cyclic; Phosphodiesterase Inhibitors; Phosphoric Diester Hydrolases; Pulmonary Disease, Chronic Obstructive

2005
PDE4 inhibitors as new anti-inflammatory drugs: effects on cell trafficking and cell adhesion molecules expression.
    Pharmacology & therapeutics, 2005, Volume: 106, Issue:3

    Topics: 3',5'-Cyclic-AMP Phosphodiesterases; Aminopyridines; Anti-Inflammatory Agents; Benzamides; Carboxylic Acids; Cell Adhesion Molecules; Cell Movement; Cyclic Nucleotide Phosphodiesterases, Type 4; Cyclohexanecarboxylic Acids; Cyclopropanes; Humans; Nitriles; Phosphodiesterase Inhibitors; Pulmonary Disease, Chronic Obstructive

2005
Phosphodiesterase inhibitors in airways disease.
    European journal of pharmacology, 2006, Mar-08, Volume: 533, Issue:1-3

    Topics: 3',5'-Cyclic-AMP Phosphodiesterases; 3',5'-Cyclic-GMP Phosphodiesterases; Aminopyridines; Animals; Anti-Inflammatory Agents; Asthma; Benzamides; Carboxylic Acids; Clinical Trials as Topic; Cyclic Nucleotide Phosphodiesterases, Type 4; Cyclic Nucleotide Phosphodiesterases, Type 5; Cyclic Nucleotide Phosphodiesterases, Type 7; Cyclohexanecarboxylic Acids; Cyclopropanes; Humans; Isoenzymes; Nitriles; Phosphodiesterase Inhibitors; Phosphoric Diester Hydrolases; Pulmonary Disease, Chronic Obstructive

2006
Evaluation of PDE4 inhibition for COPD.
    International journal of chronic obstructive pulmonary disease, 2006, Volume: 1, Issue:4

    Topics: Aminopyridines; Benzamides; Calcium Channel Blockers; Carboxylic Acids; Cyclohexanecarboxylic Acids; Cyclopropanes; Humans; Nitriles; Phosphodiesterase 4 Inhibitors; Phosphodiesterase Inhibitors; Pulmonary Circulation; Pulmonary Disease, Chronic Obstructive; Severity of Illness Index

2006
[Selective phosphodiesterase-4 (PDE-4) inhibitors in COPD].
    Tuberkuloz ve toraks, 2008, Volume: 56, Issue:4

    Topics: 3',5'-Cyclic-AMP Phosphodiesterases; Aminopyridines; Benzamides; Carboxylic Acids; Cyclic AMP; Cyclohexanecarboxylic Acids; Cyclopropanes; Humans; Nitriles; Phosphodiesterase Inhibitors; Pulmonary Disease, Chronic Obstructive

2008
PDE4-inhibitors: a novel, targeted therapy for obstructive airways disease.
    Pulmonary pharmacology & therapeutics, 2011, Volume: 24, Issue:4

    Topics: Aminopyridines; Benzamides; Clinical Trials, Phase III as Topic; Cyclic Nucleotide Phosphodiesterases, Type 7; Cyclohexanecarboxylic Acids; Cyclopropanes; Humans; Lung Diseases, Obstructive; Nitriles; Phosphodiesterase 4 Inhibitors

2011
Phosphodiesterase 4 inhibitors for chronic obstructive pulmonary disease.
    The Cochrane database of systematic reviews, 2011, May-11, Issue:5

    Topics: Administration, Oral; Aminopyridines; Benzamides; Cyclohexanecarboxylic Acids; Cyclopropanes; Forced Expiratory Volume; Humans; Nitriles; Phosphodiesterase 4 Inhibitors; Pulmonary Disease, Chronic Obstructive; Quality of Life; Randomized Controlled Trials as Topic

2011
Phosphodiesterase 4 inhibitors for chronic obstructive pulmonary disease.
    The Cochrane database of systematic reviews, 2013, Nov-04, Issue:11

    Topics: Administration, Oral; Aminopyridines; Benzamides; Cyclohexanecarboxylic Acids; Cyclopropanes; Forced Expiratory Volume; Humans; Nitriles; Phosphodiesterase 4 Inhibitors; Pulmonary Disease, Chronic Obstructive; Quality of Life; Randomized Controlled Trials as Topic

2013
Phosphodiesterase 4 inhibitors for chronic obstructive pulmonary disease.
    The Cochrane database of systematic reviews, 2017, 09-19, Volume: 9

    Topics: Administration, Oral; Aminopyridines; Benzamides; Cyclohexanecarboxylic Acids; Cyclopropanes; Disease Progression; Forced Expiratory Volume; Humans; Nitriles; Phosphodiesterase 4 Inhibitors; Pulmonary Disease, Chronic Obstructive; Quality of Life; Randomized Controlled Trials as Topic

2017
Phosphodiesterase-4 inhibitors for chronic obstructive pulmonary disease.
    The Cochrane database of systematic reviews, 2020, 05-01, Volume: 5

    Topics: Administration, Oral; Aminopyridines; Benzamides; Cyclohexanecarboxylic Acids; Cyclopropanes; Diarrhea; Disease Progression; Forced Expiratory Volume; Humans; Middle Aged; Nitriles; Peak Expiratory Flow Rate; Phosphodiesterase 4 Inhibitors; Pulmonary Disease, Chronic Obstructive; Quality of Life; Randomized Controlled Trials as Topic; Thiazoles; Vital Capacity

2020

Other Studies

21 other study(ies) available for cilomilast and roflumilast

ArticleYear
Structural basis for the activity of drugs that inhibit phosphodiesterases.
    Structure (London, England : 1993), 2004, Volume: 12, Issue:12

    Topics: Binding Sites; Crystallography, X-Ray; Phosphodiesterase Inhibitors; Phosphoric Diester Hydrolases; Protein Structure, Tertiary

2004
In silico search for multi-target anti-inflammatories in Chinese herbs and formulas.
    Bioorganic & medicinal chemistry, 2010, Mar-15, Volume: 18, Issue:6

    Topics: Anti-Inflammatory Agents; Crystallography, X-Ray; Cyclooxygenase 1; Cyclooxygenase 2; Databases, Factual; Drug Design; Drugs, Chinese Herbal; Enzyme Inhibitors; JNK Mitogen-Activated Protein Kinases; Medicine, Chinese Traditional; Models, Chemical; Models, Molecular; Molecular Conformation; p38 Mitogen-Activated Protein Kinases; Phosphodiesterase 4 Inhibitors; Structure-Activity Relationship

2010
Dual β2-adrenoceptor agonists-PDE4 inhibitors for the treatment of asthma and COPD.
    Bioorganic & medicinal chemistry letters, 2012, Feb-15, Volume: 22, Issue:4

    Topics: Adrenergic beta-2 Receptor Agonists; Animals; Asthma; Drug Design; Guinea Pigs; Inhibitory Concentration 50; Molecular Structure; Phosphodiesterase 4 Inhibitors; Pulmonary Disease, Chronic Obstructive; Trachea

2012
Discovery of triazines as potent, selective and orally active PDE4 inhibitors.
    Bioorganic & medicinal chemistry letters, 2013, Aug-01, Volume: 23, Issue:15

    Topics: Administration, Oral; Animals; Binding Sites; Cyclic Nucleotide Phosphodiesterases, Type 4; Cyclic Nucleotide Phosphodiesterases, Type 7; Drug Evaluation, Preclinical; Half-Life; Microsomes, Liver; Molecular Docking Simulation; Phosphodiesterase 4 Inhibitors; Protein Structure, Tertiary; Rats; Structure-Activity Relationship; Triazines

2013
Design, synthesis and evaluation of dual pharmacology β2-adrenoceptor agonists and PDE4 inhibitors.
    Bioorganic & medicinal chemistry letters, 2014, Jan-01, Volume: 24, Issue:1

    Topics: Adrenergic beta-2 Receptor Agonists; Cyclic Nucleotide Phosphodiesterases, Type 4; Dose-Response Relationship, Drug; Drug Design; Ethanolamines; Formoterol Fumarate; Humans; Molecular Structure; Phosphodiesterase 4 Inhibitors; Phthalazines; Receptors, Adrenergic, beta-2; Recombinant Proteins; Structure-Activity Relationship

2014
PDEStrIAn: A Phosphodiesterase Structure and Ligand Interaction Annotated Database As a Tool for Structure-Based Drug Design.
    Journal of medicinal chemistry, 2016, Aug-11, Volume: 59, Issue:15

    Topics: Databases, Protein; Dose-Response Relationship, Drug; Drug Design; Humans; Ligands; Models, Molecular; Molecular Structure; Phosphodiesterase Inhibitors; Phosphoric Diester Hydrolases; Structure-Activity Relationship

2016
Structure-Aided Identification and Optimization of Tetrahydro-isoquinolines as Novel PDE4 Inhibitors Leading to Discovery of an Effective Antipsoriasis Agent.
    Journal of medicinal chemistry, 2019, 06-13, Volume: 62, Issue:11

    Topics: Animals; Caco-2 Cells; Catalytic Domain; Cyclic Nucleotide Phosphodiesterases, Type 4; Drug Design; Drug Evaluation, Preclinical; Female; HEK293 Cells; Humans; Male; Mice; Models, Molecular; Phosphodiesterase 4 Inhibitors; Psoriasis; Rats; Stereoisomerism; Structure-Activity Relationship; Tetrahydroisoquinolines; Tissue Distribution

2019
Discovery of sulfonyl hydrazone derivative as a new selective PDE4A and PDE4D inhibitor by lead-optimization approach on the prototype LASSBio-448: In vitro and in vivo preclinical studies.
    European journal of medicinal chemistry, 2020, Oct-15, Volume: 204

    Topics: Animals; Cyclic AMP; Cyclic Nucleotide Phosphodiesterases, Type 4; Drug Design; Enzyme Inhibitors; Humans; Hydrazones; Hypersensitivity; Lung; Male; Mice

2020
Anti-inflammatory potential of the selective phosphodiesterase 4 inhibitor N-(3,5-dichloro-pyrid-4-yl)-[1-(4-fluorobenzyl)-5-hydroxy-indole-3-yl]-glyoxylic acid amide (AWD 12-281), in human cell preparations.
    The Journal of pharmacology and experimental therapeutics, 2004, Volume: 308, Issue:2

    Topics: 3',5'-Cyclic-AMP Phosphodiesterases; Amides; Aminopyridines; Anti-Inflammatory Agents; Benzamides; Cyclic Nucleotide Phosphodiesterases, Type 4; Cyclohexanecarboxylic Acids; Cyclopropanes; Cytokines; Humans; Indoles; Interleukin-2; Interleukin-4; Interleukin-5; Leukocytes, Mononuclear; Nitriles; Phosphodiesterase Inhibitors; Polyps; Tumor Necrosis Factor-alpha

2004
Inhibition of airway hyperresponsiveness and pulmonary inflammation by roflumilast and other PDE4 inhibitors.
    Pulmonary pharmacology & therapeutics, 2006, Volume: 19, Issue:5

    Topics: 3',5'-Cyclic-AMP Phosphodiesterases; Administration, Oral; Aminopyridines; Animals; Benzamides; Bronchial Spasm; Bronchoalveolar Lavage Fluid; Carboxylic Acids; Cyclic Nucleotide Phosphodiesterases, Type 4; Cyclohexanecarboxylic Acids; Cyclopropanes; Disease Models, Animal; Immunization; Male; Neutrophils; Nitriles; Ovalbumin; Phosphodiesterase Inhibitors; Pneumonia; Pyridines; Rats; Respiratory Hypersensitivity; Rolipram; Serotonin; Treatment Outcome; Tumor Necrosis Factor-alpha

2006
L-454,560, a potent and selective PDE4 inhibitor with in vivo efficacy in animal models of asthma and cognition.
    Biochemical pharmacology, 2007, Jun-15, Volume: 73, Issue:12

    Topics: 3',5'-Cyclic-AMP Phosphodiesterases; Aminopyridines; Animals; Apoenzymes; Ascaris suum; Asthma; Benzamides; Bronchoconstriction; Carboxylic Acids; Cognition Disorders; Cyclic AMP; Cyclic Nucleotide Phosphodiesterases, Type 4; Cyclohexanecarboxylic Acids; Cyclopropanes; Disease Models, Animal; Dose-Response Relationship, Drug; Guinea Pigs; Humans; Inhibitory Concentration 50; Injections, Intraperitoneal; Interferon-gamma; Male; Molecular Structure; Nitriles; Ovalbumin; Polymerase Chain Reaction; Quinolines; Rats; Sensitivity and Specificity; Sheep

2007
Phosphodiesterase 4 inhibitors augment levels of glucocorticoid receptor in B cell chronic lymphocytic leukemia but not in normal circulating hematopoietic cells.
    Clinical cancer research : an official journal of the American Association for Cancer Research, 2007, Aug-15, Volume: 13, Issue:16

    Topics: 3',5'-Cyclic-AMP Phosphodiesterases; Aminopyridines; Apoptosis; Benzamides; Carboxylic Acids; Cyclic Nucleotide Phosphodiesterases, Type 4; Cyclohexanecarboxylic Acids; Cyclopropanes; Dexamethasone; Gene Expression Regulation, Leukemic; Hematopoietic System; Humans; Leukemia, Lymphocytic, Chronic, B-Cell; Nitriles; Phosphodiesterase Inhibitors; Receptors, Glucocorticoid; Rolipram

2007
Curative effects of phosphodiesterase 4 inhibitors cilomilast, roflumilast, and rolipram in dermatitis mouse model.
    Journal of dermatological science, 2008, Volume: 51, Issue:3

    Topics: Aminopyridines; Animals; Benzamides; Carboxylic Acids; Cyclohexanecarboxylic Acids; Cyclopropanes; Dermatitis; Dermatitis, Contact; Disease Models, Animal; Eosinophil Peroxidase; Interleukin-4; Male; Mice; Mice, Inbred BALB C; Nitriles; Peroxidase; Phosphodiesterase 4 Inhibitors; Phosphodiesterase Inhibitors; Picryl Chloride; Rolipram

2008
The identification of a novel phosphodiesterase 4 inhibitor, 1-ethyl-5-{5-[(4-methyl-1-piperazinyl)methyl]-1,3,4-oxadiazol-2-yl}-N-(tetrahydro-2H-pyran-4-yl)-1H-pyrazolo[3,4-b]pyridin-4-amine (EPPA-1), with improved therapeutic index using pica feeding in
    The Journal of pharmacology and experimental therapeutics, 2009, Volume: 330, Issue:3

    Topics: Aminopyridines; Animals; Benzamides; Carboxylic Acids; Cyclohexanecarboxylic Acids; Cyclopropanes; Ferrets; Humans; Lipopolysaccharides; Mice; Mice, Inbred C57BL; Neutrophils; Nitriles; Phosphodiesterase 4 Inhibitors; Phosphodiesterase Inhibitors; Pica; Piperazines; Pyridines; Rats; Rats, Inbred Lew; Receptors, Adrenergic, alpha-2; Rolipram; Tumor Necrosis Factor-alpha; Vomiting

2009
ASP3258, an orally active potent phosphodiesterase 4 inhibitor with low emetic activity.
    International immunopharmacology, 2011, Volume: 11, Issue:6

    Topics: Adrenergic alpha-2 Receptor Antagonists; Aminopyridines; Animals; Benzamides; Blood Cells; Cyclic Nucleotide Phosphodiesterases, Type 4; Cyclohexanecarboxylic Acids; Cyclopropanes; Enzyme Inhibitors; Ferrets; Interleukin-4; Lipopolysaccharides; Macrophages, Alveolar; Naphthyridines; Nitriles; Pneumonia; Rats; Tumor Necrosis Factor-alpha; Vomiting

2011
Anti-asthmatic effect of ASP3258, a novel phosphodiesterase 4 inhibitor.
    International immunopharmacology, 2012, Volume: 12, Issue:1

    Topics: Aminopyridines; Animals; Anti-Asthmatic Agents; Benzamides; Bronchial Hyperreactivity; Bronchoconstriction; Cyclohexanecarboxylic Acids; Cyclopropanes; Disease Models, Animal; Eosinophils; Female; Guinea Pigs; In Vitro Techniques; Lung; Male; Naphthyridines; Nitriles; Ovalbumin; Phosphodiesterase 4 Inhibitors; Rats; Trachea

2012
Anti-neutrophilic inflammatory activity of ASP3258, a novel phosphodiesterase type 4 inhibitor.
    International immunopharmacology, 2012, Volume: 12, Issue:1

    Topics: Adult; Aminopyridines; Animals; Anti-Inflammatory Agents; Benzamides; Bronchoalveolar Lavage Fluid; Cells, Cultured; Chemokine CXCL1; Cyclohexanecarboxylic Acids; Cyclopropanes; Glucocorticoids; Humans; Lipopolysaccharides; Male; Naphthyridines; Neutrophils; Nitriles; Phosphodiesterase 4 Inhibitors; Pneumonia; Prednisolone; Rats; Rats, Wistar; Superoxides; Tumor Necrosis Factor-alpha

2012
Monitoring phosphodiesterase-4 inhibitors using liquid chromatography/(tandem) mass spectrometry in sports drug testing.
    Rapid communications in mass spectrometry : RCM, 2013, May-15, Volume: 27, Issue:9

    Topics: Aminopyridines; Benzamides; Chromatography, Liquid; Cyclohexanecarboxylic Acids; Cyclopropanes; Humans; Limit of Detection; Nitriles; Phosphodiesterase 4 Inhibitors; Rolipram; Spectrometry, Mass, Electrospray Ionization; Substance Abuse Detection; Tandem Mass Spectrometry

2013
Characterization of the cellular activity of PDE 4 inhibitors using two novel PDE 4 reporter cell lines.
    Molecular pharmaceutics, 2013, Oct-07, Volume: 10, Issue:10

    Topics: Aminopyridines; Animals; Benzamides; CHO Cells; Cricetulus; Cyclic AMP; Cyclic Nucleotide Phosphodiesterases, Type 4; Cyclic Nucleotide-Gated Cation Channels; Cyclohexanecarboxylic Acids; Cyclopropanes; Humans; Models, Biological; Nitriles; Phosphodiesterase 4 Inhibitors; Pyridines; Receptors, Adrenergic, beta-1; Reverse Transcriptase Polymerase Chain Reaction

2013
The role of phosphodiesterase 4B in IL-8/LTB4-induced human neutrophil chemotaxis evaluated with a phosphodiesterase 4B inhibitor.
    Acta pharmaceutica (Zagreb, Croatia), 2015, Volume: 65, Issue:2

    Topics: Adult; Aminopyridines; Benzamides; Chemotaxis; Cyclic Nucleotide Phosphodiesterases, Type 4; Cyclohexanecarboxylic Acids; Cyclopropanes; Dose-Response Relationship, Drug; Female; Humans; Interleukin-8; Leukocytes, Mononuclear; Leukotriene B4; Lipopolysaccharides; Male; Neutrophils; Nitriles; Phosphodiesterase 4 Inhibitors; Tumor Necrosis Factor-alpha

2015
Potentiation of long-acting β
    Respiratory research, 2021, Oct-19, Volume: 22, Issue:1

    Topics: Adrenergic beta-2 Receptor Agonists; Aminopyridines; Benzamides; Benzothiazoles; Budesonide; Cell Line; Chemokines; Cyclic AMP; Cyclic Nucleotide Phosphodiesterases, Type 4; Cyclohexanecarboxylic Acids; Cyclopropanes; Drug Synergism; Drug Therapy, Combination; Epithelial Cells; Formoterol Fumarate; Glucocorticoids; Humans; Lung; Multidrug Resistance-Associated Proteins; Nitriles; Phosphodiesterase 4 Inhibitors; Rolipram; Second Messenger Systems; Triazoles

2021