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| Content Provider | World Health Organization (WHO)-Global Index Medicus |
|---|---|
| Author | Pruniaux, Marie-Pierre Lagente, Vincent Ouaged, Malika Bertin, Bernadette Moreau, François Julien-Larose, Christine Rocher, Marie-Noelle Leportier, Christelle Martin, Brigitte Bouget, Anita Dubuit, Jean-Pierre Burnouf, Catherine Doherty, Annette M. Bertrand, Claude P. |
| Description | Country affiliation: France Author Affiliation: Pruniaux MP ( Pfizer Global Research and Development, Fresnes Laboratories, Fresnes, France.) |
| Abstract | The anti-inflammatory effects of CI-1044 and of the other selective PDE4 inhibitors rolipram and cilomilast were investigated in Brown-Norway (BN) rats, against lipopolysaccharide-induced tumor necrosis factor alpha (TNFalpha) production in whole blood and antigen-induced lung eosinophilia. In vitro, CI-1044 inhibited TNFalpha production with an IC(50) of 0.31 microm being equipotent to Cilomilast (IC(50) = 0.26 microm) and rolipram (IC(50) = 0.11 microm). Given orally, CI-1044 inhibited ex vivo TNFalpha production with an ED(50) value of 0.4 mg/kg after single administration, whereas rolipram (ED(50) = 1.4 mg/kg) and cilomilast (ED(50) = 1.6 mg/kg) were less potent. In the same ex vivo setting, but given repeatedly, CI-1044 led to an ED(50) of 0.5 mg/kg corresponding to a plasma concentration of 82.6 ng/mL (0.22 microm). In vivo, CI-1044 prevented TNFalpha release with an ED(50) of 1 mg/kg p.o. and inhibited ovalbumin-induced lung eosinophilia following single or repeated oral administration with an ED(50) of 3.25 and 4.8 mg/kg p.o., respectively, suggesting the absence of pharmacological tolerance. CI-1044 in this model was equipotent to rolipram (81% inhibition at 10 mg/kg) but better than cilomilast (25% inhibition at 10 mg/kg). Finally, CI-1044 (10 mg/kg) inhibited inflammatory cell recruitment with a long duration of action (up to 8 h) and was still active when given post-challenge. Our data show that CI-1044 is an orally active PDE4 inhibitor that may be used as an anti-inflammatory therapy in lung inflammatory diseases. |
| File Format | HTM / HTML |
| ISSN | 07673981 |
| Issue Number | 1 |
| Volume Number | 24 |
| e-ISSN | 14728206 |
| Journal | Fundamental & Clinical Pharmacology |
| Language | English |
| Publisher | Wiley |
| Publisher Date | 2010-02-01 |
| Publisher Place | Great Britain (UK) |
| Access Restriction | One Nation One Subscription (ONOS) |
| Subject Keyword | Discipline Pharmacology Azepines Pharmacology Inflammation Drug Therapy Niacinamide Analogs & Derivatives Phosphodiesterase 4 Inhibitors Phosphodiesterase Inhibitors Administration, Oral Animals Administration & Dosage Carboxylic Acids Cyclohexanecarboxylic Acids Disease Models, Animal Dose-response Relationship, Drug Drug Administration Schedule Physiopathology Inhibitory Concentration 50 Lipopolysaccharides Male Nitriles Pulmonary Eosinophilia Rats Rats, Inbred Bn Rolipram Tumor Necrosis Factor-alpha Drug Effects Metabolism Comparative Study Journal Article |
| Content Type | Text |
| Resource Type | Article |
| Subject | Pharmacology Pharmacology (medical) |
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