CI 1044

inhibits PDE4; structure in first source

Also Known As:

CI-1044; N-(9-amino-4-oxo-1-phenyl-3,4,6,7-tetrahydro(1,4)diazepino(6,7,1-hi)indol-3-yl)nicotinamide; 3-Pyridinecarboxamide, N-((3R)-9-amino-3,4,6,7-tetrahydro-4-oxo-1-phenyl(1,4)diazepino(6,7,1-hi)indol-3-yl)-

Networked: 11 relevant articles (0 outcomes, 4 trials/studies)

Bio-Agent Context: Research Results

Heterocyclic Compounds: 198
- 1-Ring Heterocyclic Compounds
  - Pyridines: 88
    - Nicotinic Acids: 13
      - Niacinamide: 2223
        CI 1044: 11
  - Azepines: 11
    - CI 1044: 11
- Heterocyclic Acids
  - Nicotinic Acids: 13
    - Niacinamide: 2223
      - CI 1044: 11

Experts

1.	Chevalier, Stephan: 4 articles (01/2009 - 01/2007)
2.	Sobry, Cécile: 4 articles (01/2009 - 01/2007)
3.	Freslon, Jean-Louis: 3 articles (01/2009 - 01/2007)
4.	Daguès, Nicolas: 3 articles (06/2008 - 01/2007)
5.	Hanton, Gilles: 3 articles (06/2008 - 01/2007)
6.	Lagente, Vincent: 2 articles (02/2010 - 03/2005)
7.	Pawlowski, Valérie: 2 articles (11/2007 - 01/2007)
8.	Enerson, Bradley E: 1 article (07/2011)
9.	Lawton, Michael P: 1 article (07/2011)
10.	Peters, David: 1 article (07/2011)

Related Diseases

1.	Vascular System Injuries 07/01/2011 - "SIN-1 coadministration caused vascular injury to occur at lower doses of CI-1044, compared with CI-1044 alone, with the overall incidence and severity of injury being greater across all CI-1044-dose groups. " 07/01/2011 - "Compared with vehicle controls, treatment with CI-1044 alone resulted in dose-related increases in the frequency and severity of vascular injury, SN levels, and NT residues. " 11/01/2007 - "In order to investigate the early molecular mechanisms underlying vascular injury, time-course studies were performed by treating rats for 2-24 h with high doses of the PDE4 inhibitor CI-1044. " 01/01/2007 - "The present study was undertaken to investigate the molecular mechanisms of drug-induced vascular injury in mesenteric tissue of rats treated with the selective phosphodiesterase 4 (PDE4) inhibitor CI-1044. "
2.	Necrosis 01/01/2009 - "In the present study, an administration of 160 mg/kg of CI-1044 caused perivascular and interstitial inflammation, with infiltrates of admixed neutrophils and macrophages but without evidence of vascular necrosis (ileum, 15/20 rats; duodenum + jejunum, 7/20 rats). " 06/10/2008 - "Dogs were treated for 4 days with 5, 10, 20 or 50 mg/kg of CI-1044, and a group of dogs was submitted to a 4-week recovery period after treatment with 20 mg/kg. CI-1044 induced disseminated vascular necrosis and inflammation in various organs/tissues from 20 mg/(kg day). "
3.	Inflammation (Inflammations) 01/01/2009 - "In the present study, an administration of 160 mg/kg of CI-1044 caused perivascular and interstitial inflammation, with infiltrates of admixed neutrophils and macrophages but without evidence of vascular necrosis (ileum, 15/20 rats; duodenum + jejunum, 7/20 rats). " 06/10/2008 - "Dogs were treated for 4 days with 5, 10, 20 or 50 mg/kg of CI-1044, and a group of dogs was submitted to a 4-week recovery period after treatment with 20 mg/kg. CI-1044 induced disseminated vascular necrosis and inflammation in various organs/tissues from 20 mg/(kg day). "
4.	Chronic Obstructive Pulmonary Disease (COPD) 01/01/2005 - "The novel phosphodiesterase 4 inhibitor, CI-1044, inhibits LPS-induced TNF-alpha production in whole blood from COPD patients." 01/01/2005 - "These results indicate that CI-1044 inhibits in vitro LPS-induced TNF-alpha release in whole blood from COPD patients better than rolipram and cilomilast and suggested that it could be a useful anti-inflammatory therapy in COPD." 01/01/2005 - "In the whole blood from COPD patients pre-incubation with PDE4 inhibitors or dexamethasone resulted in a dose-dependent inhibition of LPS-induced TNF-alpha release with IC(50) values of 1.3+/-0.7, 2.8+/-0.9 microM, higher to 10 microM and lesser than 0.03 microM for CI-1044, rolipram, cilomilast and dexamethasone, respectively. " 01/01/2005 - "The aim of this study was to compare the in vitro activities of the novel selective PDE4 inhibitors CI-1044 compared to well-known PDE4 inhibitors, rolipram and cilomilast, and to the glucocorticoid dexamethasone at reducing lipopolysaccharide (LPS)-induced TNF-alpha release in whole blood from COPD patients and healthy subjects. "
5.	Lung Injury 03/01/2005 - "We demonstrated that selective PDE4 inhibitor RP 73-401 reduced matrix metalloproteinase (MMP)-9 activity and TGF-beta1 release during LPS-induced lung injury in mice and that CI-1044 inhibited the production of MMP-1 and MMP-2 from human lung fibroblasts stimulated by pro-inflammatory cytokines. "

Related Drugs and Biologics

1.	Phosphodiesterase 4 Inhibitors
2.	Rolipram
3.	Tumor Necrosis Factor-alpha (Tumor Necrosis Factor)
4.	Lipopolysaccharides
5.	Cilomilast
6.	Type 4 Cyclic Nucleotide Phosphodiesterases
7.	Glucocorticoids
8.	Dexamethasone (Maxidex)
9.	Phosphodiesterase 3 Inhibitors
10.	Transforming Growth Factor beta1 (TGF beta 1)

Related Therapies and Procedures

1.	Therapeutics
2.	Aftercare (After-Treatment)