A novel phosphodiesterase type 4, inhibitor, YM976 (4-(3-chlorophenyl)-1,7-diethylpyrido[2,3-d]pyrimidin-2(1H)-one), with little emetogenic activity

Journal of Pharmacology and Experimental Therapeutics

Volumn 295, Issue 1, 2000, Pages 255-260

  Aoki, Motonori ^a   Kobayashi, Miki ^a   Ishikawa, Jun ^a   Saita, Yuji ^a   Terai, Yoshiya ^a   Takayama, Kazuhisa ^a   Miyata, Keiji ^a   Yamada, Toshimitsu ^a  

^a ASTELLAS PHARMA INC   (Japan)

Author keywords

[No Author keywords available]

Indexed keywords

4 (3 CHLOROPHENYL) 1,7 DIETHYLPYRIDO[2,3 D]PYRIMIDIN 2(1H) ONE; 4 [2 [3 (CYCLOPENTYLOXY) 4 METHOXYPHENYL] 2 PHENYLETHYL]PYRIDINE; CILOMILAST; CILOSTAMIDE; CYCLIC AMP; ISOENZYME; PHOSPHODIESTERASE; PHOSPHODIESTERASE I; PHOSPHODIESTERASE IV; PHOSPHODIESTERASE IV INHIBITOR; PICLAMILAST; PROSTAGLANDIN E2; ROLIPRAM; TUMOR NECROSIS FACTOR ALPHA; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANTIINFLAMMATORY ACTIVITY; ARTICLE; CELL INFILTRATION; COMPETITIVE INHIBITION; CONTROLLED STUDY; DOSE RESPONSE; DRUG MECHANISM; DRUG STRUCTURE; DRUG SYNTHESIS; ENZYME INHIBITION; FERRET; HUMAN; HUMAN CELL; IC 50; LEUKOCYTE; NONHUMAN; PRIORITY JOURNAL; STRUCTURE ACTIVITY RELATION; VOMITING;

ANIMALS; ANTI-INFLAMMATORY AGENTS, NON-STEROIDAL; CYCLIC AMP; FERRETS; HUMANS; MALE; PHOSPHODIESTERASE INHIBITORS; PLEURISY; PYRIDINES; PYRIMIDINONES; RATS; TUMOR NECROSIS FACTOR-ALPHA; U937 CELLS; VOMITING;

EID: 0033798777     PISSN: 00223565     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (39)

1. Microvascular permeability and number of tight junctions are modulated by cAMP
2. Effect of rolipram and dibutyryl cyclic AMP on resequestration of cytosolic calcium in FMLP-activated human neutrophils
3. Investigation of the inhibitory effects of PGE2 and selective EP agonists on chemotaxis of human neutrophils
4. Theophylline and selective phosphodiesterase inhibitors as anti-inflammatory drugs in the treatment of bronchial
5. Anti-inflammatory effects of theophylline and selective phosphodiesterase inhibitors
6. Inhibition of PAF-induced expression of CD11b and shedding of L-selectin on human neutrophils and eosinophils by the type IV selective PDE inhibitor, rolipram
7. Rolipram versus imipramine in inpatients with major, 'minor' or atypical depressive disorder: A double-blind double-dummy study aimed at testing a novel therapeutic approach
8. A family of human phosphodiesterases homologous to the dunce learning and memory gene product of Drosophila melanogaster are potential targets for antidepressant drugs
9. Further studies on carrageenan-induced pleurisy in rats
10. In vitro pharmacology of the novel phosphodiesterase type 4 inhibitor CP-80633
11. Phosphodiesterase 4-dependent regulation of cyclic AMP levels and leukotriene B4 biosynthesis in human polymorphonuclear leukocytes
12. Inhibition of chemotactic peptide-induced neutrophil adhesion to vascular endothelium by cAMP modulators
13. 3H]rolipram binding activity and their relationship to emetic behavior in the ferret
14. Differential efficacy of lymphocyte- and monocyte-selective pretreatment with a type 4 phosphodiesterase inhibitor on antigen-driven proliferation and cytokine gene expression
15. Pharmacology of the potent new non-steroidal anti-inflammatory agent aceclofenac
16. Effects of rolipram on cyclic AMP levels in alveolar macrophages and lipopolysaccharide-induced inflammation in mouse lung
17. Emetic central nervous system, and pulmonary activities of rolipram in the dog
18. Rolipram in major depressive disorder: Results of a double-blind comparative study with imipramine
19. Inhibition of bronchospasm and ozone-induced airway hyperresponsiveness in the guinea-pig by CDP840, a novel phosphodiesterase type 4 inhibitor
20. pEF-BOS, a powerful mammalian expression vector
21. Action of cAMP on expression and release of adhesion molecules in human endothelial cells
22. Effects of RP73401, a novel, potent and selective phosphodiesterase type 4 inhibitor, on contractility of human, isolated bronchial muscle
23. Amelioration of collagen II-induced arthritis in rats by the type IV phosphodiesterase inhibitor Rolipram
24. Effects of selective phosphodiesterase inhibitors on platelet-activating factor- and antigen-induced airway hyperreactivity, eosinophil accumulation, and microvascular leakage in guinea pigs
25. Compartmentalization of PDE-4 and cAMP-dependent protein kinase in neutrophils and macrophages during phagocytosis
26. Suppression of TNF-alpha expression, inhibition of Th1 activity, and amelioration of collagen-induced arthritis by rolipram
27. Selective phosphodiesterase inhibitors for the treatment of bronchial asthma and chronic obstructive pulmonary disease
28. PDE isoenzymes as targets for antiasthma drugs
29. Interleukin-10 does not mediate the inhibitory effect of PDE-4 inhibitors and other cAMP-elevating drugs on lipoplysaccharide-induced tumors necrosis factor-alpha generation from human peripheral blood monocytes
30. Role of cyclic 3',5'-adenosine monophosphate in the regulation of chemical mediator release and cytokine production from cultured human mast cells
31. Cyclic AMP-elevating agents inhibit mite-antigen-induced IL-4 and IL-13 release from basophil-enriched leukocyte preparation
32. Suppression of eosinophil function by RP73401, a potent and selective inhibitor of cyclic AMP-specific phosphodiesterase: Comparison with rolipram
33. Effects of rolipram and cilostamide on renal functions and cyclic AMP release in anesthetized dogs
34. Phosphodiesterase (PDE) 4 inhibitors: Anti-inflammatory drugs of the future
35. Ariflo (SB207499), a second generation phosphodiesterase 4 inhibitor for the treatment of asthma and COPD: From concept to clinic
36. Antiasthmatic activity of the second-generation phosphodiesterase 4 (PDE4) inhibitor SB207499 (Ariflo) in the guinea pig
37. Inhibition of antigen-induced bronchoconstriction and eosinophil infiltration in the guinea pig by the cyclic AMP-specific phosphodiesterase inhibitor, rolipram
38. Pathway of onset, development, and decay of carrageenan pleurisy in the rat
39. Differential in vivo and in vitro bronchorelaxant activities of CP-80,633, a selective phosphodiesterase 4 inhibitor