Anti-inflammatory activities of LDP-392, a dual PAF receptor antagonist and 5-lipoxygenase inhibitor

Pharmacological Research

Volumn 44, Issue 3, 2001, Pages 213-220

  Qian, Changgeng ^a   Hwang, S B ^a   Libertine Garahan, L ^b   Eckman, J B ^b   Cai, X ^b   Scannell, R T ^b   Yeh, C G ^a  

^a MILLENNIUM PHARMACEUTICALS INC   (United States)

^b UCB PHARMA   (Belgium)

Author keywords

5 lipoxygenase inhibitor; Inflammation; LDP 392; PAF antagonist

Indexed keywords

6 (2 CHLOROPHENYL) 4,7,8,10 TETRAHYDRO 9 (4 METHOXYPHENYLCARBAMOYL) 1 METHYLPYRIDO[4',3':4,5]THIENO[3,2 F][1,2,4]TRIAZOLO[4,3 A][1,4]DIAZEPINE; 6 (2 CHLOROPHENYL) 9 [(3,4 DIMETHOXYPHENYL)THIOMETHYLTHIOCARBONYL] 4,7,8,10 TETRAHYDRO 1 METHYLPYRIDO[4',3':4,5]THIENO[3,2 F][1,2,4]TRIAZOLO[4,3 A][1,4]DIAZEPINE; A 78733; BB 823; LDP 392; LEUKOTRIENE B4; LIPOXYGENASE INHIBITOR; MK 287; MODIPAFANT; N [3 (3 PHENOXYPHENYL)ALLYL]ACETOHYDROXAMIC ACID; THROMBOCYTE ACTIVATING FACTOR ANTAGONIST; UNCLASSIFIED DRUG; ZILEUTON;

ANIMAL MODEL; ANIMAL TISSUE; ANTIINFLAMMATORY ACTIVITY; ARTICLE; CONTROLLED STUDY; DOSE RESPONSE; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG STRUCTURE; EDEMA; FEMALE; GUINEA PIG; HEMOCONCENTRATION; HUMAN; ICOSANOID METABOLISM; INFLAMMATION; LETHALITY; MOUSE; NONHUMAN; PRIORITY JOURNAL;

EID: 0034835011     PISSN: 10436618     EISSN: None     Source Type: Journal    
DOI: 10.1006/phrs.2001.0808     Document Type: Article

References (52)

1. Platelet-activating factor and related acetylated lipids as potent biologically active cellular mediators
2. Platelet activating factor (PAF). A review of its effects, antagonists and possible future clinical implications (Part I)
3. Effects of various banders on platelet-activating factor-induced neutrophil chemotaxis
4. Leukotriene B4 is a potent and stereospecific stimulator of neutrophil chemotaxis and adherence
5. Comparison differences and combined effects of interleukin-8, leukotriene B4, and platelet-activating factor on neutrophil chemotaxis of the newborn
6. Preferential human eosinophil chemotactic activity of the platelet-activating factor (PAF) 1-0-hexadecyl-2-acetyl-sn-glyceryl-3-phosphocholine (AGEPC)
7. Platelet-activating factor. A potent chemotactic and chemokinetic factor for human eosinophils
8. Eosinophil chemotaxis inhibited by 5-lipoxygenase blockade and leukotriene receptor antagonism
9. Increased monocyte chemotaxis towards leukotriene B4 and platelet activating factor in patients with inflammatory dermatoses
10. 4-induced airway constriction in the Guinea-pig
11. Platelet-activating factor is a key mediator of pulmonary vasoconstriction and bronchoconstriction after antigen challenge in the perfused sensitized rabbit lung
12. Role of leukotrienes and platelet activating factor in allergic bronchoconstriction and their interactions in Guinea-pigairway in vivo
13. Paf-acether (platelet-activating factor) increases microvascular permeability and affects endothelium granulocyte interaction in microvascular beds
14. Leukotriene B4: A mediator of vascular permeability
15. 4
16. Effect of fenoterol on PAF-induced lung edema in isolated and perfused rabbit lungs
17. Effects of PAF antagonists in mouse ear oedema induced by several inflammatory agents
18. Beneficial effects of a leukotriene receptor antagonist on thrombin-induced pulmonary edema in the rat
19. Increased levels of blood platelet-activating factor in bronchial asthmatic patients with active symptoms
20. Increased plasma level of platelet-activating factor (PAF) and decreased serum PAF acetylhydrolase (PAFAH) activity in adults with bronchial asthma
21. 4 in patients with asthma. Effect of airways reactivity and sodium cromoglycate
22. Blood leukotriene levels during the acute asthma attack in children
23. Platelet activating factor (PAF) and lyso-PAF in psoriasis
24. Psoriasis and leukotriene B4
25. Chemical mediators in atopic dermatitis: Involvement of leukotriene B4 released by a type I allergic reaction in the pathogenesis of dermatitis
26. Leukotriene B4 in atopic dermatitis: Increased skin levels and altered sensitivity of peripheral blood T-cells
27. 4 are present in biologically active concentrations
28. The design of dual-acting compounds with PAF receptor antagonistic and 5-lipoxygenase inhibitory activities
29. (+/-)-Trans-2-[3-methoxy-4-(4 chlorophenylthioethoxy)-5-(N-methyl-N-hydroxyureidyl)methylphenyl]-5-(3,4,5 trimethoxyphenyl)tetrahydrofuran (LDP-392), a potentdual 5-lipoxygenase inhibitor and platelet-activating factorreceptor antagonist
30. Species difference in the specific receptors of platelet activating factor
31. Purification of arachidonate 5 lipoxygenase from porcine leukocytes and its reactivity with hydroperoxyeicosatetraenoic acid
32. Measurement of cutaneous inflammation: Estimation of neutrophil content with an enzyme marker
33. Effect of a 5-lipoxygenase (5-LO)/cyclooxygenase (CO) inhibitor, WY-47, 288, on cutaneous models of inflammation
34. Leukotriene D4 and platelet-activating factor-acether antagonists on allergic and arachidonic acid-induced reactions in Guinea-pig airways
35. The role of platelet-activating factor and peptidoleukotrienes in the vascular changes of rat passive anaphylaxis
36. Effects of platelet-activating factor antagonist and leukotriene antagonist on endotoxin shock in the rate: Role of the leukocyte
37. Effect of zileuton (A 64077) on the 5-lipoxygenase activity of human whole blood ex vivo
38. 5-Lipoxygenase inhibitory activity of zileuton
39. A-78773: A selective, potent 5-lipoxygenase inhibitor
40. Preclinical and clinical activity of zileuton and A-78773
41. MK 287: A potent, specific, and orally active receptor antagonist of platelet-activating factor
42. Prostaglandin and leukotriene synthesis in mouse ears inflamed by arachidonic acid
43. The mouse ear inflammatory response to topical arachidonic acid
44. Comparative study of the effect of CV-6209, a specific PAF-antagonist, on rat paw edema caused by different phlogogen agents
45. Involvement of platelet-activating factor (PAF) in septic shock and priming as indicated by the effect of hetrazepionic PAF antagonists
46. Cardiopulmonary dysfunction in a feline septic shock model: Possible role of leukotrienes
47. Antiinflammatory activity of the platelet activating factor receptor antagonist A-85783
48. Effects of Y-24180, a receptor antagonist to platelet-activating factor, on allergic cutaneous eosinophilia in mice
49. Topical application of a platelet-activating factor (PAF) antagonist in atopic dermatitis
50. Investigation on a novel and specific leukotriene B4 receptor antagonist in the treatment of stable plaque psoriasis
51. The leukotriene antagonist zafirlukast as a therapeutic agent for atopic dermatitis
52. 4 hydrolase inhibitor, and indomethacin on carrageenan-induced murine dermatitis