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leukotriene b4

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Description

Leukotriene B4: The major metabolite in neutrophil polymorphonuclear leukocytes. It stimulates polymorphonuclear cell function (degranulation, formation of oxygen-centered free radicals, arachidonic acid release, and metabolism). (From Dictionary of Prostaglandins and Related Compounds, 1990) [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

leukotriene B4 : A leukotriene composed of (6Z,8E,10E,14Z)-icosatetraenoic acid having (5S)- and (12R)-hydroxy substituents. It is a lipid mediator of inflammation that is generated from arachidonic acid via the 5-lipoxygenase pathway. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID5280492
CHEMBL ID65061
CHEBI ID15647
SCHEMBL ID2510602
MeSH IDM0012426

Synonyms (64)

Synonym
CHEBI:15647 ,
5(s),12(r)-dihydroxy-6(z),8(e),10(e),14(z)-icosatetraenoic acid
5s,12r-dihydroxy-6z,8e,10e,14z-eicosatetraenoic acid
(s-(r*,s*-(e,z,e,z)))-5,12-dihydroxy-6,8,10,14-eicosatetraenoic acid
(5s,12r,6z,8e,10e,14z)-5,12-dihydroxy-6,8,10,14-eicosatetraenoic acid
(5s,6z,8e,10e,12r,14z)-5,12-dihydroxyicosa-6,8,10,14-tetraenoic acid
5,12-hete
(5s,6z,8e,10e,12r,14z)-5,12-dihydroxyeicosa-6,8,10,14-tetraenoic acid
5,12-dihete
5(s),12(r)-dihydroxy-6(z),8(e),10(e),14(z)-eicosatetraenoic acid
6,8,10,14-eicosatetraenoic acid, 5,12-dihydroxy-, (5s,6z,8e,10e,12r,14z)-
6,8,10,14-eicosatetraenoic acid, 5,12-dihydroxy-, (s-(r*,s*-(e,e,z,z)))-
IDI1_033834
BSPBIO_001364
5s,12r-dihete
LMFA03020001
PDSP1_000573
PDSP1_000684
PDSP2_000571
leukotriene b4
71160-24-2
(6z,8e,10e,14z)-(5s,12r)-5,12-dihydroxyicosa-6,8,10,14-tetraenoate
C02165
(6z,8e,10e,14z)-(5s,12r)-5,12-dihydroxyeicosa-6,8,10,14-tetraenoate
ltb4
leukotriene b4, ~100 mug/ml in ethanol, >=97%
NCGC00161273-03
NCGC00161273-02
NCGC00161273-01
PDSP2_000674
NCGC00161273-04
gtpl2487
HMS1989E06
CHEMBL65061 ,
BML1-E04
HMS1361E06
HMS1791E06
bdbm50013889
dihete 12(s), 5(s)
1hgw4dr56d ,
unii-1hgw4dr56d
6,8,10,14-eicosatetraenoicacid, 5,12-dihydroxy-, (5s,6z,8e,10e,12r,14z)-
leukotriene b4 [mi]
AKOS024457041
SCHEMBL2510602
(5s,6z,8e,10e,12r,14z)-5,12-dihydroxy-6,8,10,14-eicosatetraenoic acid
HMS3402E06
mfcd00135630
DTXSID4037162
ltb4 (leukotriene b4)
(6z,8e,10e,14z)-(5s,12r)-5,12-dihydroxyicosa-6,8,10,14-tetraenoic acid
5,12-dihydroxy-6,10-trans -8,14-cis -eicosatetraenoic acid
5,12-dihydroxy-6,10-trans -8,14-cis -eicosatetraenoate
DB12961
101759-15-3
SR-01000946887-1
sr-01000946887
ltb4 (leukotriene b4) is a lipid mediator and leukotriene.
CS-0028956
HY-107608
WCA16024
ltb 4 free acid
STARBLD0009609
leukotriene b4 (ltb4)

Research Excerpts

Overview

Leukotriene B4 (LTB4) is a potent chemoattractant that can recruit and activate immune cells such as neutrophils, eosinophils, and monocytes to sites of inflammation. It is a major proinflammatory mediator that leads to the persistence of chronic inflammation in chronic obstructive pulmonary disease (COPD)

ExcerptReferenceRelevance
"Leukotriene B4 (LTB4) is a potent lipid mediator involved in the recruitment and activation of neutrophils, which is an important feature of tissue injury and inflammation. "( Role of leukotriene B4 (LTB4)-LTB4 receptor 1 signaling in post-incisional nociceptive sensitization and local inflammation in mice.
Asahara, M; Hoshino, Y; Ito, N; Nakamura, M; Sasaki, T; Shimizu, T; Yamada, Y; Yokomizo, T, 2022
)
2.6
"Leukotriene B4 (LTB4) is a potent chemoattractant that can recruit and activate immune cells such as neutrophils, eosinophils, and monocytes to sites of inflammation. "( Discovery of a novel BLT2 antagonist for the treatment of inflammatory airway diseases.
Ahn, KS; Choi, Y; Han, HK; Harmalkar, DS; Kim, JH; Kwon, J; Lee, CH; Lee, JW; Lee, K; Park, H; Park, JM; Song, JG; Sun, S; Wei, JD, 2023
)
2.35
"Leukotriene B4 (LTB4) is a major pro-inflammatory mediator that leads to the persistence of chronic inflammation in chronic obstructive pulmonary disease (COPD). "( Therapeutic potential of BLT1 antagonist for COPD: involvement of inducing autophagy and ameliorating inflammation.
Dong, R; Feng, Y; Huang, J; Zhang, L; Zhou, M, 2019
)
1.96
"Leukotriene B4 (LTB4) is a major type of lipid mediator that is rapidly generated from arachidonic acid through sequential action of 5-lipoxygenase (5-LO), 5-lipoxygenase-activating protein (FLAP) and LTA4 hydrolase (LTA4H) in response to various stimuli. "( The role of the LTB4-BLT1 axis in health and disease.
Cai, Q; Chen, Y; He, R, 2020
)
2
"Leukotriene B4 (LTB4) is a major proinflammatory mediator important in host defense, whereas resolvins (Rvs) are produced during the resolution phase of inflammation. "( Resolvin E1 Reduces Leukotriene B4-Induced Intracellular Calcium Increase and Mucin Secretion in Rat Conjunctival Goblet Cells.
Bair, JA; Dartt, DA; Hodges, RR; Serhan, CN; Yang, M, 2020
)
2.32
"Leukotriene B4 (LTB4) is a highly potent neutrophil chemoattractant and neutrophils induces inflammatory response and oxidative stress when they recruit to and infiltrate in the injuried/inflamed site, such as the brain parenchyma after aneurysmal subarachnoid hemorrhage (SAH). "( Inhibition of leukotriene B4 synthesis protects against early brain injury possibly via reducing the neutrophil-generated inflammatory response and oxidative stress after subarachnoid hemorrhage in rats.
Chen, Q; Hang, CH; Li, W; Liu, JP; Lu, Y; Wu, LY; Xia, DY; Ye, ZN; Zhang, XS; Zhang, ZH; Zhou, ML; Zhuang, Z, 2018
)
2.28
"Leukotriene B4 (LTB4) is a potent chemoattractant and inflammatory mediator involved in multiple inflammatory diseases. "( Substance P-regulated leukotriene B4 production promotes acute pancreatitis-associated lung injury through neutrophil reverse migration.
Chen, C; Dai, J; Han, X; Hu, G; Li, B; Ni, J; Wan, R; Wang, X; Wu, J; Wu, Z; Ye, X, 2018
)
2.24
"Leukotriene B4 (LTB4) is a well-known leukocyte chemoattractant via engagement of its receptor 1 (BLT1)."( BLT1 signaling in epithelial cells mediates allergic sensitization via promotion of IL-33 production.
Chen, Z; Cui, X; Du, L; He, R; Leng, Q; Li, H; Li, W; Lv, J; Mi, W; Xiong, Y; Zhou, H, 2019
)
1.24
"Leukotriene B4 (LTB4) is an important inflammatory component in a number of diseases and has been used as a pharmacodynamic (PD) biomarker. "( A highly sensitive and selective method for the determination of leukotriene B4 (LTB4) in ex vivo stimulated human plasma by ultra fast liquid chromatography-tandem mass spectrometry.
Bertelsen, K; Chen, G; de Jong, J; Fourie, A; Huang, MQ; Lin, W; Lin, ZJ; Weng, N; Xue, X; Zhao, H, 2013
)
2.07
"Leukotriene B4 (LTB4) is a potent mediator of inflammation and has been recognized as an important target for therapeutic intervention for treatment of diseases such as asthma. "( Quantitation of leukotriene B(4) in human sputum as a biomarker using UPLC-MS/MS.
Edom, RW; Fourie, A; Huang, MQ; Jian, W; Weng, N; Xue, X, 2013
)
1.83
"Leukotriene B4 (LTB4) is an endogenous lipid mediator of inflammation derived from arachidonic acid by the sequential action of cytosolic phospholipase A2 and 5-lipoxygenase. "( Leukotriene B4, an endogenous stimulator of the innate immune response against pathogens.
Brunet, A; Gosselin, J; Le Bel, M, 2014
)
3.29
"Leukotriene B4 (LTB4) is a chemotactic mediator implicated in the pathogenesis of asthma. "( Effects of JNJ-40929837, a leukotriene A4 hydrolase inhibitor, in a bronchial allergen challenge model of asthma.
Barchuk, W; Barnathan, ES; Bertelsen, K; Fourie, A; Fuhr, R; Jiang, JZ; Lambert, J; Liu, X; Silkoff, PE; Thurmond, R, 2014
)
1.85
"Leukotriene B4 (LTB4) is a proinflammatory lipid mediator that elicits eosinophil exocytosis, leading to allergic inflammation. "( NOX2-derived ROS-mediated surface translocation of BLT1 is essential for exocytosis in human eosinophils induced by LTB4.
El-Benna, J; Kim, KA; Lee, YA; Min, A; Shin, MH, 2014
)
1.85
"Leukotriene B4 (LTB4) is a potent inflammatory mediator derived from arachidonic acid. "( Two distinct leukotriene B4 receptors, BLT1 and BLT2.
Yokomizo, T, 2015
)
2.23
"Leukotriene B4 (LTB₄) is an important disease marker, but its role in inflammation of the small airways in asthma has not been established yet."( Elevated exhaled leukotriene B₄ in the small airway compartment in children with asthma.
Könitzer, S; Korten, I; Lex, C; Müller, CM; Prell, E; Trischler, J; Unverzagt, S, 2015
)
1.14
"Leukotriene B4 (LTB4 ) is a lipid mediator that is rapidly generated in inflammatory sites, and its functional receptor, BLT1, is mostly expressed on immune cells. "( Leukotriene B₄-leukotriene B₄ receptor axis promotes oxazolone-induced contact dermatitis by directing skin homing of neutrophils and CD8⁺ T cells.
He, R; Li, B; Lv, J; Xiong, Y; Yang, W; Zhao, L; Zou, L, 2015
)
1.86
"Leukotriene B4 (LTB4) is a potent mediator of inflammation and plays a key function in the pathophysiology of chronic asthma. "( Determination of urinary levels of leukotriene B(4) using ad highly specific and sensitive methodology based on automatic MEPS combined with UHPLC-PDA analysis.
Câmara, JS; Perestrelo, R; Silva, CL, 2015
)
1.86
"Leukotriene B4 (LTB4) is a potent pro-inflammatory eicosanoid that is derived from arachidonic acid, and its signaling is known to have a tumor-promoting role in several cancer types. "( The proinflammatory LTB4/BLT1 signal axis confers resistance to TGF-β1-induced growth inhibition by targeting Smad3 linker region.
Choi, J; Jeon, WK; Jo, EJ; Kim, BC; Kim, JH; Kim, SJ; Lee, YK; Letterio, JJ; Lim, S; Liu, F; Park, SJ, 2015
)
1.86
"1. Leukotriene B4 (LTB4) is a proinflammatory mediator important in the progression of a number of inflammatory diseases. "( Leveraging model-based study designs and serial micro-sampling techniques to understand the oral pharmacokinetics of the potent LTB4 inhibitor, CP-105696, for mouse pharmacology studies.
Bagrodia, S; Chung, H; Ellies, LG; Fantin, VR; Gernhardt, S; Spilker, ME; Visswanathan, R, 2017
)
1.08
"Leukotriene B4 is a proinflammatory lipid mediator whose role in peripheral nociceptive sensitization is not well understood to date."( The leukotriene B4 receptors BLT1 and BLT2 form an antagonistic sensitizing system in peripheral sensory neurons.
Angioni, C; DeBruin, N; Ferreiros, N; Geisslinger, G; Jordan, H; Kern, K; Leffler, A; Offermanns, S; Pierre, S; Scholich, K; Sisignano, M; Suo, J; Treutlein, EM; Tunaru, S; Zinn, S, 2017
)
1.73
"Leukotriene B4 (LTB4) is a potent inflammatory mediator that also stimulates the immune response. "( Leukotriene B4-loaded microspheres: a new therapeutic strategy to modulate cell activation.
Faccioli, LH; Jose, PJ; Nicolete, R; Piqueras, L; Rius, C; Sanz, MJ; Soares, EG; Sorgi, CA, 2008
)
3.23
"Leukotriene B4 (LTB4) is a powerful chemoattractant and pro-inflammatory mediator in several inflammatory diseases, including atherosclerosis. "( Leukotriene B4 enhances the activity of nuclear factor-kappaB pathway through BLT1 and BLT2 receptors in atherosclerosis.
Blanco-Colio, LM; Egido, J; Gómez-Hernández, A; Martín-Ventura, JL; Muñoz-García, B; Ortega, L; Sánchez-Galán, E; Tuñón, J; Vidal, C, 2009
)
3.24
"Leukotriene B4 (LTB4) is an inflammatory mediator with potent biological activities in the pathogenesis of many inflammatory diseases. "( Pro-survival of estrogen receptor-negative breast cancer cells is regulated by a BLT2-reactive oxygen species-linked signaling pathway.
Choi, JA; Kim, EY; Kim, H; Kim, JH; Ko, J; Lee, JW; Seo, JM, 2010
)
1.8
"Leukotriene B4 (LTB4) is an effective polymorphonuclear neutrophil (PMN) chemoattractant, as well as being a major product of PMN priming."( Leukotriene b4 and its metabolites prime the neutrophil oxidase and induce proinflammatory activation of human pulmonary microvascular endothelial cells.
Banerjee, A; Elzi, DJ; Eun, JC; Kelher, MR; Khan, SY; McLaughlin, NJ; Moore, EE; Silliman, CC, 2011
)
2.53
"Leukotriene B4 (LTB4) is a bioactive eicosanoid and macrophage and has two key enzymes for LTB4 synthesis, 5-lipoxygenase and leukotriene A4 (LTA4) hydrolase."( Role of leukotriene B4 in accelerated hyperlipidaemic renal injury.
Doi, K; Fujita, T; Hamasaki, Y; Nakao, A; Noiri, E; Nosaka, K; Shimizu, T; Suzuki, T; Toda, A, 2011
)
1.52
"Leukotriene B4 (LTB(4)) is a potent inflammatory mediator in asthma, and is increased in more severe asthma. "( The efficacy and tolerability of MK-0633, a 5-lipoxygenase inhibitor, in chronic asthma.
de Tilleghem, Cle B; Hanley, WD; Knorr, BA; Reiss, TF; Smugar, SS; Villarán, C; Wasfi, YS, 2012
)
1.82
"Leukotriene B4 (LTB4) is a potent chemotactic agent and activating factor for granulocytes. "( Leukotriene B4 receptors.
Shimizu, T; Toda, A; Yokomizo, T, 2002
)
3.2
"Leukotriene B4 (LTB4) is a potent chemoattractant for neutrophils and is thought to play a role in a variety of inflammatory responses in humans. "( Urinary metabolites of leukotriene B4 in the human subject.
Berry, KA; Borgeat, P; Flamand, L; Gosselin, J; Murphy, RC, 2003
)
2.07
"Leukotriene B4 (LTB4) is a potent chemoattractant for myeloid leukocytes, which express BLT1, the high-affinity receptor for LTB4. "( Leukotriene B4 and BLT1 control cytotoxic effector T cell recruitment to inflamed tissues.
Goodarzi, K; Goodarzi, M; Luster, AD; Tager, AM; von Andrian, UH, 2003
)
3.2
"Leukotriene B4 (LTB4) is a potent leukocyte chemoattractant, acting on specific receptors, BLT receptors. "( The contractile action of leukotriene B4 in the guinea-pig lung involves a vascular component.
Bäck, M; Dahlén, SE; Sakata, K, 2004
)
2.07
"Leukotriene B4 (LTB4) is a potent lipid mediator of inflammation that acts primarily via a seven-transmembrane-spanning, G-protein-coupled receptor denoted BLT1. "( Fluorescent leukotriene B4: potential applications.
Bristulf, J; Haeggström, JZ; Leffler, H; Owman, C; Sabirsh, A; Wetterholm, A, 2005
)
2.15
"Leukotriene B4 (LTB4) is a potent activator and chemoattractant for leukocytes and is implicated in several inflammatory diseases. "( Leukotriene B4 receptors BLT1 and BLT2: expression and function in human and murine mast cells.
Fourie, AM; Karlsson, L; Lundeen, KA; Sun, B, 2006
)
3.22
"The leukotriene B4-BLT1 pathway is an important target for the treatment of bronchial asthma."( Role of the LTB4/BLT1 pathway in allergen-induced airway hyperresponsiveness and inflammation.
Gelfand, EW; Miyahara, N; Miyahara, S; Takeda, K, 2006
)
0.81
"Leukotriene B4 (LTB4) is a potent primary stimulator of neutrophil chemotaxis, aggregation, and degranulation and induces superoxide production at higher concentrations. "( Enhancement of chemotactic factor-stimulated neutrophil oxidative metabolism by leukotriene B4.
Beckman, JK; Brash, AR; Gay, JC; Lukens, JN; Oates, JA, 1984
)
1.94
"Leukotriene B4 (LTB4) is a potent mediator of inflammation. "( Possible in vivo modulation of the immune system by the leukotriene, LTB4. I. Delayed suppression of cellular immunity.
Ades, EW; Jackson, WT; Myers, MJ; Petersen, BH, 1984
)
1.71
"Leukotriene B4 (LTB4) is a 5, 12-dihydroxy derivative of arachidonic acid generated by a variety of inflammatory cells via the lipoxygenase enzyme system. "( Leukotriene B4: an inflammatory mediator with vascular actions in vivo.
Bray, MA, 1982
)
3.15
"Leukotriene B4 is a highly potent leukocyte chemotactic compound. "( Production of intraepidermal microabscesses by topical application of leukotriene B4.
Brain, S; Camp, R; Greaves, M; Jones, RR; Woollard, P, 1984
)
1.94
"Leukotriene B4 (LTB4) is a lipoxygenase product of arachidonic acid that has potent chemotactic activity for blood leukocytes. "( Leukotriene B4 production by the human alveolar macrophage: a potential mechanism for amplifying inflammation in the lung.
Albert, RK; Altman, LC; Henderson, WR; Martin, TR, 1984
)
3.15
"Leukotriene B4 is a powerful chemoattractant for polymorphonuclear leukocytes, stimulates cellular aggregation, degranulation and the release of lysosomal enzymes."( [Pharmacology of the leukotrienes].
Borgeat, P; Sirois, P, 1984
)
0.99
"Leukotriene B4 (LTB4) is a potent proinflammatory mediator that may be of particular relevance to the pathology of several respiratory diseases. "( Leukotriene B4 in bronchoalveolar lavage fluid of patients with diffuse panbronchiolitis.
Hara, K; Kadota, J; Kohno, S; Oda, H, 1995
)
3.18
"Leukotriene B4 (LTB4) is a potent inflammatory mediator involved in the pathogenesis of many pulmonary diseases. "( Leukotriene B4 formation: human neutrophil-airway epithelial cell interactions.
Leikauf, GD; Stark, JM; Zhou, S, 1995
)
3.18
"Leukotriene B4 (LTB4) is a product of the 5-lipoxygenase pathway of arachidonic acid metabolism. "( Leukotriene B4 plays a critical role in the progression of collagen-induced arthritis.
Breslow, R; Conklyn, MJ; Farrell, CA; Griffiths, RJ; Hackman, BC; Koch, K; Milici, AJ; Pettipher, ER; Smith, MA; Wimberly, DJ, 1995
)
3.18
"Leukotriene B4 (LTB4) is a potent mediator of inflammation generated by polymorphonuclear leukocytes (PMN) in response to an appropriate stimulus. "( Impaired leukotriene B4 release by neonatal polymorphonuclear leukocytes.
Caniglia, M; Ciccimarra, F; Palumbo, A; Romano, G; Santoro, P; Viggiano, D, 1994
)
2.15
"Leukotriene B4 (LTB4) is a potent stimulus for eosinophil accumulation and activation and there is much interest in determining its importance in mediating the accumulation of eosinophils at sites of allergic inflammation in vivo."( Effect of a 5-lipoxygenase inhibitor, ZM 230487, on cutaneous allergic inflammation in the guinea-pig.
Hellewell, PG; Teixeira, MM, 1994
)
1.01
"Leukotriene B4 (LTB4) is a product of arachidonic acid metabolism and a potent chemoattractant for adult polymorphonuclear leukocytes (PMN). "( Neutrophil chemotaxis to leukotriene B4 in vitro is decreased for the human neonate.
Davidson, D; Dos Santos, C, 1993
)
2.03
"Leukotriene B4 (LTB4) is a proinflammatory product of arachidonic acid metabolism that has been implicated as a mediator in a number of inflammatory diseases. "( Leukotriene B4-induced granulocyte trafficking in guinea pig dermis. Effect of second-generation leukotriene B4 receptor antagonists, SC-50605 and SC-51146.
Anglin, CP; Djuric, SW; Fretland, DJ; Penning, TD; Widomski, DL; Yu, S, 1993
)
3.17
"Leukotriene B4 (LTB4) is a product of that pathway which may take part in the pathogenesis of GvHD through the stimulation of T-lymphopoiesis and T-lymphocyte activation."( Dietary fish oil supplementation alters LTB4:LTB5 ratios but does not affect the expression of acute graft versus host disease in mice.
Knaan-Shanzer, S; Kobb, SM; McCrohan, MB; Miller, AM; van Bekkum, DW, 1993
)
1.01
"Leukotriene B4 (LTB4) is a potent neutrophil activator and chemotaxin that is present in increased concentrations in the colonic tissue and rectal dialysates of acute ulcerative colitis patients. "( Oral efficacy of a leukotriene B4 receptor antagonist in colitic cotton-top tamarins.
Adams, L; Carson, R; Clapp, N; Fretland, D; Fuhr, J; Sanderson, T; Smith, P; Tanner, J, 1995
)
2.06
"Leukotriene B4 (LTB4) is a potent chemoattractant and a well-established stimulator of DNA-synthesis in keratinocytes. "( The dynamics of the response of normal skin to single and multiple epicutaneous leukotriene B4 applications analysed by three-colour flow cytometry.
Botermans, RJ; Glade, CP; van de Kerkhof, PC; van Erp, PE, 1995
)
1.96
"Leukotriene B4 (LTB4) is a potent proinflammatory arachidonic acid metabolite whose actions are mediated by specific receptors. "( Leukotriene B4 modulates in vivo expression of delayed-type hypersensitivity by a receptor-mediated mechanism: regulation by lipoxin A4.
Feng, Z; Godfrey, HP; Heilman, E; Lin, KT; Mandy, S; Strudwick, S; Wong, PY, 1996
)
3.18
"Leukotriene B4 is a potent inflammatory mediator that is derived from the 5-lipoxygenase pathway of arachidonic acid metabolism and that has been implicated in the pathophysiology of polymorphonuclear leukocyte-dependent reperfusion injury in a variety of organ systems. "( Ischemia-reperfusion injury in myocutaneous flaps: role of leukocytes and leukotrienes.
Chiao, JJ; Davis, JM; Fantini, GA; Fyfe, BS; Hoffman, LA; Kirschner, RE, 1997
)
1.74
"Leukotriene B4 (LTB4) is an active upregulator of neutrophil CD11b-expression, acts as a potent chemoattractant to neutrophils and is also known to upmodulate epidermal proliferation."( The regulation of CD11b integrin levels on human blood leukocytes and leukotriene B4-stimulated skin by a specific leukotriene B4 receptor antagonist (LY293111).
de Jong, EM; Kuijpers, AL; Marder, P; Mitchell, MI; Spaethe, SM; van de Kerkhof, PC; van Erp, PE; van Hooijdonk, CA; van Pelt, JP, 1997
)
1.25
"Leukotriene B4 (LTB4) is a potent chemoattractant that is primarily involved in inflammation, immune responses and host defence against infection. "( A G-protein-coupled receptor for leukotriene B4 that mediates chemotaxis.
Chang, K; Izumi, T; Shimizu, T; Takuwa, Y; Yokomizo, T, 1997
)
2.02
"Leukotriene B4 (LTB4) is a potent lipid mediator of inflammation and is involved in the receptor-mediated activation of a number of leukocyte responses including degranulation, superoxide formation, and chemotaxis. "( Leukotriene B4 stimulates the release of arachidonate in human neutrophils via the action of cytosolic phospholipase A2.
Burke, JR; Davern, LB; Gregor, KR; Tramposch, KM, 1997
)
3.18
"Leukotriene B4 (LTB4) is a product of the 5-lipoxygenase pathway of arachidonic acid (AA) metabolism. "( Involvement of leukotriene B4 in murine dermatitis models.
Horiuchi, M; Mita, S; Miyake, Y; Tsuji, F, 1998
)
2.1
"Leukotriene B4 (LTB4) is a chemotactic factor for neutrophils."( Role of leukotriene B4 in bronchial hyperresponsiveness induced by interleukin-8.
Fujimura, M; Matsuda, T; Matsushima, K; Myou, S; Tachibana, H; Tsujiura, M; Xiu, Q, 1998
)
1.46
"Leukotriene B4 is a pro-inflammatory mediator synthesised in myeloid cells from arachidonic acid. "( Leukotriene B4.
Crooks, SW; Stockley, RA, 1998
)
3.19
"Leukotriene B4 (LTB4) is a potent lipid mediator of the inflammatory response whose biological half-life is believed to be mediated principally by metabolism to inactive forms either in the tissue of origin or in the liver. "( Metabolic transformations of leukotriene B4 in primary cultures of human hepatocytes.
Bilir, B; Guenette, D; Hankin, JA; Murphy, RC; Wheelan, P, 1999
)
2.04
"Leukotriene B4 (LTB4) is a potent chemoattractant derived from arachidonic acid. "( Characterization of the leukotriene B4 receptor in porcine leukocytes. Separation and reconstitution with heterotrimeric GTP-binding proteins.
Igarashi, T; Izumi, T; Shimizu, T; Taketani, Y; Tsutsumi, O; Yokomizo, T, 1999
)
2.05
"Leukotriene B4 (LTB4) is a potent mediator of inflammation that recruits granulocytes to the site of injury during the inflammatory response. "( Effect of peroxisome proliferator-activated receptor alpha activation on leukotriene B4 metabolism in isolated rat hepatocytes.
Fiedler, J; Iwahashi, M; Murphy, RC; Simon, FR, 2001
)
1.98
"Leukotriene B4 (LTB4) is a potent chemotactic agent that activates monocytes through the LTB4 receptor (BLTR). "( Leukotriene B4 receptor antagonism reduces monocytic foam cells in mice.
Aiello, RJ; Bourassa, PA; Freeman, A; Lindsey, S; Showell, HJ; Weng, W, 2002
)
3.2
"Leukotriene B4 (LTB4) is a potent lipid inflammatory mediator which induces IL-2 and interferon-gamma (IFN-gamma) production from T cells."( Leukotriene B4 augments interleukin-2 receptor-beta (IL-2R beta) expression and IL-2R beta-mediated cytotoxic response in human peripheral blood lymphocytes.
Gagnon, N; Rola-Pleszczynski, M; Stanková, J, 1992
)
2.45
"Leukotriene B4 (LTB4) is a potent lipid mediator of inflammation, and some of its bioactivities may involve inflammatory cytokines. "( Leukotriene B4 enhances interleukin-6 (IL-6) production and IL-6 messenger RNA accumulation in human monocytes in vitro: transcriptional and posttranscriptional mechanisms.
Rola-Pleszczynski, M; Stanková, J, 1992
)
3.17
"Leukotriene B4 (LTB4) is a notable participant in inflammation and chemotaxis. "( Leukotriene B4 transcriptionally activates interleukin-6 expression involving NK-chi B and NF-IL6.
Arnold, C; Brach, MA; de Vos, S; Gruss, HJ; Herrmann, F; Mertelsmann, R, 1992
)
3.17
"Leukotriene B4 (LTB4) is a naturally occurring eicosanoid mediator which chemoattracts and stimulates human neutrophils to an activated state. "( Flow cytometric evaluation of the effects of leukotriene B4 receptor antagonists (LY255283 and SC-41930) on calcium mobilization and integrin expression of activated human neutrophils.
Herron, DK; Marder, P; Schultz, RM; Sofia, MJ; Spaethe, SM, 1992
)
1.99
"Leukotriene B4 (LTB4) is a proinflammatory product of arachidonic acid metabolism that has been implicated in a number of inflammatory diseases. "( Optical isomers of a leukotriene B4 antagonist have differential effects on granulocyte diapedesis in the guinea pig dermis.
Anglin, CP; Djuric, SW; Fretland, DJ; Widomski, DL; Yu, S, 1992
)
2.05
"Leukotriene B4 is a potent lipid mediator of inflammation, and some of its bioactivities may involve inflammatory cytokines. "( Interleukin 6 production by mononuclear phagocytes can be stimulated by leukotrienes.
Rola-Pleszczynski, M; Stanková, J, 1992
)
1.73
"Leukotriene B4 (LTB4) is a potent chemotactic compound for neutrophils and is thought to be an important mediator of myocardial ischemia-reflow injury. "( Gas chromatographic-mass spectrometric analysis of lipoxygenase products in post-ischemic rabbit myocardium.
Gentry, DL; Hughes, H; McGuire, GM; Taylor, AA, 1991
)
1.72
"Leukotriene B4 (LTB4) is an arachidonic acid lipoxygenase metabolite with well-characterized effects on leukocytes. "( Effects of leukotrienes on osteoblastic cell proliferation.
Dziak, R; Ren, W, 1991
)
1.72
"Leukotriene B4 (LTB4) is a major mediator of leukocyte activation in acute inflammatory reactions, which produce chemotaxis, lysosomal enzyme release, and cell aggregation."( Leukocyte inhibitory factor activates human neutrophils and macrophages to release leukotriene B4 and thromboxanes.
Barbacane, RC; Bongrazio, M; Borish, L; Conti, P; Dempsey, R; Fiore, S; Panara, MR; Reale, M, 1990
)
1.23
"Leukotriene B4 (LTB4) is a pro-inflammatory arachidonate metabolite. "( Transition of affinity states for leukotriene B4 receptors in sheep lung membranes.
Mong, S; Votta, B, 1990
)
2
"Leukotriene B4 is a lipoxygenase metabolite of arachidonic acid."( Leukotriene B4 release and polymorphonuclear cell infiltration in spinal cord injury.
Hogan, EL; Hsu, CY; Liu, TH; Perot, PL; Tai, HH; Xu, JA, 1990
)
2.44
"Leukotriene B4 (LTB4) is an arachidonate metabolite which elicits a variety of pro-inflammatory responses by activation of a guanine-nucleotide-binding protein-coupled membrane receptor. "( Characterization of the soluble leukotriene B4 receptor from sheep lung membranes.
Keefer, J; Mong, S; Votta, B, 1990
)
2.01
"Leukotriene B4 is thought to be a prominent proinflammatory mediator in these diseases, in that leukotriene B4 levels are increased in the colonic mucosa of inflammatory bowel disease patients and there is increased polymorphonuclear leukocyte infiltration of these tissues."( Effect of the leukotriene B4 receptor antagonist SC-41930 on colonic inflammation in rat, guinea pig and rabbit.
Djuric, SW; Fretland, DJ; Gaginella, TS; Levin, S; Shone, RL; Tsai, BS; Widomski, D; Zemaitis, JM, 1990
)
1.36
"Leukotriene B4 (LTB4) is a derivative of arachidonic acid which causes neutrophil diapedesis, endothelial swelling and increased permeability of post-capillary venules. "( Leukocyte diapedesis and plasma extravasation after leukotriene B4: lack of structural injury to the endothelium.
Hedqvist, P; Lindbom, L; Thureson-Klein, A, 1986
)
1.96
"Leukotriene B4 (LTB4) is a potent stimulus for neutrophil chemotaxis, aggregation, and activation. "( Generation of leukotriene B4 by human lung fragments and purified human lung mast cells.
Freeland, HS; Lichtenstein, LM; Peters, SP; Schleimer, RP; Schulman, ES, 1988
)
2.08
"Leukotriene B4 (LTB4) is a potent chemotactic and chemokinetic substance that causes leukocyte accumulation and increases vascular permeability. "( Leukotriene B4-induced permeability increase in postcapillary venules and its inhibition by three different antiinflammatory drugs.
Bergqvist, D; Erlansson, M; Svensjö, E, 1989
)
3.16
"Leukotriene B4 (LTB4) is a potent chemotactic agent formed via the 5-lipoxygenase pathway from arachidonic acid. "( Quantitation of leukotriene B4 in human serum by negative ion gas chromatography-mass spectrometry.
Gaskell, SJ; Hughes, H; Mitchell, JR, 1989
)
2.07
"Leukotriene B4 (LTB4) is an activator of white blood cells (WBC) and it has been suggested that its inhibition may be useful in rheumatoid arthritis (RA). "( Leukotriene b4 production by peripheral blood neutrophils in rheumatoid arthritis.
Ansell, D; Belch, JJ; O'Dowd, A; Sturrock, RD, 1989
)
3.16
"Leukotriene B4 (LTB4) is a proinflammatory product of arachidonic acid metabolism that has been implicated as a mediator in a number of inflammatory diseases. "( Effect of a leukotriene B4 receptor antagonist on leukotriene B4-induced neutrophil chemotaxis in cavine dermis.
Djurić, SW; Fretland, DJ; Shone, RL; Widomski, DL; Zemaitis, JM, 1989
)
2.1
"Leukotriene B4 (LTB4) is a major product of human alveolar macrophages and has potent chemotactic activity for neutrophils (PMN) in vitro. "( Effects of leukotriene B4 in the human lung. Recruitment of neutrophils into the alveolar spaces without a change in protein permeability.
Chi, EY; Goodman, RB; Martin, TR; Matthay, MA; Pistorese, BP, 1989
)
2.11
"Leukotriene B4 (LTB4) is a potent chemotactic factor for polymorphonuclear leukocytes. "( Effects of smoking on the synthesis of leukotriene B4 by rat alveolar macrophages.
Izumi, T; Kitamura, S; Ohishi, N; Shimizu, T; Sugiyama, Y; Takaku, F; Yotsumoto, H, 1989
)
1.99
"Leukotriene B4 (LTB4) is a potent chemoattractant for neutrophils and its topical application to human skin has already been performed without serious side effects, forming intraepidermal neutrophil abscesses."( The treatment of tinea with topically applied leukotriene B4.
Katayama, H, 1987
)
1.25
"Leukotriene B4 appears to be an important inflammatory mediator for the activation of macrophages in colonic inflammation."( Inhibition of intestinal macrophage chemotaxis to leukotriene B4 by sulphasalazine, olsalazine, and 5-aminosalicylic acid.
Elmgreen, J; Nielsen, OH; Verspaget, HW, 1988
)
1.25
"Leukotriene B4 (LTB4) is a potent chemoattractant for polymorphonuclear leukocytes in humans in vivo."( Leukotriene B4 produces hyperalgesia in humans.
Bisgaard, H; Kristensen, JK, 1985
)
2.43
"Leukotriene B4 (LTB4) is a metabolite of arachidonic acid that has potent chemotactic activity for polymorphonuclear leukocytes (PMN). "( The role of leukotriene B4 in the genesis of oxygen toxicity in the lung.
Ozawa, T; Satake, T; Sugiyama, S; Takagi, K; Taki, F; Taniguchi, H, 1986
)
2.09

Effects

Leukotriene B4 (LTB4) has been associated with the initiation and progression of atherosclerosis and abdominal aortic aneurysm (AAA) formation. The molecule has chemotactic properties for activated T cells expressing the high-affinity receptor BLT(1)

ExcerptReferenceRelevance
"Leukotriene B4 (LTB(4)) has a key role in the pathophysiology of rheumatoid arthritis (RA)."( Inhibition of leukotriene B4-induced CD11B/CD18 (Mac-1) expression by BIIL 284, a new long acting LTB4 receptor antagonist, in patients with rheumatoid arthritis.
Alten, R; Emmerich, J; Gromnica-Ihle, E; Pohl, C; Roscher, R; Schmolke, B; Sigmund, R; Steffgen, J; Steinmann, G, 2004
)
2.13
"Leukotriene B4 has recently been identified as a key molecule in lymphedema pathogenesis."( Dietary supplements in lymphedema.
Bertelli, M; Bonetti, G; Cestari, M; Dhuli, K; Michelini, S; Ricci, M, 2022
)
1.44
"Leukotriene B4 (LTB4) has been proved to play an essential role in the induction of pain and bone damage."( Pain and bone damage in rheumatoid arthritis: role of leukotriene B4.
Hong, FF; Li, KX; Yang, SL; Zheng, LX,
)
1.1
"Leukotriene B4 (LTB4) has been implicated in the pathogenesis of allergic diseases. "( Leukotriene B4 receptor BLT2 negatively regulates allergic airway eosinophilia.
Asai, Y; Fukuyama, S; Inoue, H; Kubo, M; Machida, K; Matsumoto, K; Matsunaga, Y; Matsunobu, T; Nakanishi, Y; Oike, M; Okuno, T; Sadamura, Y; Saeki, K; Sasaki, F; Yokomizo, T, 2013
)
3.28
"Leukotriene B4 (LTB4) has been associated with the initiation and progression of atherosclerosis and abdominal aortic aneurysm (AAA) formation. "( Leukotriene B4 levels in human atherosclerotic plaques and abdominal aortic aneurysms.
Bovens, SM; de Borst, GJ; de Kleijn, DP; de Vries, JP; Hoefer, IE; Koole, D; Kowala, MC; Michael, LF; Moll, FL; Pasterkamp, G; Quax, PH; Schoneveld, AH; van de Weg, SM; van den Borne, P; van der Laan, SW; Velema, E, 2014
)
3.29
"Leukotriene B4 (LTB(4) ) has chemotactic properties for activated T cells expressing the high-affinity receptor BLT(1) . "( Blockade of LTB(4) /BLT(1) pathway improves CD8(+) T-cell-mediated colitis.
Boschetti, G; Durand, PY; Flourie, B; Furhmann, L; Hacini, F; Kaiserlian, D; Le Borgne, M; Nancey, S; Sardi, F, 2011
)
1.81
"Leukotriene B4 (LTB4) has been implicated in prostate and colon carcinogenesis, but little is known about the potential role of LTB4 in celecoxib-mediated anticancer effect."( Role of leukotriene B4 in celecoxib-mediated anticancer effect.
Gao, P; Guan, L; Zheng, J, 2010
)
1.52
"Leukotriene B4 (LTB4) has been implicated in the trafficking of monocytes to inflammatory pathologic conditions, such as transplant rejection and atherosclerosis. "( Mechanisms of leukotriene B4--triggered monocyte adhesion.
Friedrich, EB; Gerszten, RE; Liu, E; Luster, AD; Munn, L; Owman, C; Pettersson, A; Tager, AM, 2003
)
2.12
"Leukotriene B4 (LTB(4)) has a key role in the pathophysiology of rheumatoid arthritis (RA)."( Inhibition of leukotriene B4-induced CD11B/CD18 (Mac-1) expression by BIIL 284, a new long acting LTB4 receptor antagonist, in patients with rheumatoid arthritis.
Alten, R; Emmerich, J; Gromnica-Ihle, E; Pohl, C; Roscher, R; Schmolke, B; Sigmund, R; Steffgen, J; Steinmann, G, 2004
)
2.13
"Leukotriene B4 (LTB4) has been detected by radioimmunoassay in inflammatory exudates obtained following the implantation of saline- or carrageenan-soaked polyester sponges in rats. "( The release of leukotriene B4 during experimental inflammation.
Moncada, S; Salmon, JA; Simmons, PM, 1983
)
2.06
"Leukotriene B4 (LTB4) (I) has been converted to its N-(3-amino-propyl)amide derivative (III) and to its hydrazide derivative (VII) via LTB4 delta-lactone. "( Studies on the conjugation of leukotriene B4 with proteins for development of a radioimmunoassay for leukotriene B4.
Rokach, J; Young, RN; Zamboni, R, 1983
)
2
"Leukotriene B4 (LTB4) has been reported to promote the formation of lung oedema when infused into the pulmonary circulation of adult animals. "( Oxygen-induced lung injury in the pre-term guinea pig: the role of leukotriene B4.
Kelly, FJ; Mohammed, W; Phillips, GJ, 1995
)
1.97
"Leukotriene B4 (LTB4) has been proposed as a local mediator of this process; its production is susceptible to specific modulation with dietary eicosapentaenoic acid (EPA)."( Eicosapentaenoic acid in cystic fibrosis: evidence of a pathogenetic role for leukotriene B4.
Lawrence, R; Sorrell, T, 1993
)
1.24
"Leukotriene B4 (LTB4) has been shown to affect several interleukin (IL)-linked functions of human lymphocytes. "( Leukotriene B4 induces interleukin 5 generation from human T lymphocytes.
Kolb, JP; Yamaoka, KA, 1993
)
3.17
"Leukotriene B4 has also been demonstrated to stimulate or inhibit osteoblastic cell proliferation, depending on the cell type tested."( Regulation of C-myc protooncogene expression in osteoblastic cells by arachidonic acid metabolites: relationship to proliferation.
Dziak, R; Kinniburgh, AJ; Ren, W, 1992
)
1
"Leukotriene B4 has been found to be increased in the serum of cigarette smokers and some patients with bronchial asthma, as well as in the sputum of patients with cystic fibrosis and COPD. "( Serum leukotriene B4 levels in patients with obstructive pulmonary disease.
Edes, TE; Seggev, JS; Thornton, WH, 1991
)
2.2
"Leukotriene B4 (LTB4) has been implicated as a mediator in the inflammatory process by virtue of its potent chemotactic activity. "( Disappearance and metabolism of leukotriene B4 during carrageenan-induced pleurisy.
Sun, FF; Taylor, BM, 1985
)
2
"Leukotriene B4 has potent effects on leukocyte function and in vivo induces leukocyte accumulation and changes in vascular permeability and modulates pain responses."( Biological actions of leukotrienes. State of the art lecture.
Ford-Hutchinson, A; Letts, G, 1986
)
0.99
"Leukotriene B4 (LTB4) has been shown to modulate lymphocyte responses in both a positive and a negative way, depending on the particular cell subsets it interacts with. "( Identification of interferon-gamma as the lymphokine that mediates leukotriene B4-induced immunoregulation.
Bouvrette, L; Gingras, D; Girard, M; Rola-Pleszczynski, M, 1987
)
1.95

Actions

Leukotriene B4 (LTB4) plays an important role in acute and chronic inflammatory and hypersensitive reactions. It promotes leukocyte adhesion to the vascular endothelium, with subsequent diapedesis and migration in the extravascular space.

ExcerptReferenceRelevance
"Leukotriene B4 specifically promotes leukocyte adhesion to the vascular endothelium, with subsequent diapedesis and further migration in the extravascular space."( Leukotrienes B4 and C4 have distinct microcirculatory actions in vivo.
Arfors, KE; Björk, J; Dahlén, SE; Hedqvist, P, 1983
)
0.99
"Leukotriene B4 was found to cause a rapid release of membrane-bound calcium at physiologically relevant concentrations."( Mechanism of action of leukotriene B4: intracellular calcium redistribution in rabbit neutrophils.
Borgeat, P; Molski, TF; Naccache, PH; Sha'afi, RI, 1984
)
1.3
"Leukotriene B4 (LTB4) plays an important role in acute and chronic inflammatory and hypersensitive reactions. "( Generation of leukotriene B4 by hemodialyzer membranes: a novel index of biocompatibility.
Schiffl, H; Strasser, T, 1991
)
2.08

Treatment

Leukotriene B4 treatment of cultured endothelium increases the binding of lymphocytes to endothelial cell monolayers within minutes. Pretreatment with leukotrie B4 deactivates rabbit neutrophils.

ExcerptReferenceRelevance
"Leukotriene B4 treatment of cultured endothelium increases the binding of lymphocytes to endothelial cell monolayers within minutes."( Leukotriene B4 increases the lymphocyte binding to endothelial cells.
Häyry, P; Leszczynski, D; Mattila, P; Renkonen, R, 1988
)
2.44
"Pretreatment with leukotriene B4 deactivates rabbit neutrophils, i.e., cells so treated do not respond to stimulation by an additional bolus of leukotriene B4."( Characterization of the secretory activity of leukotriene B4 toward rabbit neutrophils.
Becker, EL; Borgeat, P; Naccache, PH; Picard, S; Sha'afi, RI; Showell, HJ; Vallerand, P, 1982
)
0.85

Toxicity

ExcerptReferenceRelevance
" It is concluded that repeated dose inhalation exposure of small numbers of animals is a useful mode of exposure for studying parameters that may elucidate toxic effects of air pollutants emitted from automotive engines, with a possibility to evaluate engine and fuel with regard to health hazards."( Short-term exposure of rodents to diesel exhausts: usefulness for studies of genotoxic and immunotoxic effects.
Hedenskog, M; Helleberg, H; Kautiainen, A; Nilsen, A; Nilsen, OG; Rannug, U; Törnqvist, M; Trønnes, T; Westerholm, R, 1999
)
0.3
" The better GI tolerability of meloxicam was also suggested by fewer adverse GI events and no withdrawals due to adverse events compared with piroxicam."( Endoscopic comparison of the gastroduodenal safety and the effects on arachidonic acid products between meloxicam and piroxicam in the treatment of osteoarthritis.
Chang, DM; Hsieh, TC; Hsu, CT; Kuo, SY; Young, TH, 2001
)
0.31
"Nonsteroidal anti-inflammatory drugs (NSAIDs) are associated with a risk of serious adverse events."( Anti-inflammatory effects and gastrointestinal safety of NNU-hdpa, a novel dual COX/5-LOX inhibitor.
Ao, GZ; He, SY; Ju, M; Liu, F; Xu, GL; Xue, T; Zhao, Y, 2009
)
0.35
"There was no clear difference in adverse events between placebo and active drug-treated subjects in either study."( Pharmacodynamics, pharmacokinetics and safety of GSK2190915, a novel oral anti-inflammatory 5-lipoxygenase-activating protein inhibitor.
Ambery, C; Bain, G; Bentley, J; Evans, JF; Hutchinson, JH; King, CD; Norris, V; Rewolinski, M; Santini, AM; Schaab, K; Stock, N; van de Wetering de Rooij, J; Yamada, M; Zunic, J, 2013
)
0.39
" However, ICIs are associated with immune-related adverse events involving cardiotoxicity."( NLRP3 as Putative Marker of Ipilimumab-Induced Cardiotoxicity in the Presence of Hyperglycemia in Estrogen-Responsive and Triple-Negative Breast Cancer Cells.
Berretta, M; Bonelli, A; Botti, G; Caronna, A; Cocco, S; Conforti, G; De Laurentiis, M; Lombari, MC; Maurea, N; Quagliariello, V; Rea, G, 2020
)
0.56

Pharmacokinetics

The drug is an inhibitor of leukotriene A4 hydrolase. Production of LTB4 provides a direct measure of the pharmacodynamic (PD) response to acebilustat treatment.

ExcerptReferenceRelevance
" Pharmacokinetics of MK-0591 were linear, with a half-life of approximately 6 hours."( Pharmacokinetics and pharmacodynamics of multiple oral doses of MK-0591, a 5-lipoxygenase-activating protein inhibitor.
Dallob, A; de Lepeleire, I; de Schepper, PJ; Depré, M; Friedman, B; Lin, C; Porras, A; Shingo, S; Tanaka, W; Van Hecken, A, 1994
)
0.29
" Population pharmacokinetic analysis with NONMEM showed plasma concentration-time profiles of AA-2414 to be best characterized by a two-compartment open model with zero-order input and first-order elimination."( Characterization of the pharmacokinetics and pharmacodynamics of a new oral thromboxane A2-receptor antagonist AA-2414 in normal subjects: population analysis.
Granneman, GR; Hussein, Z; Locke, CS; Orchard, MA; Ringham, GL; Samara, E, 1994
)
0.29
" The pharmacokinetic and pharmacodynamic properties of a novel 2-indolealkanoic acid derivative (MK-0591), a potent inhibitor of leukotriene biosynthesis, were investigated in healthy male Japanese volunteers."( Pharmacokinetic and pharmacodynamic analysis of a novel leukotriene biosynthesis inhibitor, MK-0591, in healthy volunteers.
Friedman, BS; Hara, K; Kanamaru, M; Kosuge, K; Nakashima, M; Takenaga, N; Tanaka, W; Uchiyama, N; Uematsu, T, 1995
)
0.29
"The potential pharmacokinetic and pharmacodynamic interactions between zileuton, a 5-lipoxygenase inhibitor, and naproxen, a nonsteroidal anti-inflammatory drug that acts as a cyclo-oxygenase inhibitor, have been investigated in 24 healthy volunteers."( The pharmacokinetic and pharmacodynamic interactions between the 5-lipoxygenase inhibitor zileuton and the cyclo-oxygenase inhibitor naproxen in human volunteers.
Awni, WM; Braeckman, RA; Cavanaugh, JH; Dubé, LM; Granneman, GR; Linnen, PJ; Locke, CS, 1995
)
0.29
" Trough zileuton plasma concentrations (Cmin) immediately before the morning dose were higher than Cmin immediately before the afternoon dose, suggesting a diurnal variation in the pharmacokinetics of zileuton."( Pharmacokinetics and pharmacodynamics of zileuton after oral administration of single and multiple dose regimens of zileuton 600mg in healthy volunteers.
Awni, WM; Braeckman, RA; Dubé, LM; Granneman, GR; Witt, G, 1995
)
0.29
" This method has utility in evaluating the pharmacodynamic action of either LTB(4) receptor antagonists or immune cell modulators in effecting CD11b integrin expression and granulocyte activation in human subjects administered such drugs."( Human granulocyte CD11b expression as a pharmacodynamic biomarker of inflammation.
Carpenter, DC; Davis, HM; Griswold, DE; Hynicka, WP; Stahl, JM; Zhang, W, 2000
)
0.31
" This randomized, partially double-blind, controlled trial was conducted to evaluate the pharmacodynamic effects of the NSAID, ketoprofen (KTP), on gingival crevicular fluid (GCF) prostanoids."( Pharmacodynamic effects of ketoprofen on crevicular fluid prostanoids in adult periodontitis.
Annett, M; Binder, TA; Friedman, M; Lawrence, HP; McCombs, GB; Offenbacher, S; Paquette, DW; Smith, PC; Troullos, E; Wilder, R, 2000
)
0.31
"To summarize the physicochemical characterization, pharmacokinetic behavior, and biological evaluation of P792, a new monogadolinated MRI blood-pool agent."( Physicochemical and biological evaluation of P792, a rapid-clearance blood-pool agent for magnetic resonance imaging.
Bonnemain, B; Corot, C; Dencausse, A; Idee, JM; Lancelot, E; Lautrou, J; Meyer, D; Port, M; Raynal, I, 2001
)
0.31
" The pharmacokinetic and biodistribution profiles were studied in rabbits."( Physicochemical and biological evaluation of P792, a rapid-clearance blood-pool agent for magnetic resonance imaging.
Bonnemain, B; Corot, C; Dencausse, A; Idee, JM; Lancelot, E; Lautrou, J; Meyer, D; Port, M; Raynal, I, 2001
)
0.31
" The pharmacokinetic and biodistribution profiles are consistent with that of a rapid-clearance blood-pool agent: P792 is mainly excreted by glomerular filtration, and its diffusion across normal endothelium is limited."( Physicochemical and biological evaluation of P792, a rapid-clearance blood-pool agent for magnetic resonance imaging.
Bonnemain, B; Corot, C; Dencausse, A; Idee, JM; Lancelot, E; Lautrou, J; Meyer, D; Port, M; Raynal, I, 2001
)
0.31
" The pharmacokinetic and biodistribution profiles are consistent with those of a rapid-clearance blood-pool agent."( Physicochemical and biological evaluation of P792, a rapid-clearance blood-pool agent for magnetic resonance imaging.
Bonnemain, B; Corot, C; Dencausse, A; Idee, JM; Lancelot, E; Lautrou, J; Meyer, D; Port, M; Raynal, I, 2001
)
0.31
"4 mg/kg in a three-period cross-over study incorporating a placebo treatment to establish its pharmacokinetic and pharmacodynamic properties."( Pharmacodynamics and pharmacokinetics of phenylbutazone in calves.
Arifah, AK; Lees, P, 2002
)
0.31
" Pharmacokinetic analyses indicated that fasting plasma GLA and EPA levels plateaued within 7 days' daily consumption at all levels of intake, whereas the time to maximum plasma concentration (Tmax) was shorter for GLA than for EPA."( Inhibition of leukotriene synthesis, pharmacokinetics, and tolerability of a novel dietary fatty acid formulation in healthy adult subjects.
Chilton, FH; Edens, MB; Koumenis, IL; Surette, ME; Tramposch, KM, 2003
)
0.32
" First, a model capable of dealing with the nonlinearity in its pharmacokinetic profile was built, and then it was combined with a pharmacodynamic model previously established with data from earlier phase I trials."( Dealing with time-dependent pharmacokinetics during the early clinical development of a new leukotriene B4 synthesis inhibitor.
Antonijoan, RM; Barbanoj, MJ; Garrido, MJ; Trocóniz, IF; Valle, M; Zsolt, I, 2006
)
0.55
"RBx 7796, a 5-lipoxygenase inhibitor, was evaluated in in vivo efficacy models, in vitro ADME and in vivo pharmacokinetic models."( Pharmacodynamic and pharmacokinetic characterisation of RBx 7796: a novel 5-lipoxygenase inhibitor.
Dastidar, SG; Kakar, S; Paliwal, JK; Ray, A; Salman, M; Sattigeri, V; Sharma, P; Shirumalla, RK; Singh Saini, G; Varshney, B, 2008
)
0.35
" Pharmacokinetic profile of RBx 7796 was also determined in rat and dog."( Pharmacodynamic and pharmacokinetic characterisation of RBx 7796: a novel 5-lipoxygenase inhibitor.
Dastidar, SG; Kakar, S; Paliwal, JK; Ray, A; Salman, M; Sattigeri, V; Sharma, P; Shirumalla, RK; Singh Saini, G; Varshney, B, 2008
)
0.35
" The molecule also demonstrated acceptable pharmacokinetic profile warranting further development."( Pharmacodynamic and pharmacokinetic characterisation of RBx 7796: a novel 5-lipoxygenase inhibitor.
Dastidar, SG; Kakar, S; Paliwal, JK; Ray, A; Salman, M; Sattigeri, V; Sharma, P; Shirumalla, RK; Singh Saini, G; Varshney, B, 2008
)
0.35
" After multiple-dose administration (50-1,000 mg once daily for 11 days), there were no significant differences in the pharmacokinetic parameters between the first and last days of treatment."( Pharmacodynamics and pharmacokinetics of AM103, a novel inhibitor of 5-lipoxygenase-activating protein (FLAP).
Arruda, JM; Bain, G; Evans, JF; Hutchinson, JH; King, CD; Li, Y; Lorrain, DS; Milne, GL; Moran, M; Prasit, P; Rewolinski, M; Roffel, AF; Santini, AM; Schaab, K; Schuilenga-Hut, P; Shapiro, D; van de Wetering de Rooij, S, 2010
)
0.36
" Blood samples were collected for GSK2190915 concentrations and blood and urine were collected to measure leukotriene B₄ and leukotriene E₄, respectively, as pharmacodynamic markers of drug activity."( Pharmacodynamics, pharmacokinetics and safety of GSK2190915, a novel oral anti-inflammatory 5-lipoxygenase-activating protein inhibitor.
Ambery, C; Bain, G; Bentley, J; Evans, JF; Hutchinson, JH; King, CD; Norris, V; Rewolinski, M; Santini, AM; Schaab, K; Stock, N; van de Wetering de Rooij, J; Yamada, M; Zunic, J, 2013
)
0.39
" Maximum plasma concentrations of GSK2190915 and area under the curve increased in a dose-related manner and mean half-life values ranged from 16-34 h."( Pharmacodynamics, pharmacokinetics and safety of GSK2190915, a novel oral anti-inflammatory 5-lipoxygenase-activating protein inhibitor.
Ambery, C; Bain, G; Bentley, J; Evans, JF; Hutchinson, JH; King, CD; Norris, V; Rewolinski, M; Santini, AM; Schaab, K; Stock, N; van de Wetering de Rooij, J; Yamada, M; Zunic, J, 2013
)
0.39
" It is an inhibitor of leukotriene A4 hydrolase; therefore, production of leukotriene B4 (LTB4) in biological fluids provides a direct measure of the pharmacodynamic (PD) response to acebilustat treatment."( Phase I Studies of Acebilustat: Pharmacokinetics, Pharmacodynamics, Food Effect, and CYP3A Induction.
Ahuja, S; Bhatt, L; Elborn, JS; Grosswald, R; Springman, EB, 2017
)
0.69

Compound-Compound Interactions

The study aimed to retrospectively analyze the effects of halometasone cream combined with Simiao pill on the efficacy and expression of serum leukotriene B4 (LTB4) and thymic stromal lymphopoietin (TSLP) in patients with eczema.

ExcerptReferenceRelevance
"The effect of intradermal injection of leukotriene B4 alone and in combination with prostaglandin D2 and E2 and the effect of inhaled leukotriene B4 in combination with prostaglandin D2 were studied in six non-asthmatic men."( Effect of inhaled leukotriene B4 alone and in combination with prostaglandin D2 on bronchial responsiveness to histamine in normal subjects.
Barnes, PJ; Black, PN; Dollery, CT; Fuller, RW; Taylor, GW, 1989
)
0.88
" They expand our knowledge of the effects of AF on PMN cells, whereby reducing effects on intracellular ATP were observed with AF alone and stimulating effects in combination with LTB4."( Auranofin and its combination with LTB4 influences ATP level and migration of human polymorphonuclear cells in vitro.
Matucci-Cerinic, M; Partsch, G, 1995
)
0.29
" In this study an ultra-fast, selective and sensitive analytical method based on semi-automatic microextraction by packed sorbents (MEPS) technique, using a new digitally controlled syringe (eVol®) combined with ultra-high pressure liquid chromatography (UHPLC), is proposed for the measurement of urinary LTB4 (U-LTB4) levels in a group of asthmatic patients (APs) and healthy controls (CTRL)."( Determination of urinary levels of leukotriene B(4) using ad highly specific and sensitive methodology based on automatic MEPS combined with UHPLC-PDA analysis.
Câmara, JS; Perestrelo, R; Silva, CL, 2015
)
0.42
" This study aimed to retrospectively analyze the effects of halometasone cream combined with Simiao pill on the efficacy and expression of serum leukotriene B4 (LTB4) and thymic stromal lymphopoietin (TSLP) in patients with eczema, and identify the factors influencing its clinical efficacy."( Effect of halometasone cream combined with Simiao pill on the therapeutic effect and expression of serum leukotriene B4 (LTB4) and thymic stromal lymphopoietin (TSLP) in patients with eczema, and the factors influencing its clinical efficacy.
Cao, J; Ding, XJ; Liu, H, 2021
)
1.04
"We retrospectively collected the medical records of 195 patients with chronic eczema treated in the dermatology department from January 2020 to May 2021, and divided them into two groups according to medication: 98 cases were treated with halometasone cream (control group) and 97 cases were treated with halometasone ointment combined with Simiao pill (observation group)."( Effect of halometasone cream combined with Simiao pill on the therapeutic effect and expression of serum leukotriene B4 (LTB4) and thymic stromal lymphopoietin (TSLP) in patients with eczema, and the factors influencing its clinical efficacy.
Cao, J; Ding, XJ; Liu, H, 2021
)
0.84
"Simiao pill combined with halometasone cream can effectively improve chronic eczema and enhance the clinical efficacy of treatment, which may be related to the reduction of serum LTB4 and TSLP levels."( Effect of halometasone cream combined with Simiao pill on the therapeutic effect and expression of serum leukotriene B4 (LTB4) and thymic stromal lymphopoietin (TSLP) in patients with eczema, and the factors influencing its clinical efficacy.
Cao, J; Ding, XJ; Liu, H, 2021
)
0.84

Bioavailability

ExcerptReferenceRelevance
" Oral nafazatrom is ineffective as a 5-lipoxygenase inhibitor in man, probably because of poor bioavailability after administration."( Oral nafazatrom in man: effect on inhaled antigen challenge.
Dollery, CT; Fuller, RW; Maltby, N; Philipp, E; Richmond, R; Ritter, W; Taylor, GW, 1987
)
0.27
" In addition, the compound exhibits excellent bioavailability in dogs and monkeys with a relatively long elimination half-life in both the species (6 and 3 h, respectively)."( The properties of A-69412: a small hydrophilic 5-lipoxygenase inhibitor.
Bell, RL; Bouska, J; Brooks, DW; Carter, GW; Lanni, C; Machinist, J; Malo, PE; Summers, JB; Young, PR, 1993
)
0.29
" Absolute bioavailability of the parent compound was 50%."( A prodrug of a 2,6-disubstituted 4-(2-arylethenyl)phenol is a selective and orally active 5-lipoxygenase inhibitor.
Farina, PR; Graham, AG; Gundel, RH; Hattox, SE; Homon, CA; Lazer, ES; Riska, PS; Wegner, CD, 1993
)
0.29
" The parent compound 4 is a selective, orally bioavailable 5-LO inhibitor which can serve as a useful reference standard for in vivo pharmacological studies involving leukotriene-mediated phenonmena."( 5-Lipoxygenase inhibitors: synthesis and structure-activity relationships of a series of 1-aryl-2H,4H-tetrahydro-1,2,4-triazin-3-ones.
Basha, A; Bell, RL; Bhatia, PA; Bouska, JB; Brooks, CD; Carter, GW; Gunn, BP; Lanni, C; Ratajczyk, JD; Young, PR, 1996
)
0.29
" Bioavailability of a suspension formulation in rats was less than 1%, but increased to approximately 9% when administered as a 20% soybean oil-in-water emulsion."( Lipid-based delivery systems for improving the bioavailability and lymphatic transport of a poorly water-soluble LTB4 inhibitor.
Ficorilli, JV; Fogal, SE; Hauss, DJ; Jayaraj, AA; Keirns, JJ; Price, CA; Roy, T, 1998
)
0.3
" Preliminary pharmacokinetic evaluation in rat and cynomolgus monkey demonstrated good oral bioavailability and elimination half-lives of 9 and 5 h, respectively."( Symmetrical bis(heteroarylmethoxyphenyl)alkylcarboxylic acids as inhibitors of leukotriene biosynthesis.
Basha, A; Bell, RL; Bhatia, P; Bouska, JB; Brooks, CD; Carter, GW; Craig, RA; Gunn, DE; Harris, RR; Hulkower, KI; Kolasa, T; Malo, PE; Stewart, AO, 2000
)
0.31
" After oral dosage bioavailability (F) was 66%."( Pharmacodynamics and pharmacokinetics of phenylbutazone in calves.
Arifah, AK; Lees, P, 2002
)
0.31
" Relative bioavailability was independent of the decrease in the amount of enzyme."( Dealing with time-dependent pharmacokinetics during the early clinical development of a new leukotriene B4 synthesis inhibitor.
Antonijoan, RM; Barbanoj, MJ; Garrido, MJ; Trocóniz, IF; Valle, M; Zsolt, I, 2006
)
0.55
" The oral bioavailability of RBx 7796 in rat and dog was 83 % and 47 %, respectively."( Pharmacodynamic and pharmacokinetic characterisation of RBx 7796: a novel 5-lipoxygenase inhibitor.
Dastidar, SG; Kakar, S; Paliwal, JK; Ray, A; Salman, M; Sattigeri, V; Sharma, P; Shirumalla, RK; Singh Saini, G; Varshney, B, 2008
)
0.35
" Oral bioavailability as determined in rats was 66%."( Discovery of (2-fluoro-benzyl)-(2-methyl-2-phenethyl-2H-chromen-6-yl)-amine (KRH-102140) as an orally active 5-lipoxygenase inhibitor with activity in murine inflammation models.
Cheon, HG; Cho, YS; Gong, YD; Huh, JY; Kim, CH; Song, JS, 2011
)
0.37
"The effects of bioavailability and metabolic transformation on the biological activities of daidzein are relatively unknown."( Relative Inhibitions of 5-Lipoxygenase and Myeloperoxidase and Free-Radical Scavenging Activities of Daidzein, Dihydrodaidzein, and Equol.
Loke, WM; Tan, XY; Tan, YM; Tsen, SY; Yan, BY, 2016
)
0.43

Dosage Studied

Dose-response relationship between aerosolized leukotriene B4 (LTB4) and pulmonary neutrohilia was examined in a group of five rhesus monkeys. PGF-A enhanced both mucous glycoprotein release and the 5- and 15-lipoxygenation of arachidonic acid.

ExcerptRelevanceReference
" Based on dose-response experiments, the relative rank order of potency for the three chemoattractants was: LTB4 = FMLP greater than PAF for filter alone barrier; LTB4 greater than FMLP greater than PAF for HUVE cell barrier; and FMLP greater than LTB4 greater than PAF for MDCK and A549 epithelial cell barriers."( Degree of neutrophil chemotaxis is dependent upon the chemoattractant and barrier.
Abbas, MK; Carolan, EJ; Casale, TB, 1992
)
0.28
" In the rat 4f inhibited LTB4 synthesis in blood ex vivo and in zymosan-inflamed air pouch exudate with an ED50 3 h after oral dosing of 10 mg/kg in each system."( Methoxytetrahydropyrans. A new series of selective and orally potent 5-lipoxygenase inhibitors.
Bird, TG; Bruneau, P; Crawley, GC; Dowell, RI; Edwards, PN; Foster, SJ; Giroaeau, JM; McMillan, RM; Walker, ER; Waterson, D, 1992
)
0.28
" LTB4 induced an accumulation of IL-6 messenger RNA (mRNA) in treated monocytes with a dose-response similar to that of IL-6 protein production."( Leukotriene B4 enhances interleukin-6 (IL-6) production and IL-6 messenger RNA accumulation in human monocytes in vitro: transcriptional and posttranscriptional mechanisms.
Rola-Pleszczynski, M; Stanková, J, 1992
)
1.73
" Whereas IL-1 alpha and IL-1 beta significantly inhibited pentagastrin-stimulated acid secretion, the dose-response relationship and time course of actions suggested that effects on acid secretion did not fully account for the ability of these agents to reduce indomethacin-induced gastric injury."( Mechanisms underlying the protective effects of interleukin 1 in experimental nonsteroidal anti-inflammatory drug gastropathy.
Cucala, M; Keenan, CM; Mugridge, KG; Parente, L; Wallace, JL, 1992
)
0.28
" In this regard a low dosage of methylprednisolone is equally effective as the most often recommended high dose."( Methylprednisolone prophylaxis protects against endotoxin-induced death in rabbits.
Hoiting, BH; Jansen, NJ; van Oeveren, W; Wildevuur, CR, 1991
)
0.28
" An intradermal dose-response study showed that rIL-8 is an extremely potent inducer of selective neutrophil infiltration in canine skin."( Recombinant human interleukin-8 is a potent activator of canine neutrophil aggregation, migration, and leukotriene B4 biosynthesis.
Ahnfelt-Rønne, I; Kirstein, D; Larsen, CG; Skak-Nielsen, T; Thestrup-Pedersen, K; Thomsen, HK; Thomsen, MK, 1991
)
0.5
" Compounds from this series also were found to inhibit the in vivo production of LTB4 when dosed orally in rats."( Styrylpyrazoles, styrylisoxazoles, and styrylisothiazoles. Novel 5-lipoxygenase and cyclooxygenase inhibitors.
Belliotti, TR; Boctor, AM; Connor, DT; Flynn, DL; Kostlan, CR; Nies, DE; Ortwine, DF; Schrier, DJ; Sircar, JC, 1991
)
0.28
" Dose-response experiments (1-100 nM) indicated that at equimolar LTB4 concentrations neutrophil migration across endothelium was two- to threefold greater than that observed across filters alone and the three epithelial barriers."( Comparison of leukotriene B4-induced neutrophil migration through different cellular barriers.
Abbas, MK; Casale, TB, 1990
)
0.64
" With immunological activation of passively sensitized cells, histamine and PGD2 release had similar dose-response characteristics, but TXB2, LTC4, LTD4, and LTE4 release differed in reaching maximum at 50 micrograms/ml and declining at 125 micrograms/ml anti-human IgE."( The immunoglobulin E- and calcium-dependent release of histamine and eicosanoids from human dispersed mastocytosis spleen cells.
Agius, RM; Benyon, RC; Holgate, ST; Jones, DB; Robinson, C; Wright, DH, 1988
)
0.27
" At concentrations lacking agonist activity U-75302 was an effective antagonist, displacing the LTB4 dose-response curve."( Receptor antagonism of leukotriene B4 myotropic activity by the 2,6 disubstituted pyridine analog U-75302: characterization on lung parenchyma strips.
Fitzpatrick, FA; Lawson, CF; Morris, J; Wishka, DG,
)
0.44
" The slopes of the dose-response regression lines were similar for the three drugs."( Mechanism of action of colchicine. VI: Effect of colchicine on generation of leukotriene B4 by human polymorphonuclear leukocytes.
Bhuta, S; Chang, YH; Ouyang, Y; Wang, W,
)
0.36
" Dose-response curves for chemotaxis in Boyden chambers were analysed for sensitivity to leukotriene B4 (LTB4), its 20-hydroxy-LTB4 (20-OH-LTB4) and 20-carboxy-LTB4 (20-COOH-LTB4) catabolites, and 5- and 15-hydroxyeicosatetraenoic acids (HETEs)."( Activation of neutrophil chemotaxis by leukotriene B4 and 5-hydroxyeicosatetraenoic acid in chronic inflammatory bowel disease.
Elmgreen, J; Nielsen, OH, 1987
)
0.76
" An inverse relationship was found between the dosage of etretinate and the number of infiltrating polymorphonuclear leukocytes."( Etretinate modulates the leukotriene B4 induced intra-epidermal accumulation of polymorphonuclear leukocytes.
Lammers, AM; van de Kerkhof, PC, 1987
)
0.58
" Second, the dose-response curve for thromboxane A2, based on the amount of thromboxane B2 generated by lung strips contracted with leukotriene B4, was inconsistent with dose-response curves for lung strips contracted with a stable thromboxane A2 mimetic, U-46619 or with synthetic thromboxane A2 itself."( Myotropic activity of leukotriene B4 on lung parenchyma strips is not necessarily attributable to thromboxane A2 release.
Fitzpatrick, FA; Lawson, CF, 1988
)
0.79
" Neither dosage of leukotriene D4 significantly affected lymphatic pressure."( Effects of bolus injections of leukotrienes and norepinephrine on forelimb vascular and lymphatic pressures.
Buehn, MJ; Dabney, JM; Dobbins, DE, 1988
)
0.27
" The LxA4 dose-response curve was parallel to that of leukotriene D4 (LTD4) with LxA4 being approximately 10,000 fold less potent than LTD4."( The contractile activities of lipoxin A4 and lipoxin B4 for guinea-pig airway tissues.
Crea, AE; Jacques, CA; Lee, TH; Spur, BW, 1988
)
0.27
" LTB4 alone caused an increase in serum thromboxane B2 (TxB2) from 130 +/- 35 to 320 +/- 17 pg/ml 3 minutes after dosing but did not increase TxB2 following pre-treatment with meclofenamate."( Meclofenamate blocks the pulmonary arterial vasopressor effects of leukotriene B4 in awake sheep.
Lefferts, PL; Miller, RF; Purvis, AW; Snapper, JR, 1988
)
0.51
" Incubation of the neutrophils with cholera toxin, unlike pertussis toxin, did not inhibit the fMet-Leu-Phe induced rise in the intracellular concentration of free calcium, and caused only a shift to the right of the dose-response curve of N-acetyl-beta-glucosaminidase release."( Pertussis but not cholera toxin inhibits the stimulated increase in actin association with the cytoskeleton in rabbit neutrophils: role of the "G proteins" in stimulus-response coupling.
Becker, EL; Feinstein, MB; Molski, TF; Munoz, JJ; Naccache, PH; Sha'afi, RI; Shefcyk, J; Volpi, M; Yassin, R, 1985
)
0.27
" In the presence of 10(-4) acetylsalicylic acid (ASA), cumulative dose-response curves of phasic and tonic contractions for LTC4 were shifted to the right of controls, whereas curves of the phasic motility for LTD4 remained unaltered."( On the inotropic effects of leukotrienes in the isolated urinary bladder of guinea pigs and rats.
Chaud, MA; Gimeno, AL; Gimeno, MF; Viggiano, JM, 1985
)
0.27
" The leukotriene-generating response of monolayers of human monocytes pretreated with cytochalasin B to FMLP is receptor-mediated, as indicated by the inactivity of the structural analog N-acetyl-methionyl-leucyl-phenylalanine and by the capacity of the FMLP receptor antagonist carbobenzoxyphenylalanyl-methionine to inhibit the agonist action of FMLP in a dose-response fashion."( Generation of leukotrienes by human monocytes pretreated with cytochalasin B and stimulated with formyl-methionyl-leucyl-phenylalanine.
Austen, KF; Lee, TH; Lewis, RA; Robin, JL; Williams, JD, 1986
)
0.27
" The dose-response effect of all of these drugs on Ig production was similar to the dose response of inhibition of 5-lipoxygenase."( Mechanism of action of glucocorticoid-induced immunoglobulin production: role of lipoxygenase metabolites of arachidonic acid.
Atluru, D; Goodwin, JS, 1986
)
0.27
" Leukotriene B4 release approached a maximum around 30 min, and C6 dose-response studies performed at 1 h showed that maximal levels of leukotriene B4 were detected over a range of sublytic C5b-9 attack."( Release of leukotriene B4 from sublethally injured oligodendrocytes by terminal complement complexes.
Imagawa, DK; Shin, ML; Shirazi, Y, 1987
)
1.57
"12 to 80 microM) for 1 to 60 min at 37 degrees C to construct dose-response and time-dependence curves of lipoxygenase product generation."( Enhanced 5-lipoxygenase activity in lung macrophages compared to monocytes from normal subjects.
Bigby, TD; Holtzman, MJ, 1987
)
0.27
" The myeloid-differentiated HL60 cells respond to LTB4 by raising their [Ca2+]i with a dose-response relationship similar to that shown by normal human neutrophils."( Leukotriene B4 stimulation of phagocytes results in the formation of inositol 1,4,5-trisphosphate. A second messenger for Ca2+ mobilization.
Andersson, T; Krause, KH; Lew, DP; Monod, A; Schlegel, W; Stendahl, O, 1986
)
1.71
" Dose-response curves indicated variations in the sensitivity of monocytes and granulocytes to these mediators."( Stimulated mobilization of monocyte Mac-1 and p150,95 adhesion proteins from an intracellular vesicular compartment to the cell surface.
Bainton, DF; Borregaard, N; Miller, LJ; Springer, TA, 1987
)
0.27
" Leukotrienes, the chemotactic fragment of the fifth component of complement (C5a des arg), N-formyl-L-methionylyl-L-leucyl-L-phenylalanine (FMLP), platelet-activating factor (PAF), and phorbol myristate acetate (PMA) increased the nonadherence of human leukocytes to glass with bell-shaped dose-response curves."( Various authentic chemoattractants mediating leukocyte adherence inhibition.
Thomson, DM, 1984
)
0.27
" Furthermore, the dose-response curve of the generation of phosphatidic acid by fMet-Leu-Phe is shifted to the right when compared with that for calcium mobilization."( Leukotriene B4 mobilizes calcium without the breakdown of polyphosphoinositides and the production of phosphatidic acid in rabbit neutrophils.
Molski, TF; Naccache, PH; Sha'afi, RI; Tao, W; Volpi, M; Yassin, R, 1984
)
1.71
" PGF-A enhanced both mucous glycoprotein release and the 5- and 15-lipoxygenation of arachidonic acid as well as the formation of leukotriene B4 (LTB4) with similar dose-response relationships."( Prostaglandin-generating factor of anaphylaxis induces mucous glycoprotein release and the formation of lipoxygenase products of arachidonate from human airways.
Goetzl, EJ; Kaliner, M; Marom, Z; Shelhamer, JH; Steel, L, 1984
)
0.47
" Inhibition of LTB4-formation and cell migration by BW755C was dose-related, but the two dose-response curves were not parallel."( The effects of BW755C and other anti-inflammatory drugs on eicosanoid concentrations and leukocyte accumulation in experimentally-induced acute inflammation.
Moncada, S; Salmon, JA; Simmons, PM, 1983
)
0.27
" The parallel dose-response relationship for the antigen-induced release of the performed mediator and the generation of both leukotrienes along with the superimposable time courses of their extracellular appearance indicate the origin of these mediators from a common cell type with IgE receptors."( Immunologic and ionophore-induced generation of leukotriene B4 from mouse bone marrow-derived mast cells.
Austen, KF; Corey, EJ; Hoover, D; Lewis, RA; Mencia-Huerta, JM; Razin, E; Ringel, EW, 1983
)
0.52
" Cumulative administrations of leukotrienes desensitized the lung strip, whereas non-cumulative dose-response relationships for the leukotrienes and histamine were reasonably parallel."( Mechanisms of leukotriene-induced contractions of guinea pig airways: leukotriene C4 has a potent direct action whereas leukotriene B4 acts indirectly.
Dahlén, SE; Granström, E; Hammarström, S; Hedqvist, P; Lindgren, JA; Rådmark, O; Westlund, P, 1983
)
0.47
" The parallel antigen-induced dose-response relationship, along with the superimposable time-course of the extracellular appearance, of beta-hexosaminidase, PAF-acether, and both leukotrienes indicated that the origin of these diverse mediators was from a common cell type with IgE-Fc receptors."( Antigen-initiated release of platelet-activating factor (PAF-acether) from mouse bone marrow-derived mast cells sensitized with monoclonal IgE.
Austen, KF; Lewis, RA; Mencia-Huerta, JM; Razin, E, 1983
)
0.27
" Dose-response curves have shown that the enzyme release proceeded in parallel with increments in cyclic AMP, suggesting a linkage between cyclic AMP and leukotriene B4-induced leukocyte activation."( Relationship of cyclic-AMP levels in leukotriene B4-stimulated leukocytes to lysosomal enzyme release and the generation of superoxide anions.
Claesson, HE; Feinmark, SJ, 1984
)
0.74
" Further studies indicated that monocyte binding to endothelial cells follows similar dose-response kinetics as the up-regulation of integrins and can be partially blocked by Abs to CD11b and CD11c."( Regulation of monocyte integrin expression by beta-family chemokines.
Newton, RC; Vaddi, K, 1994
)
0.29
" VIP was mitogenic to keratinocytes at concentrations as low as 10(-12)M and exhibited a different dose-response curve depending on whether adult or newborn keratinocytes were used."( Neuropeptides modulate leukotriene B4 mitogenicity toward cultured human keratinocytes.
Farber, EM; Rabier, MJ; Wilkinson, DI, 1993
)
0.6
" Dose-response analysis revealed that maximal reduction of IL-1 binding was reached at FMLP concentrations that were also optimal for chemotaxis (50% effective dose = 5 x 10(-9) M)."( Chemoattractants induce rapid release of the interleukin 1 type II decoy receptor in human polymorphonuclear cells.
Colotta, F; Fadlon, EJ; Mantovani, A; Matteucci, C; Orlando, S; Sozzani, S, 1995
)
0.29
" Allergen inhalation challenge was performed four hours after dosing and FEV1 was measured for eight hours."( Effect of the 5-lipoxygenase inhibitor ZD2138 on allergen-induced early and late asthmatic responses.
Arm, JP; Bell, GS; Hawksworth, RJ; Lee, TH; MacMillan, R; Nasser, SM; Spruce, KE; Williams, AJ, 1994
)
0.29
" Experiments examining the influence of Promega dosage indicated that the AA/EPA ratio in neutrophil lipids decreased in a dose-dependent manner."( Dietary n-3 fatty acid effects on neutrophil lipid composition and mediator production. Influence of duration and dosage.
Chilton, FH; Fonteh, AN; Hubbard, WC; Patel, M; Triggiani, M, 1993
)
0.29
" Neutrophil infiltration into the antrum was detectable 1 hour after dosing with indomethacin, at which time damage was apparent microscopically but not macroscopically."( Do infiltrating neutrophils contribute to the pathogenesis of indomethacin induced ulceration of the rat gastric antrum?
Clayton, NM; Harman, IW; Strong, P; Trevethick, MA, 1993
)
0.29
" In contrast, it was found that 13-HODE itself induced a decrease in diastolic arterial blood pressure when it was injected intravenously after either a single dose of histamine (10, 100 or 1000 micrograms kg-1) or after a dose-response curve of histamine (0."( Hypotensive effect of 13-hydroxylinoleic acid in the rat: mediation via the release of a CGRP-like mediator from capsaicin-sensitive nerves.
Buckley, TL; Engels, F; Henricks, PA; Muis, T; Nijkamp, FP; van Heuven-Nolsen, D, 1995
)
0.29
"The dose-response relationship between aerosolized leukotriene B4 (LTB4 and pulmonary neutrohilia was examined in a group of five rhesus monkeys."( The effects of LY293111Na, a leukotriene B4 receptor antagonist, on the pulmonary neutrophilia and CD11b expression caused by inhalation of a leukotriene B4 aerosol in rhesus monkeys.
Abbott, DL; Allen, DL; Hoffman, WP; Leiter, PA; Marder, P; Matchett, MR; Wolff, RK, 1996
)
0.84
"05) after dosing with indomethacin."( The effect of indomethacin-induced gastric mucosal injury on 24-h intragastric acidity and plasma gastrin concentration in healthy volunteers.
Chiba, N; Hunt, RH; Johnson, DM; McDonald, TM; Rademaker, JW; Rainsford, KD; Stetsko, PI, 1995
)
0.29
" LXA4, caused an increase in particulate PKC-dependent histone phosphorylating activity with a bell-shaped dose-response fashion; maximal stimulation was observed at 10 nM LXA4."( Stimulation of protein kinase C redistribution and inhibition of leukotriene B4-induced inositol 1,4,5-trisphosphate generation in human neutrophils by lipoxin A4.
Chung-a-on, KO; Lee, TH; Soyombo, O; Spur, BW, 1996
)
0.53
" Although its ability to inhibit the cyclooxygenase pathway was readily observed in whole blood and in vivo, tenidap's 5-LO blockade could not be demonstrated by ionophore stimulated human blood, nor after oral dosing in rat models in which peritoneal leukotriene products were measured after challenge with three different stimuli."( Tenidap inhibits 5-lipoxygenase product formation in vitro, but this activity is not observed in three animal models.
Carty, TJ; Cheng, JD; Ernest, MJ; Eskra, JD; Griffiths, RJ; Joseph, PA; Kadin, SB; Loose, LD; Moore, PF; Murase, S; Nagahisa, A; Pazoles, PP; Pillar, JS; Sweeney, FJ, 1997
)
0.3
" Plasma concentration-time relationships and pharmacokinetic parameters for BAY Y 1015 administered intravenously and orally to six horses at a dosage of 10 mg/kg in a two period cross-over study were established."( Pharmacology of the 5-lipoxygenase inhibitors BAY Y 1015 and BAY X 1005 in the horse.
Andrews, M; Cunningham, FM; Landoni, MF; Lees, P, 1997
)
0.3
" On D28, the patients were randomized into 2 groups: 18 received the drug (fish oil: 30% n-3 PUFA) and 19 received the placebo (olive oil containing only 1% of n-3 PUFA) at a daily dosage of 6 g (i."( Pilot study on n-3 polyunsaturated fatty acids in the treatment of human experimental gingivitis.
Campan, P; Duran, D; Planchand, PO, 1997
)
0.3
" The influence of four beta2-agonists (salbutamol, terbutaline, formoterol, and salmeterol) and a corticosteroid (budesonide) on the release of interleukin-1beta (IL-1beta) and LTB4 was studied in a dose-response manner (10(-8)-10(-5) mol/L for beta2-agonists and 10(-10)-10(-6) mol/ L for budesonide)."( Effects of beta2-agonists and budesonide on interleukin-1beta and leukotriene B4 secretion: studies of human monocytes and alveolar macrophages.
Larsson, K; Linden, M; Zetterlund, A, 1998
)
0.54
" It appears that 325 mg of aspirin is sufficient to affect PGE2 production and that increasing the dosage to 650 mg daily provides an additional decrease in PGE2 synthesis."( Effect of aspirin on prostaglandin E2 and leukotriene B4 production in human colonic mucosa from cancer patients.
Dyavanapalli, M; Frommel, TO; Kazi, N; Liao, Y; Lietz, H; Mobarhan, S; Oldham, T, 1997
)
0.56
" We show that these animals have a decreased hypotension and increased survival rate after administration of a high dosage of lipopolysaccharide."( Endotoxemia in transgenic mice overexpressing human glutathione peroxidases.
Inouye, M; Kister, I; Mirochnitchenko, O; Palnitkar, U; Powell, WS; Prokopenko, O, 2000
)
0.31
" In comparing topical versus systemic formulations, all topical formulations were as equipotent as systemic dosing in altering local prostaglandin levels despite lower KTP exposures with gel treatments."( Pharmacodynamic effects of ketoprofen on crevicular fluid prostanoids in adult periodontitis.
Annett, M; Binder, TA; Friedman, M; Lawrence, HP; McCombs, GB; Offenbacher, S; Paquette, DW; Smith, PC; Troullos, E; Wilder, R, 2000
)
0.31
" dosage was characterized by slow clearance (1."( Pharmacodynamics and pharmacokinetics of phenylbutazone in calves.
Arifah, AK; Lees, P, 2002
)
0.31
" Swiss-Webster mice were dosed with celecoxib and rofecoxib and challenged with CT in ligated small intestinal loops, and intestinal segments from mice deficient in COX-1 and COX-2 were challenged with CT."( Role of cyclooxygenase enzymes in a murine model of experimental cholera.
Boldogh, I; Gessell-Lee, DL; Olano, JP; Peterson, JW; Popov, VL, 2003
)
0.32
" Pinane thromboxane, a selective thromboxane synthase inhibitor and receptor blocker, inhibited OxAA stimulation of TXB(2) and IL-8 in a dose-response manner."( Linoleic acid induces interleukin-8 production by Crohn's human intestinal smooth muscle cells via arachidonic acid metabolites.
Alzoghaibi, MA; Fowler, AA; Graham, MF; Walsh, SW; Willey, A; Yager, DR, 2004
)
0.32
" Oral treatment of quercitrin (1 or 5 mg kg(-1) day(-1)) to colitic rats ameliorated the evolution of the inflammatory process induced when administered in a preventative dosing protocol."( The intestinal anti-inflammatory effect of quercitrin is associated with an inhibition in iNOS expression.
Camuesco, D; Comalada, M; Concha, A; Gálvez, J; Lorente, MD; Nieto, A; Rodríguez-Cabezas, ME; Zarzuelo, A, 2004
)
0.32
"The aim of this study was to explore the possibility of achieving a practical dosing regimen for 2,4,6-triiodophenol (AM-24), a new leukotriene B4 (LTB4) synthesis inhibitor."( Dealing with time-dependent pharmacokinetics during the early clinical development of a new leukotriene B4 synthesis inhibitor.
Antonijoan, RM; Barbanoj, MJ; Garrido, MJ; Trocóniz, IF; Valle, M; Zsolt, I, 2006
)
0.76
"Simulations have shown that steady-state conditions eliciting 90% of maximal LTB4 synthesis inhibition can be reached after 3 weeks during an oral treatment with AM-24 administered at the dosage of 500 mg once daily."( Dealing with time-dependent pharmacokinetics during the early clinical development of a new leukotriene B4 synthesis inhibitor.
Antonijoan, RM; Barbanoj, MJ; Garrido, MJ; Trocóniz, IF; Valle, M; Zsolt, I, 2006
)
0.55
" Platelet aggregation induced by ADP and dosing of prostanoid products 6-keto-PGF1alpha, TXB2, PGE2 and LTB4 were also performed."( Modifications produced by selective inhibitors of cyclooxygenase and ultra low dose aspirin on platelet activity in portal hypertension.
Aguejouf, O; Belon, P; Desplat, V; Doutremepuich, C; Eizayaga, FX, 2007
)
0.34
" After 30 min, 6h, and 24-72 h, the rings were suspended in an organ bath and dose-response curve to methacholine (MCh) were determined."( Connective tissue mast cells are the target of formaldehyde to induce tracheal hyperresponsiveness in rats: putative role of leukotriene B4 and nitric oxide.
Breithaupt-Faloppa, AC; de Oliveira, AP; Domingos, HV; Lino-dos-Santos-Franco, A; Oliveira-Filho, RM; Shia, MK; Tavares-de-Lima, W; Vargaftig, BB, 2010
)
0.57
"We used the forced oscillation technique to test the effects of an LTA(4)H inhibitor dosed during the challenge phase on AHR."( Leukotriene A(4) hydrolase inhibition attenuates allergic airway inflammation and hyperresponsiveness.
Banie, H; Crawford, S; Dunford, PJ; Fourie, AM; Karlsson, L; Lundeen, KA; Rao, NL; Riley, JP; Sun, B; Xue, X; Yu, F, 2010
)
0.36
" This study evaluated the effect of n-3 PUFA in a low, but recommended cardioprotective dosage on the formation of 5-lipoxygenase pathway metabolites in overweight subjects."( The effect of low-dose marine n-3 fatty acids on the biosynthesis of pro-inflammatory 5-lipoxygenase pathway metabolites in overweight subjects: a randomized controlled trial.
Aardestrup, I; Gammelmark, A; Madsen, T; Nielsen, MS; Obel, T; Schmidt, EB, 2012
)
0.38
"To assess the pharmacokinetics, pharmacodynamics, safety and tolerability of the 5-lipoxygenase-activating protein inhibitor, GSK2190915, after oral dosing in two independent phase I studies, one in Western European and one in Japanese subjects, utilizing different formulations."( Pharmacodynamics, pharmacokinetics and safety of GSK2190915, a novel oral anti-inflammatory 5-lipoxygenase-activating protein inhibitor.
Ambery, C; Bain, G; Bentley, J; Evans, JF; Hutchinson, JH; King, CD; Norris, V; Rewolinski, M; Santini, AM; Schaab, K; Stock, N; van de Wetering de Rooij, J; Yamada, M; Zunic, J, 2013
)
0.39
"GSK2190915 is well-tolerated with pharmacokinetics and pharmacodynamics in Western European and Japanese subjects that support once daily dosing for 24 h inhibition of leukotrienes."( Pharmacodynamics, pharmacokinetics and safety of GSK2190915, a novel oral anti-inflammatory 5-lipoxygenase-activating protein inhibitor.
Ambery, C; Bain, G; Bentley, J; Evans, JF; Hutchinson, JH; King, CD; Norris, V; Rewolinski, M; Santini, AM; Schaab, K; Stock, N; van de Wetering de Rooij, J; Yamada, M; Zunic, J, 2013
)
0.39
" AZD8309 (300 mg) or placebo was dosed twice daily orally for 3 days prior to challenge with inhaled LPS and induced sputum was collected 6 h later."( Inhibition of LPS-induced airway neutrophilic inflammation in healthy volunteers with an oral CXCR2 antagonist.
Barnes, PJ; Leaker, BR; O'Connor, B, 2013
)
0.39
" Subjects were dosed with MEM 1414 (600 mg) or placebo, twice daily orally for 7 days."( The effect of the novel phosphodiesterase-4 inhibitor MEM 1414 on the allergen induced responses in mild asthma.
Ali, FY; Barnes, PJ; Leaker, BR; O'Connor, B; Singh, D, 2014
)
0.4
"5 mg/mL DHA solution with the dosage of 1 mL/kg via tail vein 5 minutes post injury, while rats in groups A and C with normal saline solution 1 mL/kg."( [Effects of docosahexaenoic acid on inflammation-associated cytokines in blood and pulmonary tissue of rats with severe scald injury].
Cai, C; Li, X; Xia, Z; Xu, Q; Zhang, J, 2015
)
0.42
" Inflammatory bowel disease was induced by replacing drinking water with 3 % DSS solution during the last 7 d of the AA dosing period."( Effects of arachidonic acid intake on inflammatory reactions in dextran sodium sulphate-induced colitis in rats.
Aoki, S; Furuya, M; Harauma, A; Iwai, N; Ji, X; Miyazawa, D; Moriguchi, T; Nagata, T; Naito, Y; Ohara, N; Tachibana, S; Tazura, Y, 2015
)
0.42
"8 mg/d)and low/medium/high dosage RGDT plaster treating groups(30 mg/d, 60 mg/d, 120 mg/d)."( [The antalgic and antiphiogistic function and mechanism of RGDT plaster].
Chien, XP; Liu, CM; Liu, XX; Tuo, HY; Wang, ZW, 2015
)
0.42
" Daily dosing at 100 mg/kg was not tolerated and resulted in a >20% weight loss in the mice."( Leveraging model-based study designs and serial micro-sampling techniques to understand the oral pharmacokinetics of the potent LTB4 inhibitor, CP-105696, for mouse pharmacology studies.
Bagrodia, S; Chung, H; Ellies, LG; Fantin, VR; Gernhardt, S; Spilker, ME; Visswanathan, R, 2017
)
0.46
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (4)

RoleDescription
human metaboliteAny mammalian metabolite produced during a metabolic reaction in humans (Homo sapiens).
mouse metaboliteAny mammalian metabolite produced during a metabolic reaction in a mouse (Mus musculus).
plant metaboliteAny eukaryotic metabolite produced during a metabolic reaction in plants, the kingdom that include flowering plants, conifers and other gymnosperms.
vasoconstrictor agentDrug used to cause constriction of the blood vessels.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (4)

ClassDescription
dihydroxy monocarboxylic acidAny hydroxy monocarboxylic acid carrying at least two hydroxy groups.
leukotrieneAny icosanoid from that family of C20 polyunsaturated fatty acids and their derivatives generated by leukocytes from arachidonic acid, each member having four double bonds of which three are conjugated.
long-chain fatty acidA fatty acid with a chain length ranging from C13 to C22.
hydroxy polyunsaturated fatty acidAny polyunsaturated fatty acid carrying one or more hydroxy substituents.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Pathways (68)

PathwayProteinsCompounds
Metabolism14961108
Metabolism of lipids500463
Fatty acid metabolism113203
Arachidonic acid metabolism3682
Synthesis of Leukotrienes (LT) and Eoxins (EX)1329
Biological oxidations150276
Phase I - Functionalization of compounds69175
Cytochrome P450 - arranged by substrate type30110
Eicosanoids215
Signaling Pathways1269117
Signaling by GPCR24955
GPCR ligand binding19339
Class A/1 (Rhodopsin-like receptors)16136
Eicosanoid ligand-binding receptors117
Leukotriene receptors31
GPCR downstream signalling17252
G alpha (q) signalling events7928
Arachidonic Acid Metabolism2966
Leukotriene C4 Synthesis Deficiency2966
Piroxicam Action Pathway2967
Acetylsalicylic Acid Action Pathway2967
Etodolac Action Pathway2967
Ketoprofen Action Pathway2967
Ibuprofen Action Pathway5076
Rofecoxib Action Pathway2967
Diclofenac Action Pathway2967
Sulindac Action Pathway2967
Celecoxib Action Pathway3573
Ketorolac Action Pathway2967
Suprofen Action Pathway2967
Bromfenac Action Pathway2967
Indomethacin Action Pathway3067
Mefenamic Acid Action Pathway2967
Oxaprozin Action Pathway2967
Nabumetone Action Pathway2967
Naproxen Action Pathway2967
Diflunisal Action Pathway2967
Meloxicam Action Pathway2967
Valdecoxib Action Pathway2967
Antipyrine Action Pathway2967
Antrafenine Action Pathway2967
Carprofen Action Pathway2967
Etoricoxib Action Pathway2967
Fenoprofen Action Pathway2967
Flurbiprofen Action Pathway2967
Magnesium Salicylate Action Pathway2967
Lumiracoxib Action Pathway2967
Lornoxicam Action Pathway2967
Phenylbutazone Action Pathway2967
Nepafenac Action Pathway2967
Trisalicylate-Choline Action Pathway2967
Tolmetin Action Pathway2967
Tiaprofenic Acid Action Pathway2967
Tenoxicam Action Pathway2967
Salsalate Action Pathway2967
Salicylate-Sodium Action Pathway2967
Salicylic Acid Action Pathway2967
Acetaminophen Action Pathway2967
Prostaglandin and Leukotriene metabolism ( Prostaglandin and Leukotriene metabolism )2223
Eicosanoid metabolism via lipooxygenases (LOX)040
Prostaglandin and leukotriene metabolism in senescence619
Leukotriene metabolic pathway219
Resolvin E1 and resolvin D1 signaling pathways promoting inflammation resolution75
Arachidonic acid (AA, ARA) oxylipin metabolism076
Folic acid network070
Eicosanoid metabolism via lipoxygenases (LOX)040
Selenium micronutrient network095
Eicosanoid synthesis026
Arachidonic acid metabolism via LOX (Lipooxygenase) pathway033

Protein Targets (5)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency7.07950.011212.4002100.0000AID1030
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency3.54810.035520.977089.1251AID504332
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency15.84890.354828.065989.1251AID504847
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Leukotriene B4 receptor 1Homo sapiens (human)IC50 (µMol)0.00190.00080.30913.2500AID102466
Leukotriene B4 receptor 1Homo sapiens (human)Ki0.00220.00010.51267.0000AID102636; AID102647; AID338156
Leukotriene B4 receptor 2Homo sapiens (human)Ki0.00190.00190.12800.5240AID102636
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (10)

Processvia Protein(s)Taxonomy
muscle contractionLeukotriene B4 receptor 1Homo sapiens (human)
inflammatory responseLeukotriene B4 receptor 1Homo sapiens (human)
immune responseLeukotriene B4 receptor 1Homo sapiens (human)
G protein-coupled receptor signaling pathwayLeukotriene B4 receptor 1Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayLeukotriene B4 receptor 1Homo sapiens (human)
leukotriene signaling pathwayLeukotriene B4 receptor 1Homo sapiens (human)
neuropeptide signaling pathwayLeukotriene B4 receptor 1Homo sapiens (human)
chemotaxisLeukotriene B4 receptor 2Homo sapiens (human)
negative regulation of adenylate cyclase activityLeukotriene B4 receptor 2Homo sapiens (human)
keratinocyte migrationLeukotriene B4 receptor 2Homo sapiens (human)
leukotriene signaling pathwayLeukotriene B4 receptor 2Homo sapiens (human)
neuropeptide signaling pathwayLeukotriene B4 receptor 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (4)

Processvia Protein(s)Taxonomy
nucleotide bindingLeukotriene B4 receptor 1Homo sapiens (human)
leukotriene receptor activityLeukotriene B4 receptor 1Homo sapiens (human)
G protein-coupled peptide receptor activityLeukotriene B4 receptor 1Homo sapiens (human)
leukotriene B4 receptor activityLeukotriene B4 receptor 1Homo sapiens (human)
leukotriene receptor activityLeukotriene B4 receptor 2Homo sapiens (human)
leukotriene B4 receptor activityLeukotriene B4 receptor 2Homo sapiens (human)
G protein-coupled peptide receptor activityLeukotriene B4 receptor 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (3)

Processvia Protein(s)Taxonomy
plasma membraneLeukotriene B4 receptor 1Homo sapiens (human)
plasma membraneLeukotriene B4 receptor 1Homo sapiens (human)
nucleoplasmLeukotriene B4 receptor 2Homo sapiens (human)
plasma membraneLeukotriene B4 receptor 2Homo sapiens (human)
membraneLeukotriene B4 receptor 2Homo sapiens (human)
plasma membraneLeukotriene B4 receptor 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (19)

Assay IDTitleYearJournalArticle
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346050Human BLT2 receptor (Leukotriene receptors)2008The Journal of experimental medicine, Apr-14, Volume: 205, Issue:4
12(S)-Hydroxyheptadeca-5Z, 8E, 10E-trienoic acid is a natural ligand for leukotriene B4 receptor 2.
AID1346643Rat TRPV1 (Transient Receptor Potential channels)2000Proceedings of the National Academy of Sciences of the United States of America, May-23, Volume: 97, Issue:11
Direct activation of capsaicin receptors by products of lipoxygenases: endogenous capsaicin-like substances.
AID1346050Human BLT2 receptor (Leukotriene receptors)2000The Journal of experimental medicine, Aug-07, Volume: 192, Issue:3
A second leukotriene B(4) receptor, BLT2. A new therapeutic target in inflammation and immunological disorders.
AID102647Tested for inhibition of specific binding of [3H]LTB4 to human neutrophil expressing LTB4 receptor1993Journal of medicinal chemistry, Nov-26, Volume: 36, Issue:24
Biphenylyl-substituted xanthones: highly potent leukotriene B4 receptor antagonists.
AID102297Binding affinity towards Leukotriene B4 receptor guinea pig lung membrane using [3H]LTB4 as radioligand1995Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22
Synthetic and structure/activity studies on acid-substituted 2-arylphenols: discovery of 2-[2-propyl-3-[3-[2-ethyl-4-(4-fluorophenyl)-5- hydroxyphenoxy]-propoxy]phenoxy]benzoic acid, a high-affinity leukotriene B4 receptor antagonist.
AID1666212Agonist activity at HA-epitope tagged human BLT2 Y271A/N275A double mutant expressed in CHOK1 cells assessed as induction of chemotactic motility at 300 nM incubated for 2 hrs by hematoxylin and eosin staining based optical microscopic method2020ACS medicinal chemistry letters, Aug-13, Volume: 11, Issue:8
Elucidation of Mechanism for Ligand Efficacy at Leukotriene B
AID338193Displacement of [3H]LTB4 from LTB4R assessed as specific binding relative to total binding1993Journal of natural products, Apr, Volume: 56, Issue:4
The role of receptor binding in drug discovery.
AID102636Binding affinity towards human LTB4 receptor measured as inhibition of binding of [3H]LTB4 to isolated human neutrophils1995Journal of medicinal chemistry, Oct-27, Volume: 38, Issue:22
Synthetic and structure/activity studies on acid-substituted 2-arylphenols: discovery of 2-[2-propyl-3-[3-[2-ethyl-4-(4-fluorophenyl)-5- hydroxyphenoxy]-propoxy]phenoxy]benzoic acid, a high-affinity leukotriene B4 receptor antagonist.
AID102301Tested for inhibition of specific binding of [3H]LTB4 to guinea pig lung membranes expressing LTB4 receptor1993Journal of medicinal chemistry, Nov-26, Volume: 36, Issue:24
Biphenylyl-substituted xanthones: highly potent leukotriene B4 receptor antagonists.
AID396465Inhibition of tube formation in human EAhy926 cells at 10 uM pre-incubated for 12 hrs measured after 24 hrs by phase-contrast microscopy2009Bioorganic & medicinal chemistry, Mar-15, Volume: 17, Issue:6
A new antiangiogenic C24 oxylipin from the soft coral Sinularia numerosa.
AID1666211Agonist activity at HA-epitope tagged human BLT2 Y271A mutant expressed in CHOK1 cells assessed as induction of chemotactic motility at 300 nM incubated for 2 hrs by hematoxylin and eosin staining based optical microscopic method2020ACS medicinal chemistry letters, Aug-13, Volume: 11, Issue:8
Elucidation of Mechanism for Ligand Efficacy at Leukotriene B
AID238099In vitro Ka value against human serum albumin; N=12005Bioorganic & medicinal chemistry letters, Aug-15, Volume: 15, Issue:16
In vitro binding of leukotriene B4 (LTB4) to human serum albumin: evidence from spectroscopic, molecular modeling, and competitive displacement studies.
AID1666208Agonist activity at HA-epitope tagged human BLT2 expressed in CHOK1 cells assessed as induction of chemotactic motility at 300 nM incubated for 2 hrs by hematoxylin and eosin staining based optical microscopic method2020ACS medicinal chemistry letters, Aug-13, Volume: 11, Issue:8
Elucidation of Mechanism for Ligand Efficacy at Leukotriene B
AID338156Displacement of [3H]LTB4 from LTB4R1993Journal of natural products, Apr, Volume: 56, Issue:4
The role of receptor binding in drug discovery.
AID102466Inhibition of specific binding of [3H]LTB4 to Leukotriene B4 receptor in human neutrophils1990Journal of medicinal chemistry, Oct, Volume: 33, Issue:10
Benzophenone dicarboxylic acid antagonists of leukotriene B4. 2. Structure-activity relationships of the lipophilic side chain.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (5,718)

TimeframeStudies, This Drug (%)All Drugs %
pre-19901802 (31.51)18.7374
1990's2124 (37.15)18.2507
2000's979 (17.12)29.6817
2010's672 (11.75)24.3611
2020's141 (2.47)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 46.73

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index46.73 (24.57)
Research Supply Index8.72 (2.92)
Research Growth Index4.41 (4.65)
Search Engine Demand Index80.34 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (46.73)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials232 (3.94%)5.53%
Reviews361 (6.13%)6.00%
Case Studies26 (0.44%)4.05%
Observational2 (0.03%)0.25%
Other5,265 (89.45%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]