Inhibition of LTB4 biosynthesis in situ by CGS 23885, a potent 5-lipoxygenase inhibitor, correlates with its pleural fluid concentrations in an experimentally induced rat pleurisy model

@article{Raychaudhuri1997InhibitionOL,
  title={Inhibition of LTB4 biosynthesis in situ by CGS 23885, a potent 5-lipoxygenase inhibitor, correlates with its pleural fluid concentrations in an experimentally induced rat pleurisy model},
  author={Anilbaran Raychaudhuri and Herbert Chertock and James P. Chovan and L S Jones and Earl F. Kimble and Timothy J. Kowalski and Jane V. Peppard and David H. White and Yoshitaka Satoh and Dennis M. Roland},
  journal={Naunyn-Schmiedeberg's Archives of Pharmacology},
  year={1997},
  volume={355},
  pages={470-474}
}
Abstract An intrapleural injection of carrageenan in rats induced LTB4 and LTC4/D4/E4 biosynthesis, exudate formation, and cellular influx in the pleural cavity. An injection of calcium ionophore (A23187, 100nmol) 16–18h after carrageenan injection augmented leukotriene biosynthesis and exudate formation, but not cellular influx. The carrageenan-induced pleurisy model modifid by A23187 administration was used to study the oral effect of CGS 23885 (N-hydroxy-N-[(6-phenoxy-2H-1-benzopyran-3-yl… 

Niacin inhibits carrageenan-induced neutrophil migration in mice

The results suggest that nicotinic acid plays an important role in the regulation of inflammation due to its ability to inhibit the actions of the neutrophil chemoattractants IL-8 and LTB4.

Blockade of proteinase-activated receptor 4 inhibits neutrophil recruitment in experimental inflammation in mice

It is demonstrated that PAR4 blockade impairs neutrophil migration in vivo, suggesting that Par4 plays an important role in the regulation of inflammation, at least in part because of its ability to inhibit the actions of the neutrophIL chemoattractant CXCL8.

Anti-inflammatory and antinociceptive properties of the hydroalcoholic fractions from the leaves of Annona crassiflora Mart. in mice

BackgroundAnnona crassiflora Mart., popularly known as “Araticum”, is a native tree of the Brazilian Cerrado used in folk medicine for treatment of pain and inflammatory diseases. We proposed to

2‐(4‐(Biphenyl‐4‐ylamino)‐6‐chloropyrimidin‐2‐ylthio)octanoic acid (HZ52) – a novel type of 5‐lipoxygenase inhibitor with favourable molecular pharmacology and efficacy in vivo

Assessment of the pharmacological potential of the previously identified 5‐LO inhibitor 2‐(4‐(biphenyl‐4‐ylamino)‐6‐chloropyrimidin‐2‐ylthio)octanoic acid (HZ52) is attempted.

References

SHOWING 1-10 OF 21 REFERENCES

L-663,536 (MK-886) (3-[1-(4-chlorobenzyl)-3-t-butyl-thio-5-isopropylindol-2-yl]-2,2 - dimethylpropanoic acid), a novel, orally active leukotriene biosynthesis inhibitor.

The results indicate that L-663,536 is a potent inhibitor of leukotriene biosynthesis both in vitro and in vivo indicating that the compound is suitable for studying the role ofLeukotrienes in a variety of pathological situations.

Substituted chromenes as potent, orally active 5-lipoxygenase inhibitors.

Ch chromene derivatives synthesized and evaluated for their in vitro and ex vivo 5-lipoxygenase (5-LO) inhibitory activity compare favorably with zileuton (A-64077) in all the parameters examined.

Leukotriene B, a potent chemokinetic and aggregating substance released from polymorphonuclear leukocytes

The chemokinetic and aggregating activities released from rat and human PMNs exposed to ionophore A23187 are not due to the release of mono-HETEs but to that of 5,12-di- HETE (leukotriene B), which is active over the concentration range 10 pg ml−1 to 5 ng ml-1.

Leukotriene B4: an inflammatory mediator in vivo.