Effects of flezelastine and its enantiomers on LPS-induced IL-1 beta generation in vitro and LPS-induced pyrexia in vivo.
The effects of the novel antiasthmatic/antiallergic compound flezelastine on LPS-induced actions were investigated in vitro and in vivo. In monocytes, IL-1 beta generation stimulated by LPS was inhibited dose dependently. In vivo, LPS-induced fever in rats, which is at least partly driven by the release of IL-1 beta, was also inhibited by flezelastine. These findings suggest that flezelastine inhibits IL-1 synthesis and/or release in vitro and in vivo.
Werner
U
U
Department of Pharmacology, ASTA Medica AG, Frankfurt, Germany.
Schmidt
J
J
Szelenyi
I
I
D000818:Animals; D001381:Azepines / Q000008:administration & dosage / Q000494:pharmacology*; D002460:Cell Line; D004305:Dose-Response Relationship, Drug; D005260:Female; D005334:Fever / Q000139:chemically induced / Q000188:drug therapy*; D006634:Histamine H1 Antagonists / Q000494:pharmacology*; D007375:Interleukin-1 / Q000378:metabolism*; D008070:Lipopolysaccharides / Q000633:toxicity*; D009000:Monocytes / Q000187:drug effects* / Q000378:metabolism; D010793:Phthalazines / Q000008:administration & dosage / Q000494:pharmacology*; D051381:Rats; D017207:Rats, Sprague-Dawley; D013237:Stereoisomerism
D001381:Azepines; D006634:Histamine H1 Antagonists; D007375:Interleukin-1; D008070:Lipopolysaccharides; D010793:Phthalazines; C089205:flezelastine