Pharmacological profiles of a potential LTB4-antagonist, SM-9064.
Antagonistic activity against leukotriene B4 (LTB4) and other pharmacological activities of SM-9064 were studied in vitro and in vivo. It inhibited the chemotaxis of rat polymorphonuclear leukocytes (PMNLs) induced by LTB4 (IC50 = 1.3 X 10(-7) M, not by other chemoattractants. Its agonistic activity was much less than that of LTB4. It suppressed the Arthus reaction-induced inflammation in mice with the dose of 5 mg/kg, i.p. or 10 mg/kg, p.o. These results suggest that SM-9064 is a candidate of LTB4 antagonists, which is effective in some type of inflammation.
D000818:Animals; D002634:Chemotaxis, Leukocyte / Q000187:drug effects*; D005231:Fatty Acids, Unsaturated / Q000494:pharmacology*; D066298:In Vitro Techniques; D007700:Kinetics; D007975:Leukotriene B4 / Q000037:antagonists & inhibitors* / Q000494:pharmacology; D007978:Levamisole / Q000494:pharmacology; D008297:Male; D009240:N-Formylmethionine Leucyl-Phenylalanine / Q000494:pharmacology; D009504:Neutrophils / Q000187:drug effects / Q000502:physiology*; D051381:Rats; D011919:Rats, Inbred Strains; D013329:Structure-Activity Relationship
D005231:Fatty Acids, Unsaturated; C049829:SM 9064; D007975:Leukotriene B4; D007978:Levamisole; D009240:N-Formylmethionine Leucyl-Phenylalanine