Dapsone inhibits LTB4 binding and bioresponse at the cellular and physiologic levels.
Radioligand binding studies using human neutrophils exposed to 10-100 microM dapsone indicated that this anti-inflammatory compound antagonized association of LTB4 (leukotriene B4) with its specific receptor sites. Binding inhibition was manifested in reduced biologic response of the neutrophils as determined in LTB4-stimulated chemotaxis. In addition, a physiologic model of LTB4-dependent inflammation in mice was antagonized by systemic administration of dapsone. These data suggest that inhibition of LTB4 binding may represent the cellular mechanism of action responsible for the anti-inflammatory effects of dapsone.
Maloff
B L
BL
Medical Products Department, E.I. Du Pont de Nemours and Co., Inc., Wilmington, Delaware 19898.
Fox
D
D
Bruin
E
E
Di Meo
T M
TM
D000818:Animals; D002634:Chemotaxis, Leukocyte / Q000187:drug effects; D003622:Dapsone / Q000494:pharmacology*; D005260:Female; D006801:Humans; D066298:In Vitro Techniques; D007249:Inflammation / Q000517:prevention & control; D007975:Leukotriene B4 / Q000378:metabolism*; D051379:Mice; D008807:Mice, Inbred BALB C; D009504:Neutrophils / Q000187:drug effects* / Q000502:physiology; D011971:Receptors, Immunologic / Q000187:drug effects / Q000502:physiology; D018102:Receptors, Leukotriene B4
D011971:Receptors, Immunologic; D018102:Receptors, Leukotriene B4; D007975:Leukotriene B4; D003622:Dapsone