The PAF-acether receptor antagonist BN-52021 inhibits mediator release during guinea-pig active lung anaphylaxis.
An anaphylactic reaction was induced with the specific antigen (1 mg Ovalbumin) in perfused lungs from actively sensitized guinea-pigs in order to evaluate the ability of the ginkgolide BN-52021 (0.4, 4, 40 micrograms/ml) to modulate the mediator release. The ginkgolide reduces in a dose dependent manner the release of histamine (22%, 45% and 75% of inhibition), TXB2 (77% of inhibition at the maximal dose used) and of SRS-A to a lower extent (only 33% at the higher dose). BN-52021 was still powerful in reducing histamine release induced by immunological reaction in indomethacin treated animals. In conclusion, the present "in-vitro" results confirm the beneficial activity of this ginkgolide, already demonstrated by the same Authors in "in-vivo" experiment, in anaphylactic reactions, and further substantiate the wider spectrum of action of the ginkgolide beside its specific PAF receptor antagonistic activity.
Berti
F
F
Institute of Pharmacological Sciences, University of Milan, Italy.
Galli
G
G
Magni
F
F
Rossoni
G
G
Villa
L
L
Puglisi
L
L
Pasargiklian
R
R
Braquet
P
P
D000707:Anaphylaxis / Q000276:immunology / Q000378:metabolism*; D000818:Animals; D004224:Diterpenes; D046934:Ginkgolides; D006168:Guinea Pigs; D006632:Histamine / Q000032:analysis; D006636:Histamine Release / Q000187:drug effects*; D007700:Kinetics; D007783:Lactones / Q000494:pharmacology*; D008168:Lung / Q000187:drug effects / Q000378:metabolism / Q000503:physiopathology; D008297:Male; D010047:Ovalbumin / Q000276:immunology; D013189:SRS-A / Q000378:metabolism*; D013928:Thromboxane A2 / Q000378:metabolism; D013929:Thromboxane B2 / Q000378:metabolism; D013931:Thromboxanes / Q000378:metabolism*
D004224:Diterpenes; D046934:Ginkgolides; D007783:Lactones; D013189:SRS-A; D013931:Thromboxanes; D013929:Thromboxane B2; D013928:Thromboxane A2; D006632:Histamine; D010047:Ovalbumin; C045856:ginkgolide B