The PAF-acether receptor antagonist BN-52021 inhibits mediator release during guinea-pig active lung anaphylaxis

Pharmacol Res Commun. 1988 Dec;20(12):1047-59. doi: 10.1016/s0031-6989(88)80726-4.

Abstract

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.

MeSH terms

  • Anaphylaxis / immunology
  • Anaphylaxis / metabolism*
  • Animals
  • Diterpenes*
  • Ginkgolides
  • Guinea Pigs
  • Histamine / analysis
  • Histamine Release / drug effects*
  • Kinetics
  • Lactones / pharmacology*
  • Lung / drug effects
  • Lung / metabolism
  • Lung / physiopathology
  • Male
  • Ovalbumin / immunology
  • SRS-A / metabolism*
  • Thromboxane A2 / metabolism
  • Thromboxane B2 / metabolism
  • Thromboxanes / metabolism*

Substances

  • Diterpenes
  • Ginkgolides
  • Lactones
  • SRS-A
  • Thromboxanes
  • Thromboxane B2
  • Thromboxane A2
  • Histamine
  • Ovalbumin
  • ginkgolide B