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血小板活化因子受体拮抗剂BN - 52021可抑制豚鼠主动性肺过敏反应中的介质释放。

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

作者信息

Berti F, Galli G, Magni F, Rossoni G, Villa L, Puglisi L, Pasargiklian R, Braquet P

机构信息

Institute of Pharmacological Sciences, University of Milan, Italy.

出版信息

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.

摘要

为了评估银杏内酯BN - 52021(0.4、4、40微克/毫升)调节介质释放的能力,在来自主动致敏豚鼠的灌注肺中用特异性抗原(1毫克卵清蛋白)诱导过敏反应。银杏内酯以剂量依赖性方式减少组胺释放(抑制率分别为22%、45%和75%)、TXB2释放(在所用最大剂量下抑制率为77%),对SRS - A的释放抑制程度较低(高剂量时仅为33%)。BN - 52021在减少吲哚美辛处理动物中免疫反应诱导的组胺释放方面仍然有效。总之,目前的“体外”结果证实了该银杏内酯的有益活性,同一作者在“体内”实验中已证明其在过敏反应中的活性,进一步证实了银杏内酯除其特异性PAF受体拮抗活性外更广泛的作用谱。

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BN-52021 protects guinea-pig from heart anaphylaxis.BN - 52021可保护豚鼠免受心脏过敏反应的影响。
Pharmacol Res Commun. 1988 Dec;20 Suppl 5:75-8. doi: 10.1016/s0031-6989(88)80845-2.

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