Magro A M, Hurtado I
J Immunopharmacol. 1983;5(3):191-202. doi: 10.3109/08923978309039105.
Trans-2,3,4,5,7,8b,9,10-octahydronaphtho[1,2-C:5,6-C]dipyrazole (LC-6), which is active in vivo when administered orally, inhibits histamine release from peritoneal rat mast cells and human basophils in vitro. LC-6.2Cl blocks both IgE-mediated and non-IgE-mediated histamine release. Histamine release induced by antigen, dextran, compound 48/80, or the Ca2+ ionophore A23187 was effectively inhibited. The in vitro data indicate that LC6.2HCl has the capacity to inhibit the mediator release phase of anaphylaxis. The drug has the ability to inhibit arachidonate lipoxygenase activity. The IC50 for IgE-mediated histamine release inhibition is in good agreement with the IC50 for inhibition of arachidonate lipoxygenase activity. The data indicate that LC-6 acts in vivo by blocking the release of mediators; its activity may be explained by its ability to stop the synthesis of lipoxygenase-derived arachidonic acid products.
反式-2,3,4,5,7,8b,9,10-八氢萘并[1,2-C:5,6-C]二吡唑（LC-6）口服给药时在体内具有活性，在体外可抑制大鼠腹膜肥大细胞和人嗜碱性粒细胞释放组胺。LC-6·2HCl可阻断IgE介导和非IgE介导的组胺释放。抗原、右旋糖酐、化合物48/80或Ca2+离子载体A23187诱导的组胺释放均受到有效抑制。体外数据表明，LC6·2HCl具有抑制过敏反应介质释放阶段的能力。该药物具有抑制花生四烯酸脂氧合酶活性的能力。IgE介导的组胺释放抑制的IC50与花生四烯酸脂氧合酶活性抑制的IC50高度一致。数据表明，LC-6在体内通过阻断介质释放发挥作用；其活性可能归因于其阻止脂氧合酶衍生的花生四烯酸产物合成的能力。
