Tarayre J P, Aliaga M, Barbara M, Tisseyre N, Tisné-Versailles J, Couzinier J P
Centre de Recherche Pierre Fabre, Castres, France.
Arch Int Pharmacodyn Ther. 1991 Mar-Apr;310:142-61.
Tioxamast, an anti-allergic compound inhibiting the release and synthesis of certain mediators of allergy and having no major antagonist effect towards such mediators, was experimented on various models of anaphylactic shock, hyperreactivity and bronchial inflammation in guinea-pigs. Tioxamast does not reduce passive pulmonary anaphylactic shocks induced in anaesthetized or conscious guinea-pigs by i.v. challenge of antigen. Likewise, the compound has no effect on systemic hyperreactivity towards i.v. histamine induced in anaesthetized guinea-pigs after a passive anaphylactic shock caused by i.v. challenge of antigen. On the other hand, tioxamast inhibits passive pulmonary anaphylactic shock induced in guinea-pigs by antigen aerosol in conscious guinea-pigs. Likewise, tioxamast decreases hyperreactivity to inhalation of histamine or carbamylcholine obtained after an active or passive anaphylactic shock by aerosol in conscious guinea-pigs. The oxamate derivative attenuates the increase in number of eosinophils and mononuclear cells obtained in the bronchoalveolar lavage fluid 24 hr after an active anaphylactic shock induced by aerosol. The anti-allergic activity of tioxamast on the various models carried out in guinea-pigs thus appears when these models are induced by a challenge of antigen or mediator by inhalation.
噻克索马斯是一种抗过敏化合物,可抑制某些过敏介质的释放和合成,且对这些介质无主要拮抗作用。在豚鼠的各种过敏性休克、高反应性和支气管炎症模型上对其进行了实验。噻克索马斯不能减轻静脉注射抗原激发在麻醉或清醒豚鼠中诱导的被动性肺过敏性休克。同样,该化合物对静脉注射组胺引起的全身性高反应性也无作用,这种高反应性是在静脉注射抗原引发被动性过敏性休克后在麻醉豚鼠中诱导产生的。另一方面,噻克索马斯可抑制清醒豚鼠通过抗原气雾剂诱导的被动性肺过敏性休克。同样,噻克索马斯可降低清醒豚鼠在主动或被动过敏性休克后通过气雾剂吸入组胺或氨甲酰胆碱时的高反应性。草氨酸酯衍生物可减轻气雾剂诱导的主动过敏性休克24小时后支气管肺泡灌洗液中嗜酸性粒细胞和单核细胞数量的增加。因此,当这些模型由吸入抗原或介质激发诱导时,噻克索马斯在豚鼠中进行的各种模型上的抗过敏活性就会显现出来。