Kovalev I E, Durakova L I, Kovaleva V L, Shmar'ian M I, Klimova N V
Farmakol Toksikol. 1977 Sep-Oct;40(5):573-8.
It is shown that the replacement of the ethyl or methyl radical in the molecules of aethaperazine or metherazine with the adamantyl one results in the appearance of a singular immunotropic activity. Such a drug (adapiprazine) exerts an immunodepressive action both on the primary and secondary response of the mice immunized with sheep erythrocytes. The immunodepressive action of adapiprazine is manifest with a low-dosage optimum introduced before immunization. In analogous conditions aethaperazine and metherazine fail to display any immunodepressive action. Adapiprazine arrests the rejection of a skin allotrasplant in mice differing from the donors in the presence of a strong histocompatibility locus. In in vitro tests adapiprazine in a concentration of 10(-5) mol and less has no effect on the spontaneous migration of leucocytes in the capillary, nor upon the process of immune roset-formation.
已表明,在乙哌嗪或甲硫哒嗪分子中用金刚烷基取代乙基或甲基会导致出现独特的免疫otropic活性。这样一种药物(阿地哌嗪)对用绵羊红细胞免疫的小鼠的初次和二次反应均具有免疫抑制作用。阿地哌嗪的免疫抑制作用在免疫前引入的低剂量最佳值时表现出来。在类似条件下,乙哌嗪和甲硫哒嗪未显示出任何免疫抑制作用。阿地哌嗪可阻止在存在强组织相容性位点的情况下与供体不同的小鼠皮肤同种异体移植物的排斥反应。在体外试验中,浓度为10(-5)摩尔及更低的阿地哌嗪对白细胞在毛细血管中的自发迁移以及免疫玫瑰花结形成过程均无影响。