Albouz S, Hauw J J, Berwald-Netter Y, Boutry J M, Bourdon R, Baumann N
Biomedicine. 1981 Dec;35(7-8):218-20.
Tricyclic antidepressants (imipramine and desipramine) gave rise to an important decrease of sphingomyelinase activity in murine neuroblastoma and human fibroblast cell cultures. It occurred within 1 to 2 hours at a final concentration of 1 or 2 X 10(-5) M in cell culture medium. Other lysosomal enzymes such as acid lipase, arylsulfatases A and B and hexosaminidases were not modified. Low level of sphingomyelinase activity may be related to the amphiphilic characteristics of the drugs: iminodibenzyle which has the same tricyclic core but is devoid of the side chain necessary for amphiphilic properties had no effect. As iminodibenzyle has no therapeutic action, amphiphilic may be requisite to antidepressant properties of tricyclic drugs.
三环类抗抑郁药(丙咪嗪和地昔帕明)可使小鼠神经母细胞瘤和人成纤维细胞培养物中的鞘磷脂酶活性显著降低。在细胞培养基中终浓度为1或2×10⁻⁵ M时,1至2小时内即可出现这种情况。其他溶酶体酶,如酸性脂肪酶、芳基硫酸酯酶A和B以及己糖胺酶未发生改变。鞘磷脂酶活性水平较低可能与药物的两亲性特征有关:具有相同三环核心但缺乏两亲性所需侧链的亚氨基二苄没有作用。由于亚氨基二苄没有治疗作用,两亲性可能是三环类药物具有抗抑郁特性所必需的。