膜磷酸化后配体结合的变化

Changes of ligand binding after membrane phosphorylation.

作者信息

Krulík R, Bures P, Simůnková D, Havránek M

机构信息

Psychiatric Research Unit, Faculty of Medicine, Charles University, Praha, Czechoslovakia.

出版信息

Drug Metabol Drug Interact. 1991;9(3-4):293-9. doi: 10.1515/dmdi.1991.9.3-4.293.

DOI:10.1515/dmdi.1991.9.3-4.293

PMID:1824082

Abstract

Phosphorylation of synaptic plasma brain membranes (SPM) causes a decrease of the specific binding of demethylated tricyclic antidepressants (TCA) and changes the affinity of 3H-imipramine and 3H-desmethylimipramine binding. The decrease of TCA binding was found also in lymphocyte membranes. In platelet membranes a decreased binding was found only with demethylated dibenzazepine derivatives. Bmax and Kd values are also decreased in the presence of phosphatidic acid or alpha-glycerolphosphate.

摘要

突触质膜（SPM）的磷酸化导致去甲基化三环类抗抑郁药（TCA）的特异性结合减少，并改变3H-丙咪嗪和3H-去甲丙咪嗪结合的亲和力。在淋巴细胞膜中也发现TCA结合减少。在血小板膜中，仅发现去甲基化二苯氮䓬衍生物的结合减少。在磷脂酸或α-甘油磷酸存在的情况下，Bmax和Kd值也会降低。