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首页> 外文期刊>Romanian Journal of Biophysics >RELATIONSHIP BETWEEN PROTEIN-BINDING AND FREE DRUG CONCENTRATIONS OF A SPARINGLY WATER-SOLUBLE SELECTIVE SEROTONIN REUPTAKE INHIBITORS (ESCITALOPRAM) AND ITS INTERACTION WITH ARSENIC
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RELATIONSHIP BETWEEN PROTEIN-BINDING AND FREE DRUG CONCENTRATIONS OF A SPARINGLY WATER-SOLUBLE SELECTIVE SEROTONIN REUPTAKE INHIBITORS (ESCITALOPRAM) AND ITS INTERACTION WITH ARSENIC

机译：少量水溶性选择性5-羟色胺再吸收抑制剂（雌激素）的蛋白结合与自由药物浓度之间的关系及其与砷的相互作用

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Escitalopram is the (S)-enantiomer of the racemic selective serotonin reuptake inhibitor antidepressant citalopram. Clinical studies have shown that escitalopram is effective and well tolerated in the treatment of depression and anxiety disorders. Single isomers of the selective serotonin reuptake inhibitors citalopram (escitalopram, S-citalopram) and fluoxetine (R-fluoxetine) are currently under development for the treatment of depression and other psychiatric disorders. Previous studies conducted in laboratory animals have revealed that the biological effects on serotonin reuptake for citalopram reside in the S enantiomer. In contrast, both enantiomers of fluoxetine contribute to its biological activity. The protein-binding of escitalopram was measured by equilibrium dialysis in the bovine serum albumin (BSA). Free escitalopram concentration was increased due to addition of arsenic which reduced the binding of the compounds to BSA. During concurrent administration, arsenic displaced escitalopram from its high-affinity binding Site I, and free concentration of escitalopram increased from 8.32% to 24.51% and 0.067% to 14.56% of Site I probe respectively. Thus, it can be ascribed that arsenic displaced escitalopram from its binding site resulting in an increase of the free escitalopram concentration in plasma. Potential correlation of these unique attributes of escitalopram and Arsenic are discussed.
机译：Escitalopram是消旋选择性5-羟色胺再摄取抑制剂抗抑郁药物西酞普兰的（S）-对映体。临床研究表明，依他普仑在抑郁症和焦虑症的治疗中有效且耐受性良好。选择性5-羟色胺再摄取抑制剂西酞普兰（依他普仑，S-西酞普兰）和氟西汀（R-氟西汀）的单一异构体目前正在开发中，用于治疗抑郁症和其他精神疾病。先前在实验动物中进行的研究表明，西酞普兰对5-羟色胺再摄取的生物学作用存在于S对映异构体中。相反，氟西汀的两种对映异构体均对其生物活性有贡献。通过平衡透析在牛血清白蛋白（BSA）中测量依西酞普兰的蛋白质结合。游离依他普仑的浓度由于添加了砷而增加，这降低了化合物与BSA的结合。在同时给药期间，砷从其高亲和力结合位点I置换了依他普仑，并且依他普仑的自由浓度分别从I点探针的8.32％增加至24.51％和0.067％至14.56％。因此，可以归因于砷从其结合位点置换了依他普仑，导致血浆中游离依他普仑的浓度增加。讨论了依他普仑和砷这些独特属性的潜在相关性。

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