首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Study on the binding of chiral drug duloxetine hydrochloride to human serum albumin.
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Study on the binding of chiral drug duloxetine hydrochloride to human serum albumin.

机译:手性药物盐酸度洛西汀与人血清白蛋白结合的研究。

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Duloxetine holds a special promise as an antidepressant, and its effect depends on its binding to human serum albumin (HSA). For this reason, the binding mechanism of duloxetine with HSA was investigated. The specific binding site in HSA was identified and binding constants were determined. Duloxetine could compete with dansyl-L-proline (DLP), a site II marker for binding to site II. Binding constants between duloxetine and HSA were 1.75x10(3) L mol(-1) and 3.74x10(3) L mol(-1) at pH 7.4 and pH 8.5, respectively. The interaction process of enantiomers and HSA was susceptible to pH change. It was concluded that specific binding position of duloxetine was located in site II, and the B conformation of HSA possibly excelled the N conformation in identifying and binding to enantiomers.
机译:度洛西汀作为抗抑郁药具有特殊的前景,其作用取决于与人血清白蛋白(HSA)的结合。因此,研究了度洛西汀与HSA的结合机理。鉴定HSA中的特异性结合位点并确定结合常数。度洛西汀可以与Dansyl-L-脯氨酸(DLP)竞争,后者是结合位点II的位点II标记。在pH 7.4和pH 8.5下,度洛西汀和HSA之间的结合常数分别为1.75x10(3)L mol(-1)和3.74x10(3)L mol(-1)。对映异构体和HSA的相互作用过程容易受到pH值变化的影响。结论是度洛西汀的特异性结合位置位于位点II,HSA的B构象在鉴定和结合对映体方面可能优于N构象。

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