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几种吩噻嗪类抗精神病药物与α1-酸性糖蛋白(orosomucoid)的一个共同结合位点的结合。

Binding of several phenothiazine neuroleptics to a common binding site of alpha 1-acid glycoprotein, orosomucoid.

作者信息

El-Gamal S, Wollert U, Müller W E

出版信息

J Pharm Sci. 1983 Feb;72(2):202-5. doi: 10.1002/jps.2600720229.

Abstract

The interaction of several phenothiazine neuroleptics with alpha 1-acid glycoprotein was investigated using circular dichroism and equilibrium dialysis techniques. For chlorpromazine only, one high-affinity binding site of the protein was found. The binding of the drug to this single site generated typical polyphasic extrinsic Cotton effects. Since several other phenothiazine neuroleptics gave qualitatively comparable extrinsic Cotton effects in the presence of alpha 1-acid glycoprotein and potently inhibited the binding of chlorpromazine to the single site, it was concluded that all phenothiazine derivatives investigated bound preferentially to only one common binding site of the alpha 1-acid glycoprotein molecule.

摘要

利用圆二色性和平衡透析技术研究了几种吩噻嗪类抗精神病药物与α1-酸性糖蛋白的相互作用。仅对于氯丙嗪,发现该蛋白有一个高亲和力结合位点。药物与该单个位点的结合产生了典型的多相外在科顿效应。由于其他几种吩噻嗪类抗精神病药物在α1-酸性糖蛋白存在下产生了定性上相当的外在科顿效应,并强烈抑制氯丙嗪与该单个位点的结合,因此得出结论,所研究的所有吩噻嗪衍生物都优先结合到α1-酸性糖蛋白分子的一个共同结合位点上。

相似文献

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Drug binding to alpha 1-acid glycoprotein studied by circular dichroism.
Pharm Res. 1989 Feb;6(2):156-9. doi: 10.1023/a:1015936710919.

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