Binding of several phenothiazine neuroleptics to a common binding site of alpha 1-acid glycoprotein, orosomucoid.
Binding of several phenothiazine neuroleptics to a common binding site of alpha 1-acid glycoprotein, orosomucoid.
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几种吩噻嗪类精神安定药与 α1-酸性糖蛋白 Orosumucoid 的共同结合位点的结合。
DOI：
10.1002/jps.2600720229
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发表时间：
1983
影响因子：
3.8
通讯作者：
W. Müller
中科院分区：
文献类型：
--
作者：
S. El‐Gamal;U. Wollert;W. Müller
用圆二色谱和平衡透析技术研究了几种吩噻嗪类抗精神病药与α 1-酸性糖蛋白的相互作用。仅氯丙嗪与蛋白质有一个高亲和力结合位点，药物与该位点的结合产生典型的多相外源性Cotton效应。由于其他几种吩噻嗪类抗精神病药在α 1-酸性糖蛋白存在下产生了定性可比的外源性Cotton效应，并有效抑制氯丙嗪与单一位点的结合，因此得出结论，所有研究的吩噻嗪衍生物都优先与α 1-酸性糖蛋白分子的一个共同结合位点结合。
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.