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哌嗪侧链吩噻嗪类药物奋乃静与一种血清蛋白的特异性结合(作者译)

[Specific binding of perazine, a piperazine side-chain phenothiazine drug, to a serum protein (author's transl)].

作者信息

Schley J, Nündel M, Riedel E, Müller-Oerlinghausen B

出版信息

Arzneimittelforschung. 1979;29(1):106-8.

PMID:36101
Abstract

A binding of perazine to a serum protein of 48 000 D was determined by gel filtration. The affinity constant of the perazine-protein complex was found to be 5.42 X 10(6) mol/l corresponding to a specific binding of 70 ng/ml serum. This result may gather clinical relevance with regard to the "CNS-bioavailability" and individual response to perazine, the average therapeutic serum concentrations having been shown to range between appr. 50 and 200 ng/ml serum. A specific binding of perazine to human or bovine albumine could not be detected.

摘要

通过凝胶过滤法测定了奋乃静与一种48000D血清蛋白的结合情况。发现奋乃静 - 蛋白质复合物的亲和常数为5.42×10⁶mol/l,对应于血清中70ng/ml的特异性结合。该结果可能与奋乃静的“中枢神经系统生物利用度”和个体反应具有临床相关性,已表明其平均治疗血清浓度在约50至200ng/ml血清之间。未检测到奋乃静与人或牛白蛋白的特异性结合。

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