Effects of Inorganic Ions on the Binding of Triflupromazine and Chlorpromazine to Bovine Serum Albumin Studied by Spectrometric Methods
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- Kitamura Keisuke
- Kyoto Pharmaceutical University
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- Omran1) Ahmed Ahmed
- Kyoto Pharmaceutical University
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- Nagata Chieyo
- Kyoto Pharmaceutical University
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- Kamijima Yoshiko
- Kyoto Pharmaceutical University
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- Tanaka Rumi
- Kyoto Pharmaceutical University
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- Takegami Shigehiko
- Kyoto Pharmaceutical University
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- Kitade Tatsuya
- Kyoto Pharmaceutical University
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The effects of inorganic salts, NaCl, NaBr, NaI, Na2SO4, KCl, KBr, KI, on the binding constants (Ks) of psychotropic phenothiazine drugs, triflupromazine (TFZ) and chlorpromazine, to bovine serum albumin (BSA) were examined by using second-derivative spectrophotometry. All of the salts examined, with the exception of Na2SO4, decreased the K values significantly, depending on the concentration of the salt, e.g., the decrease in the K values of both drugs were about 40% for 0.1 M NaCl. The results obtained with Na2SO4 indicated that neither Na+ nor SO42− had any affect on the binding of the phenothiazines to BSA. Based on the Na2SO4 results and the finding that the effect of each potassium salt on binding was quite similar to that of the corresponding sodium salt, the effects of these halogen salts can be considered to be derived from their anions, although the phenothiazines are positively charged at pH 7.4. The effectiveness of the anions was determined to occur in the following order: I−>>Br−>Cl−; these results coincided with the published order of the binding affinity of these anions to albumin. The 19F-NMR spectra of TFZ in the presence of each of these halogen salts revealed a concentration-dependent decrease in the intensity of the signal at 13.8 ppm that had previously been assigned to the TFZ bound to Site II. Consequently, the effects of these anions on the binding of positively charged phenothiazine drugs are thought to be local steric effects caused by the binding of these anions to Site II.
収録刊行物
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- CHEMICAL & PHARMACEUTICAL BULLETIN
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CHEMICAL & PHARMACEUTICAL BULLETIN 54 (7), 972-976, 2006
公益社団法人 日本薬学会
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詳細情報 詳細情報について
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- CRID
- 1390282679145733760
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- NII論文ID
- 110004836418
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- NII書誌ID
- AA00602100
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- ISSN
- 13475223
- 00092363
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- NDL書誌ID
- 7960442
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- 本文言語コード
- en
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- データソース種別
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- JaLC
- NDL
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