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首页> 外文期刊>Japanese Journal of Ophthalmology >Binding affinity of bunazosin, dorzolamide, and timolol to synthetic melanin
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Binding affinity of bunazosin, dorzolamide, and timolol to synthetic melanin

机译：布纳唑嗪，多佐胺和噻吗洛尔对合成黑色素的结合亲和力

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Purpose: The purpose of this study was to compare the binding affinity of bunazosin and dorzolamide to synthetic melanin relative to that of timolol.Methods: Synthetic melanin was prepared from dopa by the action of tyrosinase. Timolol, dorzolamide, and bunazosin were incubated separately at a concentration of 10(-4) M in 2 ml of 0.066 M phosphate buffer containing 5 mg of synthetic melanin. After centrifugation, the absorbance of each free drug in the supernatant was measured at its optimum wavelength. The percentage of each drug bound to melanin was calculated directly from the change in absorbance relative to the initial value.Results: The increase in the binding rates of all three drugs seemed to reach a plateau after 30min. After incubating for 60 min, the binding rate of timolol was 22.2% +/- 4.9%, bunazosin 36.3% +/- 2.5%, and dorzolamide 8.5% +/- 1.9%. There were statistically significant differences between the binding rates of each drug.Conclusions: Under our study conditions, the order of binding affinity of these ocular hypotensive agents to synthetic melanin seems to be as follows: bunazosin > timolol > dorzolamide. Jpn J Ophthahnol 2004;48:34-36 (C) Japanese Ophthalmological Society 2004.
机译：目的：本研究的目的是比较布偶氮唑和多唑胺与合成的黑色素相对于替莫洛尔的结合亲和力。方法：通过酪氨酸酶的作用从多巴制备合成的黑色素。在2 ml含5 mg合成黑色素的0.066 M磷酸盐缓冲液中，以10（-4）M的浓度分别孵育Timolol，dorzolamide和bunazosin。离心后，以最佳波长测量上清液中每种游离药物的吸光度。从吸光度相对于初始值的变化直接计算出每种药物与黑色素结合的百分比。结果：30分钟后，所有三种药物的结合率增加似乎达到了平稳状态。孵育60分钟后，噻吗洛尔的结合率为22.2％+/- 4.9％，布偶唑嗪36.3％+/- 2.5％和多唑胺8.5％+/- 1.9％。结论：在我们的研究条件下，这些降压剂对合成黑色素的结合亲和力顺序似乎为：布达唑嗪>替莫洛尔>多佐胺。 Jpn J邻苯二酚2004; 48：34-36（C）2004年日本眼科学会。

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