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雌激素受体配体R 2858(17α-乙炔基-11β-甲氧基-雌二醇-17β)放射性标记的辐射分解产物的“特异性受体结合”

'Specific receptor binding' of radioactively labeled products of radiolysis of the estrogen receptor ligand R 2858 (17 alpha-ethynyl-11 beta-methoxy-estradiol-17 beta).

作者信息

Dahlberg E

出版信息

Biochim Biophys Acta. 1983 Jan 4;755(1):148-50. doi: 10.1016/0304-4165(83)90285-4.

Abstract

Radioactively labeled steroids undergo decomposition processes, which are dependent on time, storage conditions (temperature, solvents etc.), degree of labeling etc. This communication shows that several decomposition products of 17 alpha-ethynyl-11 beta-methoxy-estradiol-17 beta (R 2858) bind to rat uterine cytosol in a way that would be interpreted as 'specific receptor binding' if some of these compounds were present in the ligand solution used for estrogen receptor determination. Thus, the binding was charcoal-resistant and displaceable with an excess of unlabeled R 2858, and the percentage of binding was of significant magnitude to seriously interfere with receptor measurements.

摘要

放射性标记的类固醇会经历分解过程,这些过程取决于时间、储存条件(温度、溶剂等)、标记程度等。本通讯表明,17α-乙炔基-11β-甲氧基雌二醇-17β(R 2858)的几种分解产物与大鼠子宫胞液的结合方式,如果这些化合物中的某些存在于用于雌激素受体测定的配体溶液中,会被解释为“特异性受体结合”。因此,这种结合具有抗活性炭特性,并且可以被过量的未标记R 2858取代,结合百分比达到显著程度,严重干扰受体测量。

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