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完整和去势大鼠前列腺对放射性碘化5α-双氢睾酮的摄取。

The uptake of radioiodinated 5 alpha-dihydrotestosterone by the prostate of intact and castrated rats.

作者信息

Tarle M, Padovan R, Spaventi S

出版信息

Eur J Nucl Med. 1981 Feb;6(2):79-83. doi: 10.1007/BF00253718.

Abstract

Radioiodinated steroid 2 alpha-125I-dihydrotestosterone was prepared by direct labeling procedure and subsequently utilized in the distribution studies on Albino Wistar male rats. Maximum radioactivity in the prostate was found 3 h after the administration of the radiolabeled steroid to 24-h castrated animals (1.29%/g wet weight) and to intact rats (0.57%). The pretreatment of animals with dihydrotestosterone yielded lower uptake by the prostate (0.29%-0.30%), epididymis, and testis while it did not influence the distribution in other androgen-insensitive tissues. The carbon-iodine bond was proved to be intact in the radiopharmacon examined and in its metabolites when retained by the rat prostate. The reported results are in line with our previous investigations on in vitro binding of radioiodinated dihydrotestosterone to androgen receptors but indicate also little utility of the same label for the visualization of the prostate gland.

摘要

通过直接标记法制备了放射性碘化甾体2α-125I-双氢睾酮,随后将其用于白化Wistar雄性大鼠的分布研究。给24小时去势动物和完整大鼠注射放射性标记的甾体后3小时,前列腺中的放射性达到最高(去势动物为1.29%/克湿重,完整大鼠为0.57%)。用双氢睾酮对动物进行预处理后,前列腺、附睾和睾丸的摄取量降低(0.29%-0.30%),而这并不影响其在其他雄激素不敏感组织中的分布。在所检测的放射性药物及其被大鼠前列腺保留的代谢产物中,碳-碘键被证明是完整的。报道的结果与我们之前关于放射性碘化双氢睾酮与雄激素受体体外结合的研究一致,但也表明相同的标记物用于前列腺显像的效用不大。

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