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分析 14 天铬(III)供应后选定脑受体的密度变化,并评估铬(III)对选定受体和转运体的亲和力。

Analysis of Density Changes of Selected Brain Receptors After a 14-Day Supply of Chromium(III) and Evaluation of Chromium(III) Affinity to Selected Receptors and Transporters.

机构信息

Department of Biochemistry and Basics of Cosmetology, University of Physical Education, al. Jana Pawła II 78, 31-571, Kraków, Poland.

Department of Pharmacobiology, Jagiellonian University Medical College, Kraków, Poland.

出版信息

Biol Trace Elem Res. 2020 Aug;196(2):359-364. doi: 10.1007/s12011-019-01924-y. Epub 2019 Nov 16.

Abstract

Chromium(III) is one of the most controversial biometals. Although, it is no longer on the list of minerals necessary for the proper functioning of the human body, and its pharmacological effect is still under discussion. One of the purposes of Cr(III) administration is to use it in patients with mood disorders and it is strictly related to its pharmacological, not dietary effect. This is because its high doses are necessary to obtain the results and additionally, no deficiencies in human population have been noted. In this study, the affinity of chromium(III) to selected receptors and transporters in the rat brain was evaluated, and the effect of the 14-day administration of this metal was assessed on the density of selected receptors. All analyses were performed in vitro using radioligand binding assays, and the results indicated lack of affinity to β and α receptors and serotonin transporter (SERT), furthermore very weak affinity to the 5-HT receptor (30% inhibition at 10 and 10 M). Analysis of the α and β adrenergic receptor density indicated lack of any adaptive effects after 14 days of Cr(III) administration through intraperitoneal injections (doses 6 and 12 mg/kg). The antidepressant activity of chromium(III) indicated in clinical trials concerned patients with atypical, seasonal, or dystonic symptoms. This effect, as it seems based on the presented results, does not depend on direct affinity to serotonin receptors and transporter nor is the result of adaptive changes in the adrenoreceptor system.

摘要

铬(III)是最具争议的生物金属之一。尽管它已不再被列入人体正常运作所需的矿物质之列,但其药理学作用仍在讨论中。三价铬的给药目的之一是将其用于情绪障碍患者,这与它的药理学作用而非饮食作用密切相关。这是因为需要高剂量才能获得结果,此外,人类群体中没有发现任何缺乏症。在这项研究中,评估了铬(III)在大鼠脑中对选定受体和转运体的亲和力,并评估了该金属 14 天给药对选定受体密度的影响。所有分析均在体外使用放射性配体结合分析进行,结果表明缺乏对β和α受体以及血清素转运体(SERT)的亲和力,此外对 5-HT 受体的亲和力非常弱(在 10 和 10 M 时抑制 30%)。通过腹腔注射(剂量为 6 和 12 mg/kg)进行 14 天的 Cr(III)给药后,对α和β肾上腺素能受体密度的分析表明不存在任何适应性效应。临床试验中表明的三价铬的抗抑郁活性涉及到具有非典型、季节性或运动障碍症状的患者。根据目前的结果,这种作用似乎不依赖于与血清素受体和转运体的直接亲和力,也不是肾上腺素能受体系统适应性变化的结果。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8851/7306032/74e728242ecc/12011_2019_1924_Fig1_HTML.jpg

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