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人淋巴细胞对活性[3H] - 多巴胺的摄取:与血清素转运体活性相关。

Active [3H]-dopamine uptake by human lymphocytes: correlates with serotonin transporter activity.

作者信息

Faraj B A, Olkowski Z L, Jackson R T

机构信息

Department of Radiology (Division of Nuclear Medicine), Emory University School of Medicine, Atlanta, Ga.

出版信息

Pharmacology. 1994 May;48(5):320-7. doi: 10.1159/000139195.

Abstract

The main objective of the present investigation was to determine whether the uptake of [3H]-dopamine in human lymphocytes is mediated through a serotonin transporter. This was examined by studying the effects of various monoamine uptake inhibitors on the uptake of [3H]-dopamine in human lymphocytes. Among the compounds tested, indatraline, imipramine and fluoxetine, selective inhibitors of neuronal serotonin transporter, were the most potent inhibitors of [3H]-dopamine uptake in lymphocytes. The 50% inhibiting concentration (IC50) for these inhibitors was in the range of 3.5-17 nmol/l. Bupropion, GBR 12909, nomifensine and xylamine, selective inhibitors of dopamine and norepinephrine transporters, had low affinity for the dopamine uptake system in human lymphocytes with IC50 values ranging between 1,000 and 40,000 nmol/l. These findings provide supportive evidence for the participation of a serotonin transporter in the uptake of [3H]-dopamine in human lymphocytes. The existence of a high affinity transport system for dopamine and serotonin in human lymphocytes may serve as a readily accessible model to detect changes in the neuronal uptake of dopamine and serotonin in addictive and psychiatric disorders.

摘要

本研究的主要目的是确定人淋巴细胞中[3H] - 多巴胺的摄取是否通过血清素转运体介导。通过研究各种单胺摄取抑制剂对人淋巴细胞中[3H] - 多巴胺摄取的影响来进行检测。在所测试的化合物中,神经元血清素转运体的选择性抑制剂茚达曲林、丙咪嗪和氟西汀是淋巴细胞中[3H] - 多巴胺摄取的最有效抑制剂。这些抑制剂的50%抑制浓度(IC50)在3.5 - 17 nmol/l范围内。安非他酮、GBR 12909、诺米芬辛和二甲苯胺,多巴胺和去甲肾上腺素转运体的选择性抑制剂,对人淋巴细胞中的多巴胺摄取系统亲和力较低,IC50值在1000至40000 nmol/l之间。这些发现为血清素转运体参与人淋巴细胞中[3H] - 多巴胺的摄取提供了支持性证据。人淋巴细胞中存在多巴胺和血清素的高亲和力转运系统,可能作为一个易于获取的模型,用于检测成瘾性和精神疾病中多巴胺和血清素神经元摄取的变化。

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