通过小鼠大脑新皮层结合试验评估抗抑郁药对毒蕈碱受体的抑制作用

IF 3 3区医学 Q2 PHARMACOLOGY & PHARMACY

Journal of pharmacological sciences Pub Date : 2024-09-11 DOI:10.1016/j.jphs.2024.09.001

Keisuke Obara, Yuki Usami, Risa Okamoto, Kento Yoshioka, Yoshio Tanaka

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引用次数: 0

摘要

我们研究了32种抗抑郁药对小鼠大脑新皮层中[3H]N-甲基东莨菪碱（[3H]NMS）特异性结合的抑制作用，以确定哪些抗抑郁药应推荐给阿尔茨海默病患者（AD）。在接受测试的药物中，有九种抗抑郁药（10-4 M）对[3H]NMS特异性结合的抑制作用较小（35%）：噻奈普汀（一种三环类药物）；曲唑酮（一种血清素 5-HT2A 阻断剂）；舒必利（一种多巴胺 D2 阻断剂）；氟伏沙明（一种选择性血清素再摄取抑制剂 (RI)）；米那西普兰、左米那西普兰、文拉法辛和去文拉法辛（血清素和去甲肾上腺素 RI）；以及安非他酮（一种去甲肾上腺素和多巴胺 RI）。因此，这些抗抑郁药对大脑的抗胆碱能作用很小，建议用于注意力缺失症患者。

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Evaluation of inhibitory actions of antidepressants on muscarinic receptors assessed by a binding assay in the mouse cerebral neocortex

We investigated the inhibitory effects of 32 antidepressants on [³H]N-methylscopolamine ([³H]NMS)-specific binding in the mouse cerebral neocortex to determine which antidepressants should be recommended for patients with Alzheimer's disease (AD). Of those tested, nine antidepressants (10⁻⁴ M) exhibited less inhibitory effect on [³H]NMS-specific binding (<35%): tianeptine (a tricyclic); trazodone (a serotonin 5-HT_2A blocker); sulpiride (a dopamine D₂ blocker); fluvoxamine (a selective serotonin reuptake inhibitor (RI)); milnacipran, levomilnacipran, venlafaxine, and desvenlafaxine (serotonin and noradrenaline RIs); and bupropion (a noradrenaline and dopamine RI). Therefore, these antidepressants show little anticholinergic effect in the brain and are recommended for use in patients with AD.

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来源期刊

Journal of pharmacological sciences 医学-药学

CiteScore

6.20

自引率

2.90%

发文量

104

审稿时长

31 days

期刊介绍： Journal of Pharmacological Sciences (JPS) is an international open access journal intended for the advancement of pharmacological sciences in the world. The Journal welcomes submissions in all fields of experimental and clinical pharmacology, including neuroscience, and biochemical, cellular, and molecular pharmacology for publication as Reviews, Full Papers or Short Communications. Short Communications are short research article intended to provide novel and exciting pharmacological findings. Manuscripts concerning descriptive case reports, pharmacokinetic and pharmacodynamic studies without pharmacological mechanism and dose-response determinations are not acceptable and will be rejected without peer review. The ethnopharmacological studies are also out of the scope of this journal. Furthermore, JPS does not publish work on the actions of biological extracts unknown chemical composition.