Arylpiperazine-containing pyrimidine 4-carboxamide derivatives targeting serotonin 5-HT(2A), 5-HT(2C), and the serotonin transporter as a potential antidepressant.

Kim JY; Kim D; Kang SY; Park WK; Kim HJ; Jung ME; Son EJ; Pae AN; Kim J; Lee J

首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >Arylpiperazine-containing pyrimidine 4-carboxamide derivatives targeting serotonin 5-HT(2A), 5-HT(2C), and the serotonin transporter as a potential antidepressant.

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Arylpiperazine-containing pyrimidine 4-carboxamide derivatives targeting serotonin 5-HT(2A), 5-HT(2C), and the serotonin transporter as a potential antidepressant.

机译：靶向5-羟色胺5-HT（2A），5-HT（2C）和5-羟色胺转运蛋白的芳基哌嗪嘧啶4-羧酰胺衍生物作为潜在的抗抑郁药。

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Pyrimidine usually has good pharmacokinetic properties as a drug substance and considerable efforts have been devoted to develop pyrimidine derivatives into drug candidates. Arylpiperazine-containing pyrimidine 4-carboxamide derivatives were synthesized and evaluated for binding to serotonin receptors and transporter. Pyrimidine derivatives showed good antidepressant activity in FST (forced swimming test) animal model and also displayed no appreciable inhibitory activity against hERG channel blocking assay. Herein SAR studies of pyrimidine derivatives targeting serotonin receptors and transporter will be disclosed.

机译：嘧啶通常作为药物具有良好的药代动力学性质，并且已经做出了很大的努力以将嘧啶衍生物开发成候选药物。合成了含芳基哌嗪的嘧啶4-羧酰胺衍生物，并评估了其与血清素受体和转运蛋白的结合。嘧啶衍生物在FST（强迫游泳试验）动物模型中显示出良好的抗抑郁活性，并且对hERG通道阻断试验也没有明显的抑制活性。本文将公开针对5-羟色胺受体和转运蛋白的嘧啶衍生物的SAR研究。

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《Bioorganic and Medicinal Chemistry Letters》 |2010年第22期|共4页
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Kim JY; Kim D; Kang SY; Park WK; Kim HJ; Jung ME; Son EJ; Pae AN; Kim J; Lee J;
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1. Arylpiperazine-containing pyrimidine 4-carboxamide derivatives targeting serotonin 5-HT(2A), 5-HT(2C), and the serotonin transporter as a potential antidepressant. [J] . Kim JY, Kim D, Kang SY, Bioorganic and Medicinal Chemistry Letters . 2010,第22期

机译：靶向5-羟色胺5-HT（2A），5-HT（2C）和5-羟色胺转运蛋白的芳基哌嗪嘧啶4-羧酰胺衍生物作为潜在的抗抑郁药。
2. Arylpiperazine-containing pyrimidine 4-carboxamide derivatives targeting serotonin 5-HT(2A), 5-HT(2C), and the serotonin transporter as a potential antidepressant. [J] . Kim JY, Kim D, Kang SY, Bioorganic and Medicinal Chemistry Letters . 2010,第22期

机译：靶向5-羟色胺5-HT（2A），5-HT（2C）和5-羟色胺转运蛋白的芳基哌嗪嘧啶4-羧酰胺衍生物作为潜在的抗抑郁药。
3. Arylpiperazine-containing pyrrole 3-carboxamide derivatives targeting serotonin 5-HT(2A), 5-HT(2C), and the serotonin transporter as a potential antidepressant. [J] . Kang SY, Park EJ, Park WK, Bioorganic and Medicinal Chemistry Letters . 2010,第5期

机译：含芳基哌嗪的吡咯3-甲酰胺衍生物靶向5-羟色胺5-HT（2A），5-HT（2C）和5-羟色胺转运蛋白作为潜在的抗抑郁药。
4. Serotonin (5-HT) released by activated white blood cells in a biological fuel cell provide a potential energy source for electricity generation [C] . Justin, Gusphyl A., Sun, Engineering in Medicine and Biology Society, 2006 Annual International Conference of the IEEE . 2006

机译：生物燃料电池中活化的白细胞释放的5-羟色胺（5-HT）为发电提供了潜在的能源
5. The serotonin (5-HT) 2C receptor (5-HT2CR) and its downstream signaling components: Distinct adaptations in cortical circuits associated with cocaine exposure. [D] . Lanfranco Gallofre, Maria Fe. 2009

机译：血清素（5-HT）2C受体（5-HT2CR）及其下游信号成分：与可卡因暴露相关的皮质回路的明显适应。
6. Changes of Serotonin (5-HT) 5-HT2A Receptor and 5-HT Transporter in the Sprague-Dawley Rats of Depression Myocardial Infarction and Myocardial Infarction Co-exist with Depression [O] . Mei-Yan Liu, Yan-Ping Ren, Wan-Lin Wei, 2015

机译：抑郁心肌梗塞和心肌梗塞与抑郁症并存的Sprague-Dawley大鼠血清素（5-HT）5-HT2A受体和5-HT转运蛋白的变化
7. Quantitative changes in intracellular calcium and extracellular-regulated kinase activation measured in parallel in CHO cells stably expressing serotonin (5-HT) 5-HT_2Aor 5-HT_2Creceptors [O] . Seitz Patricia K, Bremer Nicole M, McGinnis Andrew G, 2012

机译：在稳定表达5-羟色胺（5-HT）5-HT _{2a 或5-HT _{2C 受体的CHO细胞中平行测量细胞内钙和细胞外调节激酶活化的数量变化}}

Arylpiperazine-containing pyrimidine 4-carboxamide derivatives targeting serotonin 5-HT(2A), 5-HT(2C), and the serotonin transporter as a potential antidepressant.

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