New 3-(4-(aryl)piperazin-1-yl)-1-(benzo(b)thiophen-3-yl)propane derivatives with dual action at 5-HT1A serotonin receptors and serotonin transporter as a new class of antidepressants.

Martinez J; Perez S; Oficialdegui AM; Heras B; Orus L; Villanueva H; Palop JA; Roca J; Mourelle M; Bosch A; Del-Castillo JC; Lasheras B; Tordera R; del-Rio J; Monge A

首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >New 3-(4-(aryl)piperazin-1-yl)-1-(benzo(b)thiophen-3-yl)propane derivatives with dual action at 5-HT1A serotonin receptors and serotonin transporter as a new class of antidepressants.

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New 3-(4-(aryl)piperazin-1-yl)-1-(benzo(b)thiophen-3-yl)propane derivatives with dual action at 5-HT1A serotonin receptors and serotonin transporter as a new class of antidepressants.

机译：新的3-（4-（芳基）哌嗪-1-基）-1-（苯并（b）噻吩-3-基）丙烷衍生物对5-HT1A血清素受体和血清素转运蛋白具有双重作用，是一类新型的抗抑郁药。

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A series of new 3-[4-(aryl)piperazin-1-yl]-1-(benzo[b]thiophen-3-yl)propane derivatives were synthesized in an attempt to find a new class of antidepressant drugs with dual activity at 5-HT1A serotonin receptors and serotonin transporter. Title compounds were evaluated for in vitro activity on 5-HT1A receptor and 5-HT transporter. They show high nanomolar affinity for both activities, and in particular, compounds 1-(5-chlorobenzo[b]thiophen-3-yl)-3-[4-(2-methoxyphenyl)piperazin-1-yl]propan-1-ol (7) and 1-(5-fluorobenzo[b]thiophen-3-yl)-3-[4-(2-methoxyphenyl)piperazin-1-yl]propan-1-ol (8) show values (nM) of K(i)=30 and 2.3 for 5-HT1A receptors and K(i)=30 and 12 for serotonin transporters, respectively. In GTPgammaS binding assays, compound 8 revealed antagonist properties to 5-HT1A receptors. Such a pharmacological profile could lead to potent antidepressant agents with new dual mechanism of action.

机译：为了寻找具有双重活性的新型抗抑郁药，合成了一系列新的3- [4-（芳基）哌嗪-1-基] -1-（苯并[b]噻吩-3-基）丙烷衍生物。在5-HT1A血清素受体和血清素转运蛋白。评价了标题化合物对5-HT1A受体和5-HT转运蛋白的体外活性。它们对两种活性都显示出高的纳摩尔亲和力，特别是化合物1-（5-氯苯并[b]噻吩-3-基）-3- [4-（2-甲氧基苯基）哌嗪-1-基]丙烷-1- ol（7）和1-（5-氟苯并[b]噻吩-3-基）-3- [4-（2-甲氧基苯基）哌嗪-1-基]丙-1-醇（8）显示值（nM） 5-HT1A受体的K（i）= 30和2.3，5-羟色胺转运蛋白的K（i）= 30和12。在GTPgammaS结合测定中，化合物8揭示了对5-HT1A受体的拮抗特性。这种药理作用可能导致具有新的双重作用机制的有效抗抑郁药。

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来源
《European Journal of Medicinal Chemistry: Chimie Therapeutique》 |2001年第1期|共7页
作者
Martinez J; Perez S; Oficialdegui AM; Heras B; Orus L; Villanueva H; Palop JA; Roca J; Mourelle M; Bosch A; Del-Castillo JC; Lasheras B; Tordera R; del-Rio J; Monge A;
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正文语种 eng
中图分类医药、卫生;
关键词
Antidepressive Agents; Carrier Proteins; Membrane Glycoproteins; Piperazines; 抗抑郁药; 载体蛋白质类; 膜糖蛋白类; 哌嗪类; 受体; 血清素; 血清素拮抗药; 血清素摄取抑制药;

机译：Antidepressive Agents;Carrier Proteins;Membrane Glycoproteins;Piperazines;抗抑郁药;载体蛋白质类;膜糖蛋白类;哌嗪类;受体;血清素;血清素拮抗药;血清素摄取抑制药;

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1. New 3-(4-(aryl)piperazin-1-yl)-1-(benzo(b)thiophen-3-yl)propane derivatives with dual action at 5-HT1A serotonin receptors and serotonin transporter as a new class of antidepressants. [J] . Martinez J, Perez S, Oficialdegui AM, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2001,第1期

机译：新的3-（4-（芳基）哌嗪-1-基）-1-（苯并（b）噻吩-3-基）丙烷衍生物对5-HT1A血清素受体和血清素转运蛋白具有双重作用，是一类新型的抗抑郁药。
2. New 3-(4-(3-substituted phenyl)piperazin-1-yl)-1-(benzo(b)thiophen-3-yl)propanol derivatives with dual action at 5-HT1A serotonin receptors and serotonin transporter as a new class of antidepressants. [J] . Orus L, Martinez J, Perez S, Die Pharmazie . 2002,第8期

机译：新的3-（4-（3-取代的苯基）哌嗪-1-基）-1-（苯并（b）噻吩-3-基）丙醇衍生物对5-HT1A血清素受体和血清素转运蛋白具有双重作用抗抑郁药。
3. New 3-(4-(2,3-dihydro-14-benzodioxin-5-yl)piperazin-1-yl)-1-(5-substituted benzo(b)thiophen-3-yl)propanol derivatives with dual action at 5-HT(1A) serotonin receptors and serotonin transporter as a new class of antidepressants. [J] . Silanes SP, Orus L, Oficialdegui AM, Die Pharmazie . 2004,第7期

机译：新的3-（4-（2,3-二氢-14-苯并二恶英-5-基）哌嗪-1-基）-1-（5-取代的苯并（b）噻吩-3-基）丙醇衍生物5-HT（1A）血清素受体和血清素转运蛋白是一类新型的抗抑郁药。
4. Attachment processes and gene-environment interactions: Testing Two Initial Hypotheses Regarding the Relationship between Attachment, and Methylation of the Glucocorticoid Receptor Gene (NR3C1) and the Serotonin Transporter Gene (SLC6A4). [D] . Jones-Mason, Karen. 2011

机译：附着过程和基因与环境的相互作用：测试关于糖皮质激素受体基因（NR3C1）和血清素转运蛋白基因（SLC6A4）的附着和甲基化之间关系的两个初步假设。
5. A positron emission tomography occupancy study of brexpiprazole at dopamine D2 and D3 and serotonin 5-HT1A and 5-HT2A receptors and serotonin reuptake transporters in subjects with schizophrenia [O] . Ragy R. Girgis, Andy Forbes, Anissa Abi-Dargham, 2020

机译：多巴胺D2和D3和血清素5-HT1A和5-HT2A受体的正电子发射断层扫描占用研究以及精神分裂症的受试者中的血清素再摄取转运蛋白
6. Synthesis and Biological Evaluation of Novel Compounds within a Class of 3-Aminochroman Derivatives with Dual 5-HT1A Receptor and Serotonin Transporter Affinity [O] . -1

机译：用双5-HT1A受体和血清素转运蛋白亲和力的3-氨基氧化物衍生物内新化合物的合成与生物学评价

New 3-(4-(aryl)piperazin-1-yl)-1-(benzo(b)thiophen-3-yl)propane derivatives with dual action at 5-HT1A serotonin receptors and serotonin transporter as a new class of antidepressants.

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