Synthesis of Dihydrofuroaporphine Derivatives: Identification of a Potent and Selective Serotonin 5-HT1A Receptor Agonist

Liu ZL; Zhang H; Ye N; Zhang J; Wu QQ; Sun PH; Li LY; Zhen XC; Zhang A

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Synthesis of Dihydrofuroaporphine Derivatives: Identification of a Potent and Selective Serotonin 5-HT1A Receptor Agonist

机译：二氢呋喃卟啉衍生物的合成：有效和选择性5-羟色胺5-HT1A受体激动剂的鉴定。

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A series of new aporphine analogues were synthesized and pharmacologically evaluated. 11-Allyloxy-(17), 11-propargyloxy-(20), and dihydrofuro-(19) aporphines displayed the highest affinity at the 5-HT1A receptor with K-i values of 12.0, 14.0, and 6.7 nM, respectively. The high binding potential of the diastereomeric mixture of aporphine 19 was found residing in the cis-diastereomer (cis-19). [S-35]GTP gamma S function assays on 5-HT1A receptor indicated that aporphines 17 and 20 were partial agonists, while trans-19 behaved as a high efficacy full antagonist and cis-19 was a full agonist. The agonistic property of cis-19 at the 5-HT1A receptor was further confirmed in vitro and in vivo. This compound may be useful as a potential treatment for anxiety.

机译：合成了一系列新的阿波啡类似物并进行了药理学评估。 11-烯丙氧基-（17），11-炔丙基氧基-（20）和二氢呋喃基-（19）的阿芬对5-HT1A受体的亲和力最高，K-i值分别为12.0、14.0和6.7 nM。发现阿波啡19的非对映异构体混合物的高结合潜力存在于顺式-非对映异构体（cis-19）中。对5-HT1A受体的[S-35] GTPγS功能测定表明，阿波芬17和20是部分激动剂，而trans-19则是一种高效的完全拮抗剂，而cis-19则是完全激动剂。在体内和体外进一步证实了cis-19对5-HT1A受体的激动作用。该化合物可用作焦虑症的潜在治疗方法。

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《Journal of Medicinal Chemistry》 |2010年第3期|共10页
作者
Liu ZL; Zhang H; Ye N; Zhang J; Wu QQ; Sun PH; Li LY; Zhen XC; Zhang A;
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正文语种 eng
中图分类药学;
关键词
VENTRAL TEGMENTAL AREA; NIGRAL DOPAMINE NEURONS; ELEVATED PLUS-MAZE; (R)-APORPHINES SYNTHESIS; PARKINSONS-DISEASE; RAPHE NUCLEUS; RAT; PHARMACOLOGY; ANXIETY; COMPLICATIONS;

机译：腹侧前区;黑质多巴胺神经元;隆起的迷宫;（R）-AP的合成;帕金森病;RAPHE核;大鼠;药理学;焦虑;并发症;

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1. Synthesis of Dihydrofuroaporphine Derivatives: Identification of a Potent and Selective Serotonin 5-HT1A Receptor Agonist [J] . Liu ZL, Zhang H, Ye N, Journal of Medicinal Chemistry . 2010,第3期

机译：二氢呋喃卟啉衍生物的合成：有效和选择性5-羟色胺5-HT1A受体激动剂的鉴定。
2. Synthesis and evaluation of novel 2-oxo-1,2-dihydro-3-quinolinecarboxamide derivatives as potent and selective serotonin 5-HT4 receptor agonists. [J] . Suzuki M, Ohuchi Y, Asanuma H, Chemical and Pharmaceutical Bulletin . 2001,第1期

机译：新型2-氧-1,2-二氢-3-喹啉甲酰胺衍生物的合成和评价，作为有效和选择性的5-羟色胺5-HT4受体激动剂。
3. Novel derivatives of 2-pyridinemethylamine as selective, potent, and orally active agonists at 5-HT1A receptors. [J] . Vacher B, Bonnaud B, Funes P, Journal of Medicinal Chemistry . 1999,第9期

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4. α-Naphtyl Substituted Pirinixic Acid Derivatives as Potent Selective Agonists of the Peroxisome Proliferator-Activated Receptor Gamma [C] . Theresa M. Thieme, Ramona Steri, Ewgenij Proschak European Symposium on Organic Chemistry . 2009

机译：α-萘基取代的吡啶酸衍生物作为过氧化物体增殖物激活的受体γ的有效选择性激动剂
5. Serotonin Receptor Signaling Following Selective Serotonin Reuptake Inhibitor Treatment or: How I Learned to Stop Worrying and Love the Agonist. [D] . Van Dyke, Adam M. 2016

机译：选择性5-羟色胺再摄取抑制剂治疗后的5-羟色胺受体信号，或：我如何学会停止担心和热爱激动剂。
6. 23-Dihydro-1-Benzofuran Derivatives as a Series of Potent Selective Cannabinoid Receptor 2 Agonists: Design Synthesis and Binding Mode Prediction through Ligand-Steered Modeling [O] . Dr. Philippe Diaz, Sharangdhar S. Phatak, Dr. Jijun Xu, -1

机译：23-二氢-1-苯并呋喃衍生物作为一系列有效的选择性大麻素受体2激动剂：通过配体转向建模设计合成和结合模式预测
7. Novel Derivatives of 2-Pyridinemethylamine as Selective, Potent, and Orally Active Agonists at 5-HT1A Receptors [O] . Bernard Vacher, Bernard Bonnaud, Nathalie Jubault, 1998

机译：2-pyridinemethylamine的新衍生物作为5-HT1a受体的选择性，有效和口服活性激动剂

Synthesis of Dihydrofuroaporphine Derivatives: Identification of a Potent and Selective Serotonin 5-HT1A Receptor Agonist

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