3-Substituted 1-methyl-3-benzazepin-2-ones as 5- HT2C receptor agonists

Mahesh Shidore; Jatin Machhi; Prashant Murumkar

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3-Substituted 1-methyl-3-benzazepin-2-ones as 5- HT2C receptor agonists

机译：3-取代的1-甲基-3-苯并己己嘧啶-2-作为5-HT2C受体激动剂

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In search of potent and selective 5-HT_(2C) receptor agonists, a series of novel 3-substituted 1-methyl-3- benzazepin-2-ones and 8-chloro-1-methyl-3-benzazepin-2-ones have been synthesized and evaluated for their 5-HT_(2C) receptor agonistic potential. 5-HT2C receptor agonist activity was established with the despair swim test, plus maze test and the compounds' ability to decrease DA and 5-HT levels in rat brains similar to m-CPP. Selectivity was established with 5-HT_(2C) mediated penile erection and hypophagic responses in the presence of RS-102221 (a selective 5-HT_(2C) antagonist). The study established the selective 5-HT_(2C) receptor agonist response of compounds 7, 12-14, 24, 30, and 38 which could act as potential lead molecules for the treatment of pathological conditions associated with 5-HT2C receptors.

机译：寻找有效和选择性的5-HT_（2C）受体激动剂，一系列新的3取代的1-甲基-3-苯并嗪-2-苯并苯并-1-甲基-3-苯并嗪-2-苯并合成并评价其5-HT_（2C）受体激动潜力。用绝望的游泳试验，加上迷宫试验和化合物在类似于M-CPP的大鼠大脑中降低DA和5-HT水平的化合物的能力，确定了5-HT2C受体激动剂活性。在RS-102221（选择性5-HT_（2C）拮抗剂存在下，用5-HT_（2C）介导的阴茎勃起和药丸反应建立了选择性。该研究建立了化合物7,12-14,24,30和38的选择性5-HT_（2C）受体激动剂反应，其可以作为潜在的铅分子用于治疗与5-HT2C受体相关的病理病理。

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《RSC Advances》 |2015年第111期|共14页
作者
Mahesh Shidore; Jatin Machhi; Prashant Murumkar;
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Pharmacy Department Faculty of Technology &

Engineering Kalabhavan The M. S. University of Baroda Vadodara-390 001 India.;

Pharmacy Department Faculty of Technology &

Engineering Kalabhavan The M. S. University of Baroda Vadodara-390 001 India.;

Pharmacy Department Faculty of Technology &

Engineering Kalabhavan The M. S. University of Baroda Vadodara-390 001 India.;

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正文语种 eng
中图分类化学;
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1. 3-Substituted 1-methyl-3-benzazepin-2-ones as 5- HT2C receptor agonists [J] . Mahesh Shidore, Jatin Machhi, Prashant Murumkar RSC Advances . 2015,第111期

机译：3-取代的1-甲基-3-苯并己己嘧啶-2-作为5-HT2C受体激动剂
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机译：药物设计的新范例：设计和合成新型的生物活性肽，这些肽是阿片受体的激动剂，胆囊收缩素受体的拮抗剂。
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机译：使用5-HT2a受体激动剂持续治疗导致功能性脱敏和减少激动素标记的5-HT2a受体，尽管大鼠受体蛋白水平增加

3-Substituted 1-methyl-3-benzazepin-2-ones as 5- HT2C receptor agonists

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