- Synthesis and antidepressant activity of a series of arylalkanol and aralkyl piperazine derivatives targeting SSRI/5-HT1A/5-HT7
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A series of arylalkanol and aralkyl piperazine derivatives have been synthesized and evaluated for 5-HT reuptake inhibitory abilities and binding affinities at the 5-HT1A/5-HT7 receptors. Antidepressant activities of the compounds in
- Gu, Zheng-Song,Xiao, Ying,Zhang, Qing-Wei,Li, Jian-Qi
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supporting information
p. 5420 - 5423
(2017/11/17)
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- Synthesis and pharmacological investigation of aralkyl diamine derivatives as potential triple reuptake inhibitors
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A series of aralkyl diamine derivatives were designed, synthesized, and evaluated for their triple reuptake inhibitory abilities. Compounds 18c (5-HT, NE, DA, IC50 = 389, 69, 238 nM), 36a (5-HT, NE, DA, IC50 = 378, 477, 247 nM), and
- Zheng, Yong-Yong,Weng, Zhi-Jie,Xie, Peng,Zhu, Mei-Yu,Xing, Long-Xuan,Li, Jian-Qi
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p. 219 - 234
(2014/09/17)
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- ARALKYL DIAMINE DERIVATIVES AND USES THEREOF AS ANTIDEPRESSANTS
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Aralkyl diamine derivative of the following formula, pharmaceutically acceptable salts or uses thereof as antidepressants. The derivatives have triplex inhibiting activities of the reuptake of 5-HT, dopamine and noradrenalin, which can be administered to the patients in need of such treatment in the form of compositions orally or injectedly et al.
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Paragraph 0161
(2013/03/28)
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- ARALKYL DIAMINE DERIVATIVES AND USES THEREOF AS ANTIDEPRESSANT
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Aralkyl diamine derivative of the following formula, pharmaceutically acceptable salts or uses thereof as antidepressants. The derivatives have triplex inhibiting activities of the reuptake of 5-HT, dopamine and noradrenalin, which can be administered to the patients in need of such treatment in the form of compositions orally or injectedly et al.
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Paragraph 0027; 0033
(2013/03/28)
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- Synthesis and antidepressant activity of arylalkanol-piperidine derivatives as triple reuptake inhibitors
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A series of arylalkanol-piperidine derivatives was synthesized, and their triple reuptake inhibition and in vivo activities have been evaluated. Among them, compounds 2a, 2j, 2k, 2m and 2n exhibited high potency for 5-HT, NA and DA transporters. Optimized compounds 2j and 2m showed significant reduction of immobility time compared to that of vehicle in the mouse tail suspension test (TST) test at doses ranging from 10 to 50 mg/kg po, and were not generally motor stimulants at 50 mg/kg dose. In addition, compounds 2j and 2m displayed desirable pharmacokinetic properties in SD rats.
- Zheng, Yong-Yong,Guo, Lin,Zhen, Xue-Chu,Li, Jian-Qi
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experimental part
p. 123 - 136
(2012/09/08)
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