2. Academic Validation
  3. Synthesis and antidepressant activity of arylalkanol-piperidine derivatives as triple reuptake inhibitors

Synthesis and antidepressant activity of arylalkanol-piperidine derivatives as triple reuptake inhibitors

  • Eur J Med Chem. 2012 Aug:54:123-36. doi: 10.1016/j.ejmech.2012.04.030.
Yong-Yong Zheng 1,  Lin Guo,  Xue-Chu Zhen,  Jian-Qi Li
Affiliations

Affiliation

  • 1 Novel Technology Center of Pharmaceutical Chemistry, Shanghai Institute of Pharmaceutical Industry, 1111 North Zhongshan No.1 Road, Shanghai 200437, PR China.
PMID: 22608762 DOI: 10.1016/j.ejmech.2012.04.030
Abstract

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.

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