Structure-activity relationship studies of CNS agents, Part 22. A search for new trazodone-like antidepressants: synthesis and preliminary receptor binding studies

Arch Pharm (Weinheim). 1995 Jul-Aug;328(7-8):623-5. doi: 10.1002/ardp.19953280711.

Abstract

New 1-phenyl- and 1-(3-chlorophenyl)piperazines containing a 4-[3-(heterocyclic)propyl] fragment were synthesized. It was found that of all the investigated compounds 11b (Ki = 13 +/- 2 nM) and 8b (Ki = 38 +/- 2 nM) were the most active 5-HT1A and 5-HT2A ligands, respectively. Several derivatives (3a, 4a, 8b, 11b, 12b, 13a, and 13b) were selected as good candidates for new, potential antidepressants on the basis of their 5-HT1A/5-HT2A receptor binding profiles.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 8-Hydroxy-2-(di-n-propylamino)tetralin / pharmacology
  • Animals
  • Antidepressive Agents / chemistry*
  • Antidepressive Agents / pharmacology*
  • Molecular Structure
  • Receptors, Serotonin / drug effects*
  • Structure-Activity Relationship
  • Trazodone / chemistry*
  • Trazodone / pharmacology*

Substances

  • Antidepressive Agents
  • Receptors, Serotonin
  • 8-Hydroxy-2-(di-n-propylamino)tetralin
  • Trazodone