Studies toward the discovery of the next generation of antidepressants. Part 2: incorporating a 5-HT(1A) antagonist component into a class of serotonin reuptake inhibitors

Bioorg Med Chem Lett. 2002 Feb 11;12(3):307-10. doi: 10.1016/s0960-894x(01)00746-6.

Abstract

The design and synthesis of a novel series of indole derivatives (9) having dual 5-HT transporter reuptake and 5-HT(1A) antagonist activity are described.

MeSH terms

  • Antidepressive Agents, Second-Generation / chemical synthesis*
  • Antidepressive Agents, Second-Generation / pharmacology
  • Carrier Proteins / drug effects
  • Carrier Proteins / metabolism
  • Drug Design
  • Humans
  • Indicators and Reagents
  • Jurkat Cells
  • Kinetics
  • Membrane Glycoproteins / drug effects
  • Membrane Glycoproteins / metabolism
  • Membrane Transport Proteins*
  • Nerve Tissue Proteins*
  • Piperidines / chemistry
  • Piperidines / pharmacology
  • Receptors, Serotonin / drug effects*
  • Receptors, Serotonin, 5-HT1
  • Selective Serotonin Reuptake Inhibitors / chemical synthesis*
  • Selective Serotonin Reuptake Inhibitors / pharmacology
  • Serotonin Antagonists / chemical synthesis*
  • Serotonin Antagonists / pharmacology
  • Serotonin Plasma Membrane Transport Proteins
  • Structure-Activity Relationship

Substances

  • Antidepressive Agents, Second-Generation
  • Carrier Proteins
  • Indicators and Reagents
  • Membrane Glycoproteins
  • Membrane Transport Proteins
  • Nerve Tissue Proteins
  • Piperidines
  • Receptors, Serotonin
  • Receptors, Serotonin, 5-HT1
  • SLC6A4 protein, human
  • Serotonin Antagonists
  • Serotonin Plasma Membrane Transport Proteins
  • Serotonin Uptake Inhibitors
  • indalpine