SLV310, a novel, potential antipsychotic, combining potent dopamine D2 receptor antagonism with serotonin reuptake inhibition

Bioorg Med Chem Lett. 2003 Feb 10;13(3):405-8. doi: 10.1016/s0960-894x(02)00996-4.

Abstract

In this paper, SLV310 is presented as a novel, potential antipsychotic displaying the interesting combination of potent dopamine D(2) receptor antagonism and serotonin reuptake receptor inhibition in one molecule. As such, SLV310 could be useful in treating a broad range of symptoms in schizophrenia. This paper describes the structure-activity relationship in a series of compounds leading to SLV310 (6b, 2-[4-[4-(5-fluoro-1H-indol-3-yl)-3,6-dihydro-2H-pyridin-1-yl]-butyl]-phthalimide) together with pharmacological data showing the unique profile of this compound.

MeSH terms

  • 5-Hydroxytryptophan / pharmacology
  • Animals
  • Antipsychotic Agents / pharmacology*
  • Apomorphine / antagonists & inhibitors
  • Behavior, Animal / drug effects
  • CHO Cells
  • Cricetinae
  • Dopamine Agonists / pharmacology
  • Dopamine Antagonists / pharmacology*
  • Dopamine D2 Receptor Antagonists*
  • Dose-Response Relationship, Drug
  • Humans
  • Indicators and Reagents
  • Mice
  • Motor Activity / drug effects
  • Phthalimides / chemical synthesis*
  • Phthalimides / pharmacology*
  • Pyridines / chemical synthesis*
  • Pyridines / pharmacology*
  • Selective Serotonin Reuptake Inhibitors / pharmacology*
  • Structure-Activity Relationship

Substances

  • 2-(4-(4-(5-fluoro-1H-indol-3-yl)-3,6-dihydro-2H-pyridin-1-yl)butyl)-phthalimide
  • Antipsychotic Agents
  • Dopamine Agonists
  • Dopamine Antagonists
  • Dopamine D2 Receptor Antagonists
  • Indicators and Reagents
  • Phthalimides
  • Pyridines
  • Serotonin Uptake Inhibitors
  • 5-Hydroxytryptophan
  • Apomorphine