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

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.

• Authors: Rolf van Hes, Pieter Smid, Cees N J Stroomer, Koos Tipker, Martin Th M Tulp, Jan A M van der Heyden, Andrew C McCreary, Mayke B Hesselink, Chris G Kruse
• Journal: Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 13 Issue 3 Pg. 405-8 (Feb 10 2003) ISSN: 0960-894X [Print] England
• PMID: 12565939 (Publication Type: Journal Article)

Chemical References

• 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

Topics

• 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, pharmacology)
• Pyridines (chemical synthesis, pharmacology)
• Selective Serotonin Reuptake Inhibitors (pharmacology)
• Structure-Activity Relationship