Schizophrenia and L-745,870, a novel dopamine D4 receptor antagonist.

Abstract

The discovery of a novel high-affinity and selective dopamine D4 receptor antagonist, L-745,870, and the results of clinical trials with this compound are reviewed. Despite several lines of evidence which suggest that a selective D4 receptor antagonist may be an effective antipsychotic agent with a lower propensity to induce extrapyramidal side-effects, L-745,870 was ineffective as an antipsychotic in humans.

• Authors: L J Bristow, M S Kramer, J Kulagowski, S Patel, C I Ragan, G R Seabrook
• Journal: Trends in pharmacological sciences (Trends Pharmacol Sci) Vol. 18 Issue 6 Pg. 186-8 (Jun 1997) ISSN: 0165-6147 [Print] England
• PMID: 9226994 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't, Review)

Chemical References

• 3-((4-(4-chlorophenyl)piperazin-1-yl)methyl)-1H-pyrrolo(2,3-b)pyridine
• Antipsychotic Agents
• DRD4 protein, human
• Dopamine Antagonists
• Dopamine D2 Receptor Antagonists
• Pyridines
• Pyrroles
• Receptors, Dopamine D4

Topics

• Animals
• Antipsychotic Agents (pharmacokinetics, pharmacology, therapeutic use)
• Biological Availability
• Clinical Trials as Topic
• Dopamine Antagonists (pharmacokinetics, pharmacology, therapeutic use)
• Dopamine D2 Receptor Antagonists
• Humans
• Pyridines (pharmacokinetics, pharmacology, therapeutic use)
• Pyrroles (pharmacokinetics, pharmacology, therapeutic use)
• Receptors, Dopamine D4
• Rodentia
• Schizophrenia (drug therapy, physiopathology)