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.
Publication types
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Research Support, Non-U.S. Gov't
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Review
MeSH terms
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Animals
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Antipsychotic Agents / pharmacokinetics
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Antipsychotic Agents / pharmacology
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Antipsychotic Agents / therapeutic use*
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Biological Availability
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Clinical Trials as Topic
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Dopamine Antagonists / pharmacokinetics
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Dopamine Antagonists / pharmacology
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Dopamine Antagonists / therapeutic use*
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Dopamine D2 Receptor Antagonists*
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Humans
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Pyridines / pharmacokinetics
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Pyridines / pharmacology
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Pyridines / therapeutic use*
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Pyrroles / pharmacokinetics
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Pyrroles / pharmacology
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Pyrroles / therapeutic use*
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Receptors, Dopamine D4
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Rodentia
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Schizophrenia / drug therapy*
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Schizophrenia / physiopathology
Substances
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3-((4-(4-chlorophenyl)piperazin-1-yl)methyl)-1H-pyrrolo(2,3-b)pyridine
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Antipsychotic Agents
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DRD4 protein, human
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Dopamine Antagonists
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Dopamine D2 Receptor Antagonists
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Pyridines
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Pyrroles
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Receptors, Dopamine D4