Abstract
As a continuation of our efforts to develop innovative ligands for D(3), 5-HT(1A), and 5-HT(2A) receptors with low propensity to block hERG channels, we propose a series bishetero(homo)arylpiperazines 5a-m as novel and potent multifunctional ligands characterized by low occupancy at D(2) and 5-HT(2C) receptors.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Antipsychotic Agents / chemical synthesis*
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Antipsychotic Agents / pharmacokinetics
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Antipsychotic Agents / pharmacology
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ERG1 Potassium Channel
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Ether-A-Go-Go Potassium Channels / antagonists & inhibitors
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Ether-A-Go-Go Potassium Channels / metabolism
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Humans
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Ligands
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Mice
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Models, Molecular
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Piperazines / chemical synthesis*
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Piperazines / pharmacokinetics
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Piperazines / pharmacology
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Receptor, Serotonin, 5-HT1A / metabolism*
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Receptor, Serotonin, 5-HT2A / metabolism*
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Receptors, Dopamine D3 / metabolism*
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Structure-Activity Relationship
Substances
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Antipsychotic Agents
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ERG1 Potassium Channel
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Ether-A-Go-Go Potassium Channels
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KCNH2 protein, human
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Ligands
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Piperazines
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Receptor, Serotonin, 5-HT2A
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Receptors, Dopamine D3
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Receptor, Serotonin, 5-HT1A