Abstract
As part of an on-going effort to investigate the chemical space requirements for D(2)/5-HT(2A) receptor antagonists as atypical antipsychotics, new 1-aminoindanes were synthesized. The replacement of the heterocycle (oxindole) in ziprasidone with a carbocycle (indane) was well tolerated and was found to retain binding affinities for dopamine D(2), serotonin 5-HT(2A), and serotonin 5-HT(1A). Such compounds hold promise as a new chemical motif with atypical antipsychotic properties for the treatment of schizophrenia and related disorders.
MeSH terms
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Antipsychotic Agents / chemistry
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Antipsychotic Agents / metabolism
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Antipsychotic Agents / pharmacology*
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ERG1 Potassium Channel
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Ether-A-Go-Go Potassium Channels / drug effects
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Humans
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Indans / chemistry
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Indans / metabolism
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Indans / pharmacology*
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Molecular Structure
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Receptor, Serotonin, 5-HT1A / metabolism
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Receptor, Serotonin, 5-HT2A / metabolism
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Receptors, Dopamine D2 / metabolism
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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Indans
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Receptor, Serotonin, 5-HT2A
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Receptors, Dopamine D2
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Receptor, Serotonin, 5-HT1A
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1-aminoindan