Abstract
In searching for a next generation molecule to the novel wake promoting agent modafinil (compound 1), a series of fluorene-derived wakefulness enhancing agents were developed and evaluated in rat. Extensive pharmacokinetic studies of a potent member of the series (compound 15) revealed that the wake promotion activity of the analog was likely due to an active metabolite (compound 3).
Copyright © 2012 Elsevier Ltd. All rights reserved.
MeSH terms
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Animals
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Benzhydryl Compounds / chemical synthesis
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Benzhydryl Compounds / chemistry*
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Benzhydryl Compounds / pharmacokinetics
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Brain / drug effects
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Brain / metabolism
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Fluorenes / chemical synthesis
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Fluorenes / chemistry*
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Fluorenes / pharmacokinetics
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Injections, Intraperitoneal
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Modafinil
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Neuroprotective Agents / chemical synthesis
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Neuroprotective Agents / chemistry*
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Neuroprotective Agents / pharmacokinetics
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Rats
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Sulfoxides / chemical synthesis
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Sulfoxides / chemistry*
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Sulfoxides / pharmacokinetics
Substances
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Benzhydryl Compounds
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Fluorenes
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Neuroprotective Agents
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Sulfoxides
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fluoren-9-ol
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Modafinil