Abstract
Utilizing atypical wake-promoting agent modafinil (inactive in both rH(3) and hH(3) binding assays) as a launching pad, a series of sulfinyl- and sulfone-derived H(3) receptor inverse agonists were developed. Brain-permeable compound 27, a potent member of the series displayed excellent selectivity against related family members (H(1), H(2), and H(4) receptors).
© 2012 John Wiley & Sons A/S.
MeSH terms
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Administration, Oral
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Animals
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Benzhydryl Compounds / agonists
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Benzhydryl Compounds / chemistry*
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Benzhydryl Compounds / pharmacokinetics
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Central Nervous System Stimulants / agonists
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Central Nervous System Stimulants / chemistry
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Central Nervous System Stimulants / pharmacokinetics
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Drug Inverse Agonism
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Half-Life
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Kinetics
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Modafinil
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Protein Binding
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Pyrrolidines / agonists
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Pyrrolidines / chemistry*
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Pyrrolidines / pharmacokinetics
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Rats
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Receptors, Histamine H3 / chemistry*
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Receptors, Histamine H3 / metabolism
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Structure-Activity Relationship
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Sulfones / agonists
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Sulfones / chemistry*
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Sulfones / pharmacokinetics
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Wakefulness / drug effects
Substances
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Benzhydryl Compounds
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Central Nervous System Stimulants
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Pyrrolidines
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Receptors, Histamine H3
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Sulfones
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Modafinil