Abstract
With the aim of identifying structurally novel, centrally acting histamine H(3) antagonists, a series of 2-(4-alkylpiperazin-1-yl)quinolines was prepared. Systematic variation of the substituents led to highly potent histamine H(3) antagonists with low polar surface area and appropriate log P for blood-brain barrier penetration.
MeSH terms
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Animals
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Biochemistry / methods
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Blood-Brain Barrier / drug effects
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Drug Evaluation, Preclinical / methods
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Histamine Antagonists / chemistry*
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Histamine Antagonists / pharmacology*
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Humans
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Imidazoles / chemistry
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Inhibitory Concentration 50
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Quinolines / chemistry
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Quinolines / pharmacology
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Rats
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Receptors, Histamine H3 / drug effects*
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Receptors, Histamine H3 / metabolism
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Receptors, Serotonin / drug effects
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Receptors, Serotonin / metabolism
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Structure-Activity Relationship
Substances
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Histamine Antagonists
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Imidazoles
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Quinolines
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Receptors, Histamine H3
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Receptors, Serotonin