Abstract
A series of imidazole-containing (non-)chiral carbamates were tested at human histamine H(3) receptor (H(3)R). All compounds displayed K(i) values below 100 nM. A trend for a stereoselectivity at human H(3)R was observed for the chiral alpha-branched ligands. Selected compounds were also tested at human histamine H(4) receptor and showed moderate to weak affinities (118-1460 nM).
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Carbamates / chemical synthesis
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Carbamates / chemistry
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Carbamates / pharmacology*
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Drug Design
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Humans
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Imidazoles / chemistry
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Molecular Structure
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Receptors, G-Protein-Coupled / drug effects*
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Receptors, Histamine / drug effects*
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Receptors, Histamine H3 / drug effects*
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Receptors, Histamine H4
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Stereoisomerism
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Structure-Activity Relationship
Substances
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Carbamates
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HRH4 protein, human
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Imidazoles
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Receptors, G-Protein-Coupled
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Receptors, Histamine
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Receptors, Histamine H3
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Receptors, Histamine H4
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imidazole