Abstract
Novel diamine derivatives containing imidazolidinylidene propanedinitrile were synthesized and evaluated for histamine H(3) receptor-binding affinities. High-affinity ligands 3d, 3k, and 3n showed potent H(3) receptor antagonism and excellent selectivity over human H(1), H(2) and H(4) receptors.
MeSH terms
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Animals
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COS Cells
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Chlorocebus aethiops
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Diamines / chemical synthesis
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Diamines / pharmacology*
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Histamine H3 Antagonists / chemical synthesis
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Histamine H3 Antagonists / pharmacology*
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Humans
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Imidazolidines / chemistry
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Imidazolidines / pharmacology*
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Ligands
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Models, Chemical
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Nitriles / chemistry
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Nitriles / pharmacology*
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Receptors, Histamine H1 / drug effects*
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Receptors, Histamine H1 / metabolism
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Receptors, Histamine H2 / drug effects*
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Receptors, Histamine H2 / metabolism
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Receptors, Histamine H3 / drug effects*
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Receptors, Histamine H3 / metabolism
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Stereoisomerism
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Structure-Activity Relationship
Substances
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Diamines
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Histamine H3 Antagonists
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Imidazolidines
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Ligands
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Nitriles
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Receptors, Histamine H1
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Receptors, Histamine H2
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Receptors, Histamine H3