Abstract
High throughput screening, using the recombinant human H(3) receptor, was used to identify novel histamine H(3) receptor antagonists. Evaluation of the lead compounds ultimately afforded potent, selective, orally bioavailable compounds (e.g., 38) with favorable blood-brain barrier penetration.
MeSH terms
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Administration, Oral
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Animals
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Biological Availability
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Blood-Brain Barrier
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Brain Chemistry
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Histamine Antagonists / chemical synthesis*
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Histamine Antagonists / pharmacokinetics*
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Histamine Antagonists / pharmacology
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Humans
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Ligands
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Pyridines / chemical synthesis
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Pyridines / pharmacokinetics
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Pyridines / pharmacology
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Radioligand Assay
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Rats
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Receptors, Histamine H3 / chemistry*
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Structure-Activity Relationship
Substances
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Histamine Antagonists
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Ligands
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Pyridines
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Receptors, Histamine H3