Abstract
Following the discovery of the human histamine H4 receptor, a high throughput screen of our corporate compound collection identified compound 6 as a potential lead. Investigation of the SAR resulted in the discovery of novel compounds 10e and 10l, which are the first potent and selective histamine H4 receptor antagonists to be described.
MeSH terms
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Animals
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Cell Line
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Dose-Response Relationship, Drug
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Histamine Antagonists / chemistry*
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Histamine Antagonists / metabolism
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Histamine Antagonists / pharmacology*
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Humans
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Indoles / chemistry
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Indoles / metabolism
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Indoles / pharmacology
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Kinetics
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Ligands
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Neurons / cytology
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Piperazines / chemistry*
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Piperazines / metabolism
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Piperazines / pharmacology*
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Radioligand Assay
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Rats
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Receptors, Cell Surface / drug effects*
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Receptors, Cell Surface / genetics
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Receptors, Cell Surface / metabolism
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Receptors, G-Protein-Coupled*
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Receptors, Histamine H4
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Receptors, Histamine*
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Recombinant Proteins / drug effects
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Recombinant Proteins / genetics
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Recombinant Proteins / metabolism
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Structure-Activity Relationship
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Transfection
Substances
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HRH4 protein, human
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Histamine Antagonists
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Hrh4 protein, rat
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Indoles
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Ligands
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Piperazines
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Receptors, Cell Surface
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Receptors, G-Protein-Coupled
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Receptors, Histamine
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Receptors, Histamine H4
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Recombinant Proteins