Abstract
SAR studies for novel non-imidazole containing H(3) receptor antagonists with high potency and selectivity for rat H(3) receptors are described. A high throughput screening lead, A-923, was further elaborated in a systematic manner to clarify a pharmacophore for this class of aryloxyalkyl piperazine based compounds.
MeSH terms
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Amines / chemistry
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Animals
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Binding, Competitive
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Carbamates / chemistry
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Cerebral Cortex / metabolism
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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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Ketones / chemistry*
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Kinetics
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Ligands
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Piperazines / chemistry*
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Rats
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Receptors, Histamine H1 / metabolism
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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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A-923 compound
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Amines
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Carbamates
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Histamine Antagonists
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Ketones
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Ligands
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Piperazines
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Receptors, Histamine H1
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Receptors, Histamine H2
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Receptors, Histamine H3