Abstract
A new series of H(3) antagonists derived from the natural product Conessine are presented. Several compounds from these new series retain the potency and selectivity of earlier diamine based analogs while exhibiting improved PK characteristics. One compound (3u) demonstrated functional antagonism of the H(3) receptor in an in vivo pharmacological model.
MeSH terms
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Alkaloids / pharmacokinetics*
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Animals
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Binding, Competitive / drug effects
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Central Nervous System / drug effects
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Chemistry, Pharmaceutical / methods*
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Drug Design
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Histamine Antagonists / chemistry
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Histamine Antagonists / pharmacology*
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Kinetics
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Models, Chemical
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Molecular Structure
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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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Alkaloids
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Histamine Antagonists
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Receptors, Histamine H3
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conessine