Abstract
Compounds containing a substituted 4-piperidinol core have been found to be potent antagonists of the human H(3) receptor. The compounds exhibited up to a 60-fold preference for inhibiting the human H(3) receptor over the mouse and showed a low binding affinity for the hERG channel.
Copyright © 2010 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Crystallography, X-Ray
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Ether-A-Go-Go Potassium Channels / drug effects
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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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Indicators and Reagents
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Mice
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Models, Molecular
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Piperidines / chemical synthesis*
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Piperidines / pharmacology*
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Stereoisomerism
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Structure-Activity Relationship
Substances
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Ether-A-Go-Go Potassium Channels
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Histamine H3 Antagonists
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Indicators and Reagents
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Piperidines