Abstract
Novel derivatives of the highly potent and selective histamine H3-receptor antagonist ciproxifan (3) with different chain lengths as well as with structural variants of the cyclopropyl ketone moiety have been prepared and screened for their antagonist H3-receptor potencies in vitro and in vivo. Some derivatives (2, 6-8, 12) containing other functionalities were effective in vitro in the same (sub)nanomolar concentration range and in vivo in a remarkably low oral dose.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Cerebral Cortex / physiology
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Drug Design
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Histamine Antagonists / chemical synthesis*
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Histamine Antagonists / chemistry
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Histamine Antagonists / pharmacology
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Histamine Release / drug effects*
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Imidazoles / chemical synthesis*
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Imidazoles / chemistry*
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Imidazoles / pharmacology
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Molecular Structure
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Rats
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Receptors, Histamine H3 / drug effects*
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Receptors, Histamine H3 / physiology
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Structure-Activity Relationship
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Synaptosomes / drug effects
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Synaptosomes / physiology
Substances
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Histamine Antagonists
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Imidazoles
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Receptors, Histamine H3
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ciproxifan