Abstract
Recently novel leads for histamine H3 receptor antagonists of the non-imidazole type have been described. As a continuation of this research eleven new carbamate derivatives possessing an additional ether functionality were prepared. The compounds were evaluated in vitro for their antagonist activity on isolated organs of guinea-pig (GP) H3 as well as H2, H1, and M3 receptors, respectively. All compounds investigated possessed moderate antagonist affinities at guinea-pig histamine H3 receptors (pA2 6.11-6.76). An ether functionality introduced in different places of the lipophilic part of carbamates differently influenced activity and selectivity toward H3, M3, and other histamine receptors tested.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Carbamates / chemical synthesis*
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Carbamates / pharmacology*
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Electric Stimulation
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Ethers / chemistry
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Guinea Pigs
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Histamine Antagonists / pharmacology*
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Histamine H1 Antagonists / pharmacology
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Histamine H2 Antagonists / pharmacology
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Ileum / drug effects
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In Vitro Techniques
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Magnetic Resonance Spectroscopy
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Muscle Contraction / drug effects
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Muscle, Smooth / drug effects
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Piperidines / chemical synthesis*
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Piperidines / pharmacology*
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Receptor, Muscarinic M3
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Receptors, Histamine H3 / drug effects*
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Receptors, Muscarinic / drug effects
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Structure-Activity Relationship
Substances
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Carbamates
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Ethers
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Histamine Antagonists
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Histamine H1 Antagonists
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Histamine H2 Antagonists
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Piperidines
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Receptor, Muscarinic M3
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Receptors, Histamine H3
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Receptors, Muscarinic