Abstract
We report the synthesis and pharmacological properties of several cytisine derivatives. Among them, two 10-substituted derivatives showed much higher selectivities for the alpha4beta2 nAChR subtype in binding assays than cytisine. The 9-vinyl derivative was found to have a very similar agonist activity profile to that of cytisine.
Publication types
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Research Support, N.I.H., Extramural
MeSH terms
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Alkaloids / chemical synthesis
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Alkaloids / chemistry*
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Alkaloids / pharmacology*
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Azocines / chemical synthesis
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Azocines / chemistry
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Azocines / pharmacology
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Cholinergic Agonists / chemical synthesis
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Cholinergic Agonists / chemistry
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Cholinergic Agonists / pharmacology
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Hydrophobic and Hydrophilic Interactions
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Ligands
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Molecular Structure
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Nicotine / chemical synthesis
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Nicotine / chemistry*
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Nicotine / classification
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Nicotine / pharmacology*
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Quinolizines / chemical synthesis
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Quinolizines / chemistry
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Quinolizines / pharmacology
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Receptors, Cholinergic / metabolism
Substances
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Alkaloids
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Azocines
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Cholinergic Agonists
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Ligands
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Quinolizines
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Receptors, Cholinergic
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cytisine
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Nicotine