Abstract
Epibatidine is a potent but nonselective nAChR agonist. Its biological effects appear to be mediated largely by alpha4beta2 nAChRs. Surprisingly, only a limited number of epibatidine analogues have been synthesized and evaluated in in vitro assays. Even fewer analogues have received in vivo pharmacological evaluation. In this paper, SAR studies directed toward epibatidine analogues will be reviewed.
Publication types
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Research Support, U.S. Gov't, P.H.S.
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Review
MeSH terms
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Bridged Bicyclo Compounds, Heterocyclic / chemical synthesis
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Bridged Bicyclo Compounds, Heterocyclic / chemistry*
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Bridged Bicyclo Compounds, Heterocyclic / pharmacology
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Molecular Structure
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Nicotinic Agonists / chemical synthesis
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Nicotinic Agonists / chemistry*
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Nicotinic Agonists / pharmacology
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Pyridines / chemical synthesis
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Pyridines / chemistry*
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Pyridines / pharmacology
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Receptors, Nicotinic / drug effects
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Stereoisomerism
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Structure-Activity Relationship
Substances
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Bridged Bicyclo Compounds, Heterocyclic
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Nicotinic Agonists
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Pyridines
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Receptors, Nicotinic
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nicotinic receptor alpha4beta2
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epibatidine