Abstract
We report the synthesis of a series of [3.2.1]azabicyclic biaryl ethers as selective agonists of alpha3- and alpha6-containing nicotinic receptors. In particular, compound 17a from this series is a potent alpha3beta4 and alpha6/4beta4 receptor agonist in terms of both binding and functional activity. Compound 17a also shows potent in vivo activity in CNS-mediated animal models that are sensitive to antipsychotic drugs. Compound 17a may thus be a useful tool for studying the role of alpha3beta4 and alpha6/4beta4 nicotinic receptors in CNS pharmacology.
MeSH terms
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Azabicyclo Compounds / chemical synthesis
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Azabicyclo Compounds / chemistry*
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Azabicyclo Compounds / pharmacology
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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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Receptors, Nicotinic / chemistry*
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Receptors, Nicotinic / metabolism
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Structure-Activity Relationship
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Sulfonamides / chemical synthesis
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Sulfonamides / chemistry*
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Sulfonamides / pharmacology
Substances
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Azabicyclo Compounds
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Nicotinic Agonists
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Receptors, Nicotinic
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Sulfonamides
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alpha(4)beta(4) nicotinic receptor
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nicotinic receptor alpha3beta4
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nicotinic receptor alpha6