Abstract
Biaryl substituted 2,5-diazabicyclo[2.2.1]heptanes have been synthesized and tested for their affinity toward alpha7 neuronal nicotinic receptors (NNRs). SAR studies established that 5-N-methyl substituent, heteroaryl linker and the nature of terminal aryl group are critical for the ligand to achieve potent alpha7 NNR agonist activity.
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MeSH terms
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Animals
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Heptanes / chemical synthesis
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Heptanes / chemistry*
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Heptanes / pharmacology*
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Humans
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Ligands
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Neurons / metabolism
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Nicotinic Agonists / chemical synthesis
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Nicotinic Agonists / chemistry*
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Protein Binding
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Radioligand Assay
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Rats
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Receptors, Nicotinic / drug effects
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Receptors, Nicotinic / metabolism
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Structure-Activity Relationship
Substances
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Heptanes
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Ligands
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Nicotinic Agonists
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Receptors, Nicotinic