Abstract
The alpha7 subtype of the neuronal nicotinic acetylcholine receptors (nAChRs) was targeted for the design of selective agonists deriving from the quinuclidine scaffold. Arylidene groups at the 3-position and N-methyl quinuclidine were found to be selective agonists with EC(50)s of 1.5 and 40 microM, respectively.
Publication types
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Research Support, N.I.H., Extramural
MeSH terms
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Animals
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Humans
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Nicotinic Agonists / chemical synthesis*
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Nicotinic Agonists / pharmacology*
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Oocytes / metabolism
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Quinuclidines / chemical synthesis*
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Quinuclidines / pharmacology*
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RNA, Messenger / biosynthesis
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RNA, Messenger / genetics
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Receptors, Nicotinic / drug effects*
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Structure-Activity Relationship
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Xenopus
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alpha7 Nicotinic Acetylcholine Receptor
Substances
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Chrna7 protein, human
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Nicotinic Agonists
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Quinuclidines
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RNA, Messenger
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Receptors, Nicotinic
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alpha7 Nicotinic Acetylcholine Receptor