Abstract
The synthesis and structure-activity relationship of a series of carbamate potentiators of alpha4beta2 nAChR is reported herein. These compounds were highly selective for alpha4beta2 over other nAChR subtypes. In addition, compounds increased the response of alpha4beta2 nAChRs to acetylcholine, as measured with patch-clamp electrophysiology.
MeSH terms
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Acetylcholine / chemistry
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Calcium / chemistry
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Carbamates / chemistry
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Chemistry, Pharmaceutical / methods*
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Drug Design
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Humans
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Models, Chemical
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Nervous System / metabolism
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Neurons / metabolism
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Patch-Clamp Techniques
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Pyrazoles / chemistry
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Pyridines / chemistry
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Receptors, Nicotinic / chemistry*
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Receptors, Nicotinic / metabolism
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Structure-Activity Relationship
Substances
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Carbamates
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Pyrazoles
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Pyridines
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Receptors, Nicotinic
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nicotinic receptor alpha4beta2
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Acetylcholine
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Calcium