Abstract
A series of conformationally restricted analogues of nicotine has been synthesized and evaluated as agonists of neuronal acetylcholine receptors. Compound 2 (SIB-1663), which selectively activated human recombinant alpha 2 beta 4 and alpha 4 beta 4 nAChRs, was shown to be active in animal models of Parkinson's disease and pain.
MeSH terms
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Anabasine / analogs & derivatives*
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Anabasine / chemical synthesis
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Anabasine / chemistry*
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Anabasine / pharmacology
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Animals
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Antiparkinson Agents / chemical synthesis
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Antiparkinson Agents / chemistry
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Antiparkinson Agents / pharmacology
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Calcium / metabolism
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Cell Line
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Cholinergic Agonists / chemical synthesis*
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Cholinergic Agonists / chemistry
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Cholinergic Agonists / pharmacology
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Drug Design
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Humans
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Macromolecular Substances
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Molecular Conformation
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Neurons / metabolism*
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Nicotine / analogs & derivatives*
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Nicotine / chemical synthesis
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Nicotine / chemistry*
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Nicotine / pharmacology
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Parkinson Disease, Secondary / drug therapy
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Piperidines / chemical synthesis*
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Piperidines / chemistry
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Piperidines / pharmacology
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Pyridines / chemical synthesis*
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Pyridines / chemistry
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Pyridines / pharmacology
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Recombinant Proteins / drug effects
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Structure-Activity Relationship
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Transfection
Substances
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Antiparkinson Agents
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Cholinergic Agonists
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Macromolecular Substances
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Piperidines
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Pyridines
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Recombinant Proteins
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Nicotine
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Anabasine
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Calcium