Conformationally restricted analogues of nicotine and anabasine

A series of conformationally restricted analogues of nicotine has been synthesized and evaluated as agonists of neuronal acetylcholine receptors. Compounds 2 (SIB-1663), which selectively activated human recombinant α2β4 and α4β4 nAChRs, was shown to be active in animal models of Parkinson's di...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 1998-08, Vol.8 (16), p.2173-2178
Hauptverfasser:	Vernier, Jean-Michel, Holsenback, Heather, Cosford, Nicholas D.P., Whitten, Jeffrey P., Menzaghi, Frédérique, Reid, Richard, Rao, Tadimeti S., Sacaan, Aida I., Lloyd, G.Kenneth, Suto, Carla M., Chavez-Noriega, Laura E., Washburn, Mark S., Urrutia, Arturo, McDonald, Ian A.
Format:	Artikel
Sprache:	eng
Schlagworte:	Anabasine - analogs & derivatives Anabasine - chemical synthesis Anabasine - chemistry Anabasine - pharmacology Animals Antiparkinson Agents - chemical synthesis Antiparkinson Agents - chemistry Antiparkinson Agents - pharmacology Biological and medical sciences Calcium - metabolism Cell Line Cholinergic Agonists - chemical synthesis Cholinergic Agonists - chemistry Cholinergic Agonists - pharmacology Cholinergic system Drug Design Humans Macromolecular Substances Medical sciences Molecular Conformation Neurons - metabolism Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Nicotine - analogs & derivatives Nicotine - chemical synthesis Nicotine - chemistry Nicotine - pharmacology Parkinson Disease, Secondary - drug therapy Pharmacology. Drug treatments Piperidines - chemical synthesis Piperidines - chemistry Piperidines - pharmacology Pyridines - chemical synthesis Pyridines - chemistry Pyridines - pharmacology Recombinant Proteins - drug effects Structure-Activity Relationship Transfection
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