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.
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container_end_page 2178
container_issue 16
container_start_page 2173
container_title Bioorganic & medicinal chemistry letters
container_volume 8
creator 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.
description 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 disease and pain. 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 α2β4 and α4β4 nAChRs, was shown to be active in animal models of Parkinson's disease and pain.
doi_str_mv 10.1016/S0960-894X(98)00394-1
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Compounds 2 (SIB-1663), which selectively activated human recombinant α2β4 and α4β4 nAChRs, was shown to be active in animal models of Parkinson's disease and pain. 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 α2β4 and α4β4 nAChRs, was shown to be active in animal models of Parkinson's disease and pain.</abstract><cop>Oxford</cop><pub>Elsevier Ltd</pub><pmid>9873508</pmid><doi>10.1016/S0960-894X(98)00394-1</doi><tpages>6</tpages></addata></record>
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subjects 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
title Conformationally restricted analogues of nicotine and anabasine
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