title: Conformationally restricted analogues of nicotine and anabasine.
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.
authors.affiliation: SIBIA Neurosciences Inc., La Jolla, CA 92037, USA.
authors.forename: J M
authors.initials: JM
authors.lastname: Vernier
authors.forename: H
authors.initials: H
authors.lastname: Holsenback
authors.forename: N D
authors.initials: ND
authors.lastname: Cosford
authors.forename: J P
authors.initials: JP
authors.lastname: Whitten
authors.forename: F
authors.initials: F
authors.lastname: Menzaghi
authors.forename: R
authors.initials: R
authors.lastname: Reid
authors.forename: T S
authors.initials: TS
authors.lastname: Rao
authors.forename: A I
authors.initials: AI
authors.lastname: Sacaan
authors.forename: G K
authors.initials: GK
authors.lastname: Lloyd
authors.forename: C M
authors.initials: CM
authors.lastname: Suto
authors.forename: L E
authors.initials: LE
authors.lastname: Chavez-Noriega
authors.forename: M S
authors.initials: MS
authors.lastname: Washburn
authors.forename: A
authors.initials: A
authors.lastname: Urrutia
authors.forename: I A
authors.initials: IA
authors.lastname: McDonald
mesh_terms: D000691:Anabasine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D000818:Animals; D000978:Antiparkinson Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D002118:Calcium / Q000378:metabolism; D002460:Cell Line; D018679:Cholinergic Agonists / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D015195:Drug Design; D006801:Humans; D046911:Macromolecular Substances; D008968:Molecular Conformation; D009474:Neurons / Q000378:metabolism*; D009538:Nicotine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D010302:Parkinson Disease, Secondary / Q000188:drug therapy; D010880:Piperidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011725:Pyridines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011994:Recombinant Proteins / Q000187:drug effects; D013329:Structure-Activity Relationship; D014162:Transfection
chemical_list: D000978:Antiparkinson Agents; D018679:Cholinergic Agonists; D046911:Macromolecular Substances; D010880:Piperidines; D011725:Pyridines; D011994:Recombinant Proteins; D009538:Nicotine; D000691:Anabasine; D002118:Calcium