Quinuclidines as selective agonists for alpha-7 nicotinic acetylcholine receptors.
The alpha7 subtype of the neuronal nicotinic acetylcholine receptors (nAChRs) was targeted for the design of selective agonists deriving from the quinuclidine scaffold. Arylidene groups at the 3-position and N-methyl quinuclidine were found to be selective agonists with EC(50)s of 1.5 and 40 microM, respectively.
Leonik
Fedra M
FM
Department of Chemistry, University of Florida, Gainesville, FL 32611-7200, USA.
Papke
Roger L
RL
Horenstein
Nicole A
NA
D000818:Animals; D006801:Humans; D018722:Nicotinic Agonists / Q000138:chemical synthesis* / Q000494:pharmacology*; D009865:Oocytes / Q000378:metabolism; D011812:Quinuclidines / Q000138:chemical synthesis* / Q000494:pharmacology*; D012333:RNA, Messenger / Q000096:biosynthesis / Q000235:genetics; D011978:Receptors, Nicotinic / Q000187:drug effects*; D013329:Structure-Activity Relationship; D014981:Xenopus; D064569:alpha7 Nicotinic Acetylcholine Receptor
C579167:Chrna7 protein, human; D018722:Nicotinic Agonists; D011812:Quinuclidines; D012333:RNA, Messenger; D011978:Receptors, Nicotinic; D064569:alpha7 Nicotinic Acetylcholine Receptor