title: Gamma-lactams--a novel scaffold for highly potent and selective alpha 7 nicotinic acetylcholine receptor agonists.
abstract: A novel class of alpha7 nicotinic acetylcholine receptor (nAChR) agonists has been discovered through high-throughput screening. The cis gamma-lactam scaffold has been optimized to reveal highly potent and selective alpha7 nAChR agonists with in vitro activity and selectivity and with good brain penetration in mice.
authors.affiliation: Novartis Institutes for Biomedical Research, Neuroscience Disease Area, 4002 Basel, Switzerland.
authors.forename: Albert
authors.initials: A
authors.lastname: Enz
authors.forename: Dominik
authors.initials: D
authors.lastname: Feuerbach
authors.forename: Mathias U
authors.initials: MU
authors.lastname: Frederiksen
authors.forename: Conrad
authors.initials: C
authors.lastname: Gentsch
authors.forename: Konstanze
authors.initials: K
authors.lastname: Hurth
authors.forename: Werner
authors.initials: W
authors.lastname: Müller
authors.forename: Joachim
authors.initials: J
authors.lastname: Nozulak
authors.forename: Bernard L
authors.initials: BL
authors.lastname: Roy
mesh_terms: D000818:Animals; D001665:Binding Sites; D001921:Brain / Q000378:metabolism; D006801:Humans; D007769:Lactams / Q000737:chemistry*; D051379:Mice; D018722:Nicotinic Agonists / Q000737:chemistry / Q000378:metabolism*; D011485:Protein Binding; D011817:Rabbits; D011978:Receptors, Nicotinic / Q000737:chemistry / Q000378:metabolism*; D064569:alpha7 Nicotinic Acetylcholine Receptor
chemical_list: C579167:Chrna7 protein, human; C579166:Chrna7 protein, mouse; D007769:Lactams; D018722:Nicotinic Agonists; D011978:Receptors, Nicotinic; D064569:alpha7 Nicotinic Acetylcholine Receptor