Gamma-lactams--a novel scaffold for highly potent and selective alpha 7 nicotinic acetylcholine receptor agonists.
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.
Enz
Albert
A
Novartis Institutes for Biomedical Research, Neuroscience Disease Area, 4002 Basel, Switzerland.
Feuerbach
Dominik
D
Frederiksen
Mathias U
MU
Gentsch
Conrad
C
Hurth
Konstanze
K
Müller
Werner
W
Nozulak
Joachim
J
Roy
Bernard L
BL
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
C579167:Chrna7 protein, human; C579166:Chrna7 protein, mouse; D007769:Lactams; D018722:Nicotinic Agonists; D011978:Receptors, Nicotinic; D064569:alpha7 Nicotinic Acetylcholine Receptor