Homomeric α7 nicotinic acetylcholine receptors (nAChRs) are implicated in the regulation
of cognitive processes such as memory and attention and have potential as therapeutic
targets for the treatment of the cognitive deficits associated with schizophrenia. Though numerous
α7 nAChR agonists have been developed, and several have progressed to clinical trials, these
are derived from few common chemotypes. Consequently, many of these α7 nAChR clinical
candidates share unfavorable side-effect profile. SEN12333 represents a novel chemotype for the
development of α7 nAChR agonists, and exploration of this scaffold has produced structurally diverse ligands with promising pharmacological
properties. This review will summarize structure-affinity and -activity relationships surrounding analogs of SEN12333.
Keywords: Nicotinic receptors, schizophrenia, Alzheimer’s disease, SEN12333.
Rights & PermissionsPrintExport