Selective α7 Nicotinic Acetylcholine Receptor Ligands

摘要: Neuronal nicotinic acetylcholine receptors (nAChRs) are ligand gated ion channels of broad distribution and structural heterogeneity. Their functional diversity demonstrated involvement in a variety neuronal processes (e.g., sensory gating cognitive function) generated great interest them as targets for therapeutic intervention number neuropathological conditions diseases. In order to control distinct functions pharmacologically, it is important design ligands that selectively interact with receptor subtypes such way maximize the effect minimize adverse effects. The α7 nAChR, CNS subtype, has been most intensively studied nAChR recent years. Selective agonists have developed potential candidates treatment schizophrenia, disorders (including Alzheimers disease), inflammation. Despite early concerns rapid desensitization property would limit their potential, several already advanced clinical trials PH-399733, Pfizer; MEM 3454, Memory Pharmaceuticals/Roche). Further development allosteric modulators pharmaceutically relevant antagonists might expand compounds target nAChRs. this review we briefly describe structure function its vitro vivo pharmacology, discuss relevance these efforts, current progress development.