Therapeutic Potential of α7 Nicotinic Acetylcholine Receptors

• Published in: Pharmacological reviews Vol. 67; no. 4; pp. 1025 - 1073
• Main Authors: Bertrand, Daniel, Lee, Chih-Hung L, Flood, Dorothy, Marger, Fabrice, Donnelly-Roberts, Diana
• Format: Journal Article
• Language: English
• Published: United States 01.10.2015
• Subjects: alpha7 Nicotinic Acetylcholine Receptor - genetics; alpha7 Nicotinic Acetylcholine Receptor - metabolism; Animals; Brain - metabolism; Cardiovascular Diseases - genetics; Cardiovascular Diseases - physiopathology; Humans; Immune System Diseases - genetics; Immune System Diseases - physiopathology; Nervous System Diseases - genetics; Nervous System Diseases - physiopathology; Polymorphism, Single Nucleotide; Signal Transduction; Structure-Activity Relationship
• ISSN: 1521-0081
• DOI: 10.1124/pr.113.008581

Progress in the fields of neuroscience and molecular biology has identified the forebrain cholinergic system as being important in many higher order brain functions. Further analysis of the genes encoding the nicotinic acetylcholine receptors (nAChRs) has highlighted, in particular, the role of α7 nAChRs in these higher order brain functions as evidenced by their peculiar physiologic and pharmacological properties. As this receptor has gained the attention of scientists from academia and industry, our knowledge of its roles in various brain and bodily functions has increased immensely. We have also seen the development of small molecules that have further refined our understanding of the roles of α7 nAChRs, and these molecules have begun to be tested in clinical trials for several indications. Although a large body of data has confirmed a role of α7 nAChRs in cognition, the translation of small molecules affecting α7 nAChRs into therapeutics has to date only progressed to the stage of testing in clinical trials. Notably, however, most recent human genetic and biochemical studies are further underscoring the crucial role of α7 nAChRs and associated genes in multiple organ systems and disease states. The aim of this review is to discuss our current knowledge of α7 nAChRs and their relevance as a target in specific functional systems and disease states.