Nicotinic acetylcholine receptors: an overview on drug discovery

Abstract

Background: Nicotinic acetylcholine receptors (nAChRs) are ligand-gated ion channels that participate in many physiological functions. Receptors result from the assembly of five homologous or heterologous subunits that form the ligand-binding site and an ionic pore. In vertebrates, 17 subunits have been identified, α (1 – 10), β (1 – 4), γ, δ and ϵ. Assembly of different subunit combinations allows a diversity of physiological and pharmacological properties. Objective: To review the putative involvement of nAChRs in several diseases. Methods: We discuss the expression pattern of the subunits, the pharmacological tools for distinguishing them and their role in pathogenesis. Results/conclusion: Long-standing efforts in this field should soon result in the finding of new molecules that might be applicable to situations ranging from neurological diseases to immune treatments.

Keywords::

• addiction
• Alzheimer's disease
• audition
• cardiovascular dysfunction
• epilepsy
• immune system
• ligand gated channel
• neuromuscular junction
• nicotinic acetylcholine receptors
• pain
• Parkinson's disease
• schizophrenia
• skin
• therapeutic treatments
• α4β2
• α6
• α7