Nicotinic Acetylcholine Receptor Ligands
Neuronal nicotinic acetylcholine receptors (nAChRs) are ligand-gated ion channels that mediate fast neurotransmission in the central and peripheral nervous systems. They are broadly distributed across the peripheral nervous system (PNS) and central nervous system (CNS) where they play a wide range of functions from the mediation of different cognitive processes to synaptic transmission from nerves to muscle.
Homomeric α7 nAChRs and heteromeric α4β2 nAChRs are predominantly expressed in the human brain where they contribute to the pathogenesis of a range of neurological disorders including Alzheimer’s disease, Parkinson’s disease, schizophrenia and depression. α7 and α4β2 nAChRs also contribute to other non-neurological diseases, including a correlation of both subtypes with nicotine addiction and nicotine-induced behaviors and the overexpression of α7 nAChRs associated with small-cell lung carcinomas. Given their potential roles in disease development and progression, α7 and α4β2 nAChRs are currently one of the most studied nAChR subtypes.
In our lab we have a long history of research in this field and we are keen on developing novel ligands (agonists, silent agonists, antagonists, positive allosteric modulators) of nAChRs for therapeutic and investigational purposes.