Nicotinic acetylcholine receptors (nAChRs) are a pharmacologically diverse family of neurotransmitter receptors expressed in vertebrates and invertebrates. They are targets for insecticides but are also important targets for pharmaceutical drug discovery. Research in our lab is focused on understanding the pharmacological diversity of nAChRs � our principal experimental approach being the use of molecular biological and pharmacological techniques to examine recombinant nAChRs. Studies conducted with insect nAChRs have helped to understand the mechanism of action of, and the role of target-site resistance to, insecticides such as neonicotinoids and spinosad. In addition, studies conducted with both insect and mammalian nAChRs have revealed remarkable diversity in pharmacological properties amongst this important family of receptors. For example, in addition agonists and antagonists that interact with the receptor's extracellular 'orthosteric' binding site, a variety of allosteric modulators (including potentiators, inhibitors and allosteric agonists) have been identified that interact with the receptor's transmembrane domain.

Nicotinic acetylcholine receptors: Insecticides and pharmacological diversity

248th National Meeting (2014)

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