AMPA receptor positive allosteric modulators – a case history

Ward, Simon (2014) AMPA receptor positive allosteric modulators – a case history. In: Cox, Brian and Gosling, Martin (eds.) Ion channel drug discovery. RSC drug discovery . Royal Society of Chemistry, pp. 105-134. ISBN 9781849731867

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Significant advances have been made over recent years in our understanding of the tremendous complexity underlying the function of the human brain, in particular gaining insight into the mechanisms of synaptic plasticity which are key to developmental, adaptive and learning processes. Glutamate, the major excitatory neurotransmitter in the central nervous system (CNS), is of critical importance to these processes, acting at chemical synapses on two major classes of receptors – the metabotropic family of G-protein coupled receptors (mGluRs 1-8), and ionotropic family of ion channel forming receptors (iGluRs). The latter comprises the α-amino-3-hydroxyl-5-methyl-4-isoxazole-propionic acid (AMPA), N-methyl-d-aspartate (NMDA) and kainate receptors. Despite similarities shared within this ion channel family, there exist clear structural and pharmacological differences which underlie their individual modes of action. This chapter provides a case history of ion channel lead optimisation, discusses challenges in lead optimisation and selection of clinical discovery candidates, and thoughts on the future of drug discovery programmes.

Item Type: Book Section
Schools and Departments: School of Life Sciences > Chemistry
Subjects: Q Science > QD Chemistry
Depositing User: Tom Gittoes
Date Deposited: 09 Mar 2015 17:03
Last Modified: 19 Feb 2016 09:20
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