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The positive mnemonic effects of positive modulators of the α-amino-3-hydroxy-5-methyl-4-isoxazole-propionic acid (AMPA) receptor have been well documented in the preclinical setting. This encouraging level of target validation has galvanised efforts by a number of research organisations towards identifying developable and efficacious AMPA receptor modulators for the treatment of cognitive deficits associated with both schizophrenia and Alzheimer’s Disease. This contribution will give an overview of significant developments in the area, including chemical classes studied and associated pharmacology, as well as discussing the impact of Structure Based Drug Design (SBDD) in efforts to identify new chemotypes for this important molecular target.

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