Structure Based Design and Profiling of Novel AMPA Receptor Modulators

Description

AMPA receptors mediate the majority of fast excitatory neurotransmission in the mammalian CNS. The role of AMPA receptors appears to be critical in mediating synaptic plasticity and long-term potentiation (LTP), a process which is believed to encode various forms of learning and memory. AMPA receptor modulators have been shown to enhance LTP and are, therefore, under serious consideration as therapeutic agents for a range of neurological disorders including schizophrenia, Alzheimer’s disease, Parkinson’s disease and ADHD. Starting from a screening derived hit, application of biostructural data facilitated rapid optimization to into a series of novel AMPA receptor modulators with excellent developability properties. This is the first demonstration of how structure based drug design can be exploited in an optimization programme for a transmembrane receptor such as an ion channel.

Period	25 Jan 2012
Held at	Glasgow Neuroscience Meeting
Event type	Conference
Location	Glasgow, United Kingdom