Title:AMPA Receptor Positive Allosteric Modulators: Potential for the Treatment of Neuropsychiatric and Neurological Disorders
Volume: 16
Issue: 29
Author(s): Tristan Reuillon, Simon E. Ward and Paul Beswick
Affiliation:
Keywords:
AMPA receptor, AMPAR positive modulators, Cognition deficit, DMPK properties, Glutamate, Ion channel, X-ray
crystallography.
Abstract: The neurotransmitter glutamate and its receptors have long been of interest to scientists involved
in pharmaceutical research since dysfunction of the glutamatergic signalling pathway has been
associated with the pathophysiology of several psychiatric and neurological disorders. The research
on AMPAR positive allosteric modulators offers opportunities to modulate fast excitatory synaptic
transmission and identify new potential therapeutic agents for a range of neurodiseases. The field of
AMPAR modulators continues to be a dynamic area of drug discovery with a pronounced diversification
of the chemotypes explored in recent years. This article reviews literature published in this area
in the last 6 years, focusing on the new core templates, some derived from high-throughput screens,
with an emphasis on structure-activity relationships, drug metabolism and pharmacokinetics properties,
and pharmacological profiles of these series.
