Abstract
Maintaining excitatory/inhibitory balance is essential for the synchronised signalling required for cognitive function and is impaired in schizophrenia. Evidence from clinical and pre-clinical research have implicated GABAergic interneuronsin this synchronised signalling. Therefore, modulating interneuron activity has therapeutic potential for improving cognitive function. The 5-HT3 receptor (5-HTR3) is expressed on a subset of interneurons in the cortex and existing antagonists of this receptor have been shown to modulate cortical function, but have poor CNS drug-like characteristics and unsuitable pharmacokinetic or off-target activity, precluding use for schizophrenia. Here we describe the development of CVN058, a 5-HTR3 antagonist with good CNS properties and potential for the treatment of cognitive impairment associated with schizophrenia (CIAS).
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