AV965

AV-965 acts by blocking the 5-HT_1A receptor, a G protein-coupled receptor prevalent in the brain, especially in the raphe nuclei (where it acts as an autoreceptor) and in limbic and cortical regions (where it functions as a heteroreceptor).^[1][2] Antagonism of 5-HT_1A autoreceptors can disinhibit serotonergic neuron firing, potentially enhancing serotonin release and improving cognitive and behavioral outcomes in conditions marked by reduced serotonergic tone.^[1][3]

AV-965 has entered early clinical trials, with Phase I studies in healthy volunteers demonstrating a favorable safety and tolerability profile.^[4]

The compound is under investigation for the treatment of cognitive impairment, particularly in schizophrenia and possibly Alzheimer’s disease.^[5][6] The rationale for targeting the 5-HT_1A receptor is supported by research showing its influence on cognition, mood, and anxiety.^[1][7]

Avera Pharmaceuticals is developing AV-965.^[5] Selective 5-HT_1A receptor modulation is a promising strategy in neuropsychiatric drug development, as both agonists and antagonists have shown potential in preclinical models for improving cognitive and behavioral symptoms.^[7]

• Aripiprazole