AV-965 is a pharmacological compound being studied as a selectiveantagonist of the serotonin5-HT1A receptor, with potential applications inneuropsychiatric disorders such ascognitive impairment andschizophrenia.
AV-965 acts by blocking the 5-HT1A receptor, aG protein-coupled receptor prevalent in the brain, especially in theraphe nuclei (where it acts as an autoreceptor) and inlimbic andcortical regions (where it functions as a heteroreceptor).[1][2] Antagonism of 5-HT1Aautoreceptors can disinhibitserotonergic neuron firing, potentially enhancingserotonin release and improving cognitive and behavioral outcomes in conditions marked by reducedserotonergic 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-HT1A receptor is supported by research showing its influence on cognition, mood, and anxiety.[1][7]
Avera Pharmaceuticals is developing AV-965.[5] Selective 5-HT1A receptor modulation is a promising strategy in neuropsychiatric drug development, as bothagonists and antagonists have shown potential in preclinical models for improving cognitive and behavioral symptoms.[7]