Novel Antidepressant Agomelatin Targets Melatonin and Serotonin Receptors: Presented at CPA

The soon-to-be-available antidepressant agomelatin offers excellent efficacy with great tolerability and sleep improvements to boot.

Raymond W. Lam, MD, Professor and Head of Clinical Neuroscience, Department of Psychiatry, Faculty of Medicine, University of British Columbia, Vancouver, Canada, presented the latest findings on this agent here at the 57th Annual Conference of the Canadian Psychiatric Association (CPA).

Agomelatin is a new antidepressant with a novel mechanism of action. It acts as an agonist to both the melatonin receptors MT1 and MT2. It is also an antagonist to the 5HT2C serotonin receptor. It also appears to have no other action in any other receptor site, and over 80 sites have been studied so far, said Dr. Lam.

Both the M1 and M2 receptors are known to be involved in regulation of circadian rhythms. Stimulation of M1 has a positive effect on sleep by attenuating the alerting signal produced by the suprachiasmatic nucleus (SCN) in the brain. M2 has a phase-shifting effect on circadian rhythms. Antagonism of the 5HT2C increases the activity of dopamine and noradrenalin in the frontal cortex, which can have both anxiolytic and antidepressant effects. It also promotes slow wave sleep or deep, restorative sleep.

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