Molecular and structural insights into the 5‐HT2C receptor as a therapeutic target for substance use disorders

Summary

The review discusses the role of the serotonin 2C receptor (5-HT2C) in substance use disorder (SUD), noting that current therapies have high relapse rates. It highlights the potential of psychedelics, which act on 5-HT receptors, to treat SUD and emphasizes renewed interest in 5-HT2C due to recent studies. The review covers structural, molecular, and cellular mechanisms of 5-HT2C receptor function related to SUD, suggesting avenues for future research.

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Abstract

Abstract Substance use disorder (SUD) is a chronic condition, with maintained abuse of a substance leading to physiological and psychological alterations and often changes in cognitive and social behaviours. Current therapies include psychotherapy coupled with medication; however, high relapse rates reveal the shortcomings of these therapies. The signalling, expression profile, and neurological function of the serotonin 2C receptor (5‐HT 2C receptor) make it a candidate of interest for the treatment of SUD. Recently, psychedelics, which broadly act at 5‐HT 2 receptors, have indicated potential for the treatment of SUD, implicating the 5‐HT 2C receptor. The modern psychedelic movement has rekindled interest in the 5‐HT 2C receptor, resulting in many new studies, especially structural analyses. This review explores the structural, molecular and cellular mechanisms governing 5‐HT 2C receptor function in the context of SUD. This provides the basis of the preclinical and clinical evidence for their role in SUD and highlights the potential for future exploration.

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