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

期刊

BRITISH JOURNAL OF PHARMACOLOGY
卷 -, 期 -, 页码 -

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WILEY
DOI: 10.1111/bph.16233

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5-HT; 5-HT2C receptor; cell signalling; drug discovery; GPCR; SUDs

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Substance use disorder is a chronic condition with limited treatment options. The serotonin 2C receptor shows potential for the treatment of SUD, and research on psychedelics has also focused on this receptor. New studies provide a basis for further exploration.
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-HT2C receptor) make it a candidate of interest for the treatment of SUD. Recently, psychedelics, which broadly act at 5-HT2 receptors, have indicated potential for the treatment of SUD, implicating the 5-HT2C receptor. The modern psychedelic movement has rekindled interest in the 5-HT2C receptor, resulting in many new studies, especially structural analyses. This review explores the structural, molecular and cellular mechanisms governing 5-HT2C 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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