Small-Molecule Heterocyclic Compounds: Gq-Biased Agonists for the 5-HT2A Receptor in Neuropsychiatric Treatment
ACS Medicinal Chemistry Letters October 19, 2023 DOI: 10.1021/acsmedchemlett.3c00444 (opens in new tab)
Study at a glance
AI-extracted from the abstract| Characteristics | Commentary Peer reviewed |
|---|---|
| Topics | Serotonin |
| Citations | 2 |
| Key points | Describes small-molecule heterocyclic compounds that act as Gq-biased agonists of the 5-HT2A receptor, selectively activating 5-HT2A-mediated Gq signaling while excluding 5-HT2B and 5-HT2C. The authors propose that this selectivity could enable more targeted and efficient treatment of depression, anxiety, and substance abuse, and suggest further research is needed to establish clinical potential. |
Abstract
Addressing the significant challenges of treating depression, anxiety, and substance abuse, this Patent Highlight explores the development of innovative small-molecule heterocyclic compounds as Gq-biased agonists of the 5-HT2A receptor. Unlike traditional treatments, these compounds selectively activate 5-HT2A-mediated Gq signaling, excluding related receptors like 5-HT2B and 5-HT2C. This selectivity suggests a more targeted and efficient therapeutic approach. The discovery of these compounds could herald a new era in neuropsychiatric treatment, promising safer, faster, and more effective interventions. Further research will illuminate their potential and applicability in clinical settings.
Citations in the library
Cites 6
- The risk of chronic psychedelic and MDMA microdosing for valvular heart disease Journal of Psychopharmacology August 12, 2023
- Psilocybin history, action and reaction: A narrative clinical review Journal of Psychopharmacology August 31, 2023
- Assessing the risk of symptom worsening in psilocybin-assisted therapy for depression: A systematic review and individual participant data meta-analysis Psychiatry Research July 23, 2023
- Scoping Review of Experiential Measures from Psychedelic Research and Clinical Trials. Journal of Psychoactive Drugs 2023
- Beyond Psilocybin: Reviewing the Therapeutic Potential of Other Serotonergic Psychedelics in Mental and Substance Use Disorders Journal of Psychoactive Drugs August 24, 2023
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