Overcoming Depression with 5-HT2A Receptor Ligands
Agata Zięba, Piotr Stępnicki, Dariusz Matosiuk, Agnieszka A. Kaczor
International Journal of Molecular Sciences December 21, 2021 DOI: 10.3390/ijms23010010 (opens in new tab)
Study at a glance
AI-extracted from the abstract| Characteristics | Review Peer reviewed |
|---|---|
| Topics | Depression Serotonin |
| Keywords | Virtual screening Receptor Depression economics Antidepressant Pharmacology Bioinformatics Drug discovery |
| Citations | 55 |
| Key findings | Modulators of 5-HT2A receptor signaling show promise for developing novel antidepressants, supported by recent virtual screening and ligand synthesis. |
Abstract
Depression is a multifactorial disorder that affects millions of people worldwide, and none of the currently available therapeutics can completely cure it. Thus, there is a need for developing novel, potent, and safer agents. Recent medicinal chemistry findings on the structure and function of the serotonin 2A (5-HT2A) receptor facilitated design and discovery of novel compounds with antidepressant action. Eligible papers highlighting the importance of 5-HT2A receptors in the pathomechanism of the disorder were identified in the content-screening performed on the popular databases (PubMed, Google Scholar). Articles were critically assessed based on their titles and abstracts. The most accurate papers were chosen to be read and presented in the manuscript. The review summarizes current knowledge on the applicability of 5-HT2A receptor signaling modulators in the treatment of depression. It provides an insight into the structural and physiological features of this receptor. Moreover, it presents an overview of recently conducted virtual screening campaigns aiming to identify novel, potent 5-HT2A receptor ligands and additional data on currently synthesized ligands acting through this protein.
Comparable studies
Other narrative reviews on serotonin, most cited first.
Citations in the library
Cited by 10
- Serotonin 2A Receptor (5-HT2AR) Agonists: Psychedelics and Non-Hallucinogenic Analogues as Emerging Antidepressants Chemical Reviews November 30, 2023
- Antidepressant and anxiolytic effects of activating 5HT2A receptors in the anterior cingulate cortex and the theoretical mechanisms underlying them - A scoping review of available literature. Brain Research 2025
- Alkaloids from the entheogenic plant Peganum harmala Australian Journal of Chemistry July 17, 2023
- The Selective 5HT2A Receptor Agonist, 25CN-NBOH Exerts Excitatory and Inhibitory Cellular Actions on Mouse Medial Prefrontal Cortical Neurons. Synapse March 1, 2025
- Synthetic studies toward the marine alkaloid convolutindole A, a structurally remarkable derivative of the hallucinogen N,N-Dimethyltryptamine (DMT) Tetrahedron Letters September 13, 2023
and 5 more in the library
Cites 13
- Psychedelics Promote Structural and Functional Neural Plasticity Cell Reports June 1, 2018
- A non-hallucinogenic psychedelic analogue with therapeutic potential. Nature 2021
- Harnessing psilocybin: antidepressant-like behavioral and synaptic actions of psilocybin are independent of 5-HT2R activation in mice Proceedings of the National Academy of Sciences April 13, 2021
- A Single Dose of Psilocybin Increases Synaptic Density and Decreases 5-HT2A Receptor Density in the Pig Brain International Journal of Molecular Sciences January 15, 2021
- Efficacy of psychedelic treatments on depressive symptoms: A meta-analysis Journal of Psychopharmacology May 25, 2020
and 8 more in the library