The 5-HT2A serotonin receptor represents the principal molecular target for the actions of both classic hallucinogens, which function as agonists, and atypical antipsychotic drugs, which function as inverse agonists. Pharmacological agents that modify the activity of 5-HT2A receptors are known to modulate human perception and cognition. 5-HT2A receptors are found predominantly in the apical dendritic segment and dendritic spines of cortical pyramidal neurons. This review discusses our current understanding of the molecular and cellular mechanisms governing the preferential targeting of 5-HT2A receptors to apical dendrites and dendritic spines. Uncovering the processes responsible for the polarization of 5-HT2A receptors to neuronal subdomains will likely provide crucial insights into the modulating mechanisms that can affect human cognition and perception.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1615/critrevneurobiol.v16.i4.10 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
N, N-dimethyltryptamine (DMT) in rodent brain: Concentrations, distribution, and recent pharmacological data.
Prog Neuropsychopharmacol Biol Psychiatry
January 2025
Louisiana State University, Department of Comparative Biomedical Sciences, Baton Rouge, LA 70803, United States of America. Electronic address:
Renewed interest in the clinical use of psychedelic drugs acknowledges their therapeutic effectiveness. It has also provided a changing frame of reference for older psychedelic drug study data, especially regarding concentrations of N, N-dimethyltryptamine (DMT) reported in rodent brains and recent discoveries in DMT receptor interactions in rat brain neurons and select brain areas. The mode of action of DMT in its newly defined role as a neuroplastogen, its effectiveness in treating neuropsychiatric disorders, and its binding to intracellular sigma-1 and 5HT2a receptors may define these possible roles.
View Article and Find Full Text PDFExploring DMT: Endogenous Role and Therapeutic Potential.
Neuropharmacology
January 2025
Behavioral Neuroscience Lab, Institute of Psychology, SWPS University.
N,N-Dimethyltryptamine (DMT) is a naturally occurring amine and psychedelic compound, found in plants, animals, and humans. While initial studies reported only trace amounts of DMT in mammalian brains, recent findings have identified alternative methylation pathways and DMT levels comparable to classical neurotransmitters in rodent brains, calling for a re-evaluation of its biological role and exploration of this inconsistency. This study evaluated DMT's biosynthetic pathways, focusing on indolethylamine N-methyltransferase (INMT) and its isoforms, and possible regulatory mechanisms, including alternative routes of synthesis and how physiological conditions, such as stress and hypoxia influence DMT levels.
View Article and Find Full Text PDFThe Relationship Between Impulsivity Traits and In Vivo Cerebral Serotonin Transporter and Serotonin 2A Receptor Binding in Healthy Individuals: A Double-Tracer PET Study with C-11 DASB and C-11 MDL100907.
Int J Mol Sci
December 2024
Neuroscience Research Institute, Gachon University, Incheon 21565, Republic of Korea.
To elucidate the potential roles of presynaptic and postsynaptic serotonergic activity in impulsivity traits, we investigated the relationship between self-reported impulsiveness and serotonin transporter (5-HTT) and 5-HT2A receptors in healthy individuals. In this study, 26 participants completed 3-Tesla magnetic resonance imaging and positron emission tomography with [C]DASB and [C]MDL100907. To quantify 5-HTT and 5-HT2A receptor availability, the binding potential (BP) of [C]DASB and [C]MDL100907 was derived using the simplified reference tissue model with cerebellar gray matter as the reference region.
View Article and Find Full Text PDFSynthesis and Biological Evaluation of Peripheral HTR2A Antagonists for Colorectal Cancer.
J Med Chem
January 2025
Department of Chemistry, Gwangju Institute of Science and Technology, Gwangju 61005, Republic of Korea.
Colorectal cancer is a prevalent and prominent contributor to global cancer-related fatalities with challenges in drug resistance and metastasis. Recent research highlights the potential relationship between serotonin and cancer. 5-Hydroxytryptamine receptor 2A (HTR2A) mRNA expression in colorectal cancer cells was found to be notably elevated compared to that in normal colon cells.
View Article and Find Full Text PDFA Clinically Oriented Review of New Antipsychotics for Schizophrenia.
Neuropsychiatr Dis Treat
December 2024
Department of Medicine and Surgery, Kore University of Enna, Enna (EN), Italy.
Article Synopsis
- Current antipsychotics mainly target dopamine but often fail to address the complexity of schizophrenia and can cause significant side effects, highlighting a need for new treatments.
- Recent research is focusing on non-dopaminergic antipsychotics, such as muscarinic agonists and 5-HT2A antagonists, to offer better therapeutic options for schizophrenia.
- While new drugs like xanomeline-trospium have been approved, others like bitopertin and pimavanserin were halted in development, emphasizing the need for cautious evaluation of their efficacy and safety.
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!