Insights into the regulation of 5-HT2A serotonin receptors by scaffolding proteins and kinases.
John A Allen, Prem N. Yadav, Bryan L. Roth
Neuropharmacology July 2, 2008 DOI: 10.1016/j.neuropharm.2008.06.048 (opens in new tab)
Study at a glance
AI-extracted from the abstract| Characteristics | Review Peer reviewed |
|---|---|
| Topics | Serotonin |
| Keywords | Animals Humans Arrestin Receptor, serotonin, 5-ht2a Caveolins Endocytosis Protein transport Models, biological |
| Key findings | The authors propose that multiple scaffolding proteins, including PSD95, arrestin, and caveolin, regulate 5-HT2A serotonin receptor trafficking, targeting, and signaling, and they report that a novel interaction between p90 ribosomal S6 kinase and the receptor attenuates receptor signaling. |
Abstract
5-HT(2A) serotonin receptors are essential molecular targets for the actions of LSD-like hallucinogens and atypical antipsychotic drugs. 5-HT(2A) serotonin receptors also mediate a variety of physiological processes in peripheral and central nervous systems including platelet aggregation, smooth muscle contraction, and the modulation of mood and perception. Scaffolding proteins have emerged as important regulators of 5-HT(2A) receptors and our recent studies suggest multiple scaffolds exist for 5-HT(2A) receptors including PSD95, arrestin, and caveolin. In addition, a novel interaction has emerged between p90 ribosomal S6 kinase and 5-HT(2A) receptors which attenuates receptor signaling. This article reviews our recent studies and emphasizes the role of scaffolding proteins and kinases in the regulation of 5-HT(2A) trafficking, targeting and signaling.
Comparable studies
Other narrative reviews on serotonin, most cited first.
Citations in the library
Cited by 7
- Rapid modulation of spine morphology by the 5-HT 2A serotonin receptor through kalirin-7 signaling Proceedings of the National Academy of Sciences November 4, 2009
- Psychedelics as Transformative Therapeutics. American Journal of Psychiatry May 1, 2023
- Receptor Interaction Profiles of 4-Alkoxy-3,5-Dimethoxy-Phenethylamines (Mescaline Derivatives) and Related Amphetamines Frontiers in Pharmacology February 9, 2022
- A Multidisciplinary Hypothesis about Serotonergic Psychedelics. Is it Possible that a Portion of Brain Serotonin Comes From the Gut? Journal of Integrative Neuroscience August 31, 2022
- Serotonin 5-HT2A receptor expression is chronically decreased in the anterior cerebral cortex of male rats following repetitive low-level blast exposure Frontiers in Neurology June 25, 2025
and 2 more in the library
Cites 6
- Salvinorin A: a potent naturally occurring nonnitrogenous kappa opioid selective agonist. Proceedings of the National Academy of Sciences September 3, 2002
- 5-HT2AReceptor-Mediated Regulation of Brain-Derived Neurotrophic Factor mRNA in the Hippocampus and the Neocortex Journal of Neuroscience April 15, 1997
- Salvinorin A: the "magic mint" hallucinogen finds a molecular target in the kappa opioid receptor. TIPS - Trends in Pharmacological Sciences March 1, 2003
- Hallucinogens. Pharmacology & Therapeutics February 1, 2004
- Agonist induced-phosphorylation of Galpha11 protein reduces coupling to 5-HT2A receptors. Journal of Pharmacology and Experimental Therapeutics October 2007
and 1 more in the library