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Molecular biology of 5-HT receptors
Abstract
Serotonin (5-hydroxytryptamine; 5-HT) is a monoamine neurotransmitter whose effects are mediated by at least 13 distinct G protein-coupled receptors (GPCRs) of the type A family which includes the monoamine receptors and a combination of ligand-gated ion channels (5-HT3) of the Cys loop family which constitutes heteropentamers. 5-HT receptors are currently divided into seven classes (5-HT1 to 5-HT7), based on structural, transductional and operational features. While this degree of physical diversity clearly underscores the physiological importance of serotonin, evidence for an even greater degree of operational diversity is supported by the existence of a great number of splice and editing variants for several 5-HT receptors, their possible modulation by accessory proteins and chaperones, as well as their potential to form homo or heteromers both at the GPCR and at the ligand-gated channel level.
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“Serotonin 5HT2A receptors typically couple to the Gq/11-mediated signaling pathway, which activates phospholipase C (PLC) to stimulate the formation of inositol phosphates and diacylglycerol, leading to Ca2+ release from the endoplasmic reticulum [30].”
From Molecular and Functional Imaging Studies of Psychedelic Drug Action in Animals and Humans. (2021) · cites this paper as [30]
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Metadata
- Authors
- Hannon, J., & Hoyer, D.
- Affiliations
- Novartis (Switzerland) (CH)
- Venue
- Behavioural Brain Research
- Publisher
- Elsevier BV
- Published
- 2008-12
- Volume
- 195
- Issue
- 1
- Pages
- 198-213
- ISSN
- 0166-4328 (ISSN-L)
- OpenAlex
- W2010391271
- Cited by
- 815
- References
- 243
- Citations by year
- 2026: 20 · 2025: 41 · 2024: 39 · 2023: 47 · 2022: 39 · 2021: 54 · 2020: 46 · 2019: 52 · 2018: 52 · 2017: 44 · 2016: 53 · 2015: 45 · 2014: 53 · 2013: 59 · 2012: 54
- FWCI
- 15.83
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Behavioural Brain Research (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Receptor Mechanisms and Signaling
- Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neurotransmitter Receptor Influence on Behavior
- Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuroscience and Neuropharmacology Research
- Keywords
- serotonin receptors, G protein-coupled receptors, 5-HT3 receptor, ligand-gated ion channels, Cys-loop receptors, receptor splice variants, alternative splicing, receptor editing, accessory proteins, molecular chaperones, receptor heteromers
- MeSH terms
- Animals, Humans, Ligands, Protein Binding, Receptors, Serotonin, Serotonin, Receptors, G-Protein-Coupled, Intracellular Signaling Peptides and Proteins
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