Serotonin is a neuromodulator that mediates a wide range of effects by interacting with multiple receptors. Using a strategy based on nucleotide sequence homology between genes encoding receptors that interact with guanine nucleotide-binding proteins, we have isolated a mouse gene encoding an additional serotonin receptor. When expressed in cultured cells, it displayed the pharmacological profile and coupling with adenylate cyclase characteristic of the 5HT1B receptor subtype. In NIH 3T3 cells expressing this receptor, serotonin induced a decrease in forskolin-stimulated cAMP levels. This effect was blocked by pertussis toxin, indicating that the 5HT1B receptor interacts with a pertussis toxin-sensitive guanine nucleotide-binding protein. To obtain clues as to the possible function of the 5HT1B receptor, we have analyzed its pattern of expression in the adult mouse brain by in situ hybridization. Our results, together with previous autoradiographic studies, suggest that the 5HT1B receptors are localized presynaptically on the terminals of striatal neurons and Purkinje cells and that they might modulate the release of neurotransmitters such as gamma-aminobutyric acid. The predominant expression of the 5HT1B receptor in the striatum and cerebellum points to an involvement of this receptor in motor control.
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http://dx.doi.org/10.1073/pnas.89.7.3020 | DOI Listing |
Biophys Chem
December 2024
Department of Chemistry and Center for Atomic, Molecular, Optical Sciences and Technologies (CAMOST), Indian Institute of Science, Education and Research (IISER) Tirupati, Yerpedu Mandal, Tirupati 517619, India. Electronic address:
Serotonin-receptor binding plays a key role in several neurological and biological processes, including mood, sleep, hunger, cognition, learning, and memory. In this article, we performed molecular dynamics simulation to examine the key residues that play an essential role in the binding of serotonin to the G-protein-coupled 5-HT receptor (5HTR) via electrostatic interactions. Key residues for electrostatic interactions were identified via bond distance analysis and frustration analysis methods.
View Article and Find Full Text PDFExpert Opin Drug Saf
December 2024
Shanghai Mental Health Center, Shanghai Jiao Tong University School of Medicine, Shanghai, China.
Background: Sexual dysfunction (SD) is a commonly occurring yet often underestimated adverse event associated with the use of antidepressants. This study aimed to analyze the reporting of SD associated with the use of antidepressants in comparison with one another, and to explore potential receptor mechanisms based on the real-world data from the Food and Drug Administration Adverse Event Reporting System (FAERS).
Methods: Disproportionality analysis was conducted based on FAERS reports (2004 Q1 to 2024 Q2) using reporting odds ratios (ROR) and information components (IC) methods.
Int J Mol Sci
December 2024
Department of Embryology, Faculty of Biology, Lomonosov Moscow State University, Moscow 119234, Russia.
Serotonin (5-HT), a versatile signaling molecule, plays a variety of roles in both neurotransmission and tissue regulation. The influence of serotonin on early development was first studied in marine invertebrate embryos and has since been documented in a variety of vertebrate species, including mammals. The present study investigates the expression and functional activity of serotonin components in mouse embryos, focusing on key receptors and transporters.
View Article and Find Full Text PDFPharmacol Biochem Behav
February 2025
Sumitomo Pharma America, Inc., 84 Waterford Drive, Marlborough, MA 01752, USA.
Ketamine is noted for its rapid onset antidepressant response and effectiveness in patients with treatment resistant depression. While most research has focused on glutamatergic mechanisms, recent studies show that antidepressant-like effects in rodents are dependent upon the serotonergic (5-HT) system and suggest a potential contribution of the 5-HT receptor. In this study we utilized CP-94253 to examine whether 5-HT receptor agonism produces rapid and sustained antidepressant-like effects, focusing on rodent models and treatment approaches commonly used to demonstrate the differentiated response to ketamine.
View Article and Find Full Text PDFJ Headache Pain
October 2024
Department of Pharmacy, Translational Pharmacokinetics/Pharmacodynamics group (tPKPD), Uppsala University, Uppsala, Sweden.
Background: Triptans are potent 5-HT receptor agonists used in migraine therapy, thought to act through peripheral mechanisms. It remains unclear whether triptans cross the blood-brain barrier (BBB) sufficiently to stimulate central 5-HT receptors. This study investigates the disposition of eletriptan and sumatriptan in central nervous system (CNS) and peripheral nervous system (PNS) regions and predicts regional 5-HT receptor occupancies at clinically relevant concentrations.
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