Related Papers
Neuropharmacology
A review of central 5HT receptors and their function
1999 •
Trevor Sharp
Naunyn-schmiedebergs Archives of Pharmacology
Cardiovascular responses produced by 5-hydroxytriptamine:a pharmacological update on the receptors/mechanisms involved and therapeutic implications
2007 •
David Centurión
Pharmaceuticals
Modulation of the Serotonergic Receptosome in the Treatment of Anxiety and Depression: A Narrative Review of the Experimental Evidence
2021 •
Roberto Kenji Nakamura Cuman
Serotonin (5-HT) receptors are found throughout central and peripheral nervous systems, mainly in brain regions involved in the neurobiology of anxiety and depression. 5-HT receptors are currently promising targets for discovering new drugs for treating disorders ranging from migraine to neuropsychiatric upsets, such as anxiety and depression. It is well described in the current literature that the brain expresses seven types of 5-HT receptors comprising eighteen distinct subtypes. In this article, we comprehensively reviewed 5-HT1-7 receptors. Of the eighteen 5-HT receptors known today, thirteen are G protein-coupled receptors (GPCRs) and represent targets for approximately 40% of drugs used in humans. Signaling pathways related to these receptors play a crucial role in neurodevelopment and can be modulated to develop effective therapies to treat anxiety and depression. This review presents the experimental evidence of the modulation of the “serotonergic receptosome” in the treatme...
Serotonin receptors and systems: endless diversity?
2002 •
Jason Hannon
Serotonin is probably unique among the monoamines in that its effects are subserved by as many as 13 distinct heptahelical, G protein-coupled receptors (GPCRs) and a ligand-gated ion channel family (5-HT3). These receptors are divided into seven distinct classes (5-HT1 to 5-HT7) largely on the basis of their structural, transductional and operational char- acteristics. While this degree of physical diversity clearly underscores the physiological importance of serotonin, evidence for an even greater degree of operational diversity continues to emerge. Here, we will review this diversity and its physiological and possibly pathophysiological consequences. Indeed, 5-HT research which is about 50 years old, has resulted in numerous therapeutic agents, some of which have a major impact on disease man- agement. Thus, selective 5-HT reuptake inhibitors (SSRIs) are among the most widely used drugs in depression and other disorders such as anxiety, social phobia, panic disorders, or obsessive...
Molecular Brain Research
Cultured astrocytes express messenger RNA for multiple serotonin receptor subtypes, without functional coupling of 5HT 1 receptor subtypes to adenylyl cyclase
1998 •
Warren Hirst
Multiplicity of mechanisms of serotonin receptor signal transduction
Yurii V Mukhin
The serotonin (5-hydroxytryptamine, 5-HT) receptors have been divided into 7 subfamilies by convention, 6 of which include 13 different genes for G-protein-coupled receptors. Those subfamilies have been characterized by overlapping pharmacological properties, amino acid sequences, gene organization, and second messenger coupling pathways. Post-genomic modifications, such as alternative mRNA splicing or mRNA editing, creates at least 20 more G-protein-coupled 5-HT receptors, such that there are at least 30 distinct 5-HT receptors that signal through G-proteins. This review will focus on what is known about the signaling linkages of the G-protein-linked 5-HT receptors, and will highlight some fascinating new insights into 5-HT receptor signaling. D
Neuroscience & Biobehavioral Reviews
5-HT system and cognition
1999 •
Alfredo Meneses
IUPHAR/BPS Guide to Pharmacology CITE
5-Hydroxytryptamine receptors (version 2019.4) in the IUPHAR/BPS Guide to Pharmacology Database
Theresa Branchek
5-HT receptors (nomenclature as agreed by the NC-IUPHAR Subcommittee on 5-HT receptors [194] and subsequently revised [176]) are, with the exception of the ionotropic 5-HT3 class, GPCRs where the endogenous agonist is 5-hydroxytryptamine. The diversity of metabotropic 5-HT receptors is increased by alternative splicing that produces isoforms of the 5-HT2A (non-functional), 5-HT2C (non-functional), 5-HT4, 5-HT6 (non-functional) and 5-HT7 receptors. Unique amongst the GPCRs, RNA editing produces 5-HT2C receptor isoforms that differ in function, such as efficiency and specificity of coupling to Gq/11 and also pharmacology [40, 482]. Most 5-HT receptors (except 5-ht1e and 5-ht5b) play specific roles mediating functional responses in different tissues (reviewed by [463, 382]).
Techniques in Coloproctology
Serotonin receptors and their role in the pathophysiology and therapy of irritable bowel syndrome
2014 •
Massimo Bellini
Pharmacodynamics of Serotonin. Emphasis on 5HT-3 Antagonists and SSRI Medication (II)
2016 •
Ion Fulga
This paper presents a literature review of the pharmacology of serotonin. It focuses on the metabolism and transport of serotonin and on 5-HT receptors and their clinical signifi cance. This report highlights the substances that affect serotonin signalling and body levels and may be employed in treating various disorders: either directly, by influencing the serotonin receptors or, indirectly, by inhibiting serotonin reuptake. The review will be published in two separate parts. The fi rst part will contain a short introduction in the pharmacology of serotonin and it will emphasize the pharmacological properties of the fi rst three of the 5-HT receptors (5-HT1, 5-HT2, 5-HT3). In the second part, the other four types of 5-HT receptors (5-HT4, 5-HT5, 5-HT6, 5-HT7) will be presented along with tendencies and prospects in influencing serotonin transporter (SERT) through selective serotonin reuptake inhibitors (SSRIs). Recent research involving serotonin aims to improve the safety and effe...
