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The correct title of this article is 5-HT3 receptor. It appears incorrectly here because of technical restrictions.
Identifiers
SymbolHTR3A
Alt. 5-hydroxytryptamine (serotonin receptor 3A, also known as HTR3A, is a human Gene. SymbolsHTR3
Entrez3359
HUGO5297
OMIM182139
RefSeqNM_000869
UniProtP46098
Other data
LocusChr. 11 q23.1-23.2
5-hydroxytryptamine (serotonin) receptor 3B
Identifiers
SymbolHTR3B
Entrez9177
HUGO5298
OMIM604654
RefSeqNM_006028
UniProtO95264
Other data
LocusChr. 11 q23.1
5-hydroxytryptamine (serotonin) receptor 3C
Identifiers
SymbolHTR3C
Entrez170572
HUGO24003
OMIM610121
RefSeqNM_130770
UniProtA2RRR5
Other data
LocusChr. 3 q27
5-hydroxytryptamine (serotonin) receptor 3D
Identifiers
SymbolHTR3D
Entrez200909
HUGO24004
OMIM610122
RefSeqNM_182537
UniProtQ70Z44
Other data
LocusChr. 3 q27
5-hydroxytryptamine (serotonin) receptor 3E
Identifiers
SymbolHTR3E
Entrez285242
HUGO24005
OMIM610123
RefSeqNM_182589
UniProtQ495G3
Other data
LocusChr. 3 q27

The 5-HT3 receptor is a member of the superfamily of ligand-gated ion channels, a family that also includes the neuronal nicotinic acetylcholine receptors (nAChRs), and the inhibitory neurotransmitter receptors for GABA (both GABAA and GABAC receptors) and glycine. The Entrez Global Query Cross-Database Search System is a powerful Federated search engine or Web portal that allows users to search many discrete Health sciences The Human Genome Organisation (HUGO is an organization involved in the Human Genome Project, a project about mapping the human genome The Mendelian Inheritance in Man project is a Database that catalogues all the known Diseases with a genetic component, and—when possible—links them The National Center for Biotechnology Information ( NCBI) is part of the United States National Library of Medicine (NLM a branch of the National Institutes Swiss-Prot is a manually curated Biological database of Protein sequences In the fields of Genetics and Evolutionary computation, a locus (plural loci) is a fixed position on a Chromosome such as the position of a Chromosome 11 is one of the 23 pairs of Chromosomes in Humans People normally have two copies of this chromosome The Entrez Global Query Cross-Database Search System is a powerful Federated search engine or Web portal that allows users to search many discrete Health sciences The Human Genome Organisation (HUGO is an organization involved in the Human Genome Project, a project about mapping the human genome The Mendelian Inheritance in Man project is a Database that catalogues all the known Diseases with a genetic component, and—when possible—links them The National Center for Biotechnology Information ( NCBI) is part of the United States National Library of Medicine (NLM a branch of the National Institutes Swiss-Prot is a manually curated Biological database of Protein sequences In the fields of Genetics and Evolutionary computation, a locus (plural loci) is a fixed position on a Chromosome such as the position of a Chromosome 11 is one of the 23 pairs of Chromosomes in Humans People normally have two copies of this chromosome The Entrez Global Query Cross-Database Search System is a powerful Federated search engine or Web portal that allows users to search many discrete Health sciences The Human Genome Organisation (HUGO is an organization involved in the Human Genome Project, a project about mapping the human genome The Mendelian Inheritance in Man project is a Database that catalogues all the known Diseases with a genetic component, and—when possible—links them The National Center for Biotechnology Information ( NCBI) is part of the United States National Library of Medicine (NLM a branch of the National Institutes Swiss-Prot is a manually curated Biological database of Protein sequences In the fields of Genetics and Evolutionary computation, a locus (plural loci) is a fixed position on a Chromosome such as the position of a 125px|right Chromosome 3 is one of the 23 pairs of Chromosomes in Humans People normally have two copies of this chromosome The Entrez Global Query Cross-Database Search System is a powerful Federated search engine or Web portal that allows users to search many discrete Health sciences The Human Genome Organisation (HUGO is an organization involved in the Human Genome Project, a project about mapping the human genome The Mendelian Inheritance in Man project is a Database that catalogues all the known Diseases with a genetic component, and—when possible—links them The National Center for Biotechnology Information ( NCBI) is part of the United States National Library of Medicine (NLM a branch of the National Institutes Swiss-Prot is a manually curated Biological database of Protein sequences In the fields of Genetics and Evolutionary computation, a locus (plural loci) is a fixed position on a Chromosome such as the position of a 125px|right Chromosome 3 is one of the 23 pairs of Chromosomes in Humans People normally have two copies of this chromosome The Entrez Global Query Cross-Database Search System is a powerful Federated search engine or Web portal that allows users to search many discrete Health sciences The Human Genome Organisation (HUGO is an organization involved in the Human Genome Project, a project about mapping the human genome The Mendelian Inheritance in Man project is a Database that catalogues all the known Diseases with a genetic component, and—when possible—links them The National Center for Biotechnology Information ( NCBI) is part of the United States National Library of Medicine (NLM a branch of the National Institutes Swiss-Prot is a manually curated Biological database of Protein sequences In the fields of Genetics and Evolutionary computation, a locus (plural loci) is a fixed position on a Chromosome such as the position of a 125px|right Chromosome 3 is one of the 23 pairs of Chromosomes in Humans People normally have two copies of this chromosome The Ligand-gated ion channels, also referred to as LGICs, or ionotropic receptors, are a group of intrinsic transmembrane ion channels that are Structure Nicotinic receptors with a molecular mass of 290 kDa, are made up of five subunits arranged symmetrically around the central pore. Gamma-aminobutyric acid (GABA is the chief inhibitory Neurotransmitter in the Mammalian Central nervous system. The GABAA receptor is one of two ligand-gated Ion channels responsible for mediating the effects of Gamma-aminobutyric acid (GABA the major The GABAC receptor is one of two Ligand-gated ion channels responsible for mediating the effects of Gamma-Amino Butyric Acid ( GABA) the major inhibitory [1][2] The 5-HT3 receptor is most closely related by homology to the nicotinic acetylcholine receptor.

The 5-HT3 receptor consists of 5 subunits arranged around a central ion conducting pore which is permeable to sodium, potassium, and calcium ions. Binding of the neurotransmitter 5-hydroxytryptamine (serotonin) to the 5-HT3 receptor opens the channel which in turn leads to an excitatory response in neurons. See Chemical synapse for an introduction to concepts and terminology used in this article Serotonin (ˌsɛrəˈtoʊnən ( 5-hydroxytryptamine, or 5-HT) is a Monoamine Neurotransmitter synthesized in serotonergic Neurons The 5-HT3 receptor differs markedly in structure and mechanism from the other 5-HT receptor subtypes which are all G-protein-coupled. In the field of Neurochemistry, 5-HT receptors are receptors for the Neurotransmitter and peripheral signal mediator Serotonin, also G protein-coupled receptors ( GPCRs) also known as seven transmembrane domain receptors, 7TM receptors, heptahelical receptors, and

Contents

Structure

As with other ligand gated ion channels, the 5-HT3 receptor is composed of five subunits pseudo symmetrically arranged about a central ion conducting pore. These subunits are proteins encoded by the HTR3A, HTR3B, HTR3C, HTR3D, and/or HTR3E genes.

Functional channels may be comprised of five identical 5-HT3A subunits (homopentameric) or a mixture of 5-HT3A and one of the other four 5-HT3B,[3][4][5] 5-HT3C, 5-HT3D, or 5-HT3E subunits (heteropentameric). 5-hydroxytryptamine (serotonin receptor 3A, also known as HTR3A, is a human Gene. [6] It appears that only the 5-HT3A subunits form functional homopentameric channels. All other subunit subtypes must heteropentamerize with 5-HT3A subunits to form functional channels.

Tissue distribution

The 5-HT3 receptor is expressed throughout the central and peripheral nervous systems and mediates a variety of physiological functions. In Vertebrates the central nervous system ( CNS) is the part of the Nervous system which is enclosed in the Meninges. The peripheral nervous system ( PNS) resides or extends outside the Central nervous system (CNS which consists of the Brain and Spinal cord. [2] On a cellular level, it has been shown that postsynaptic 5-HT3 receptors mediate fast excitatory synaptic transmission in rat neocortical interneurons and amygdala, and in ferret visual cortex. The la amygdalae ( Latin, also la corpus amygdaloideum, singular la amygdala, from Greek el αμυγδαλή grc-Latn amygdalē, 'almond' The term visual cortex refers to the primary visual cortex (also known as striate cortex or [7][8][9] 5-HT3 receptors are also present on presynaptic nerve terminals, where they are thought to mediate or modulate neurotransmitter release. [10][11][12]

Effects

When the receptor is activated to open the ion channel by agonists, the following effects are observed:

Agonists

Agonists (channel openers) for the receptor include:

Antagonists

Antagonists (channel closers) for the receptor (sorted by their respective therapeutic application) include:

Discovery

Identification of the 5-HT3 receptor did not take place until 1986 because of a lack of selective pharmacological tool. In Vertebrates the central nervous system ( CNS) is the part of the Nervous system which is enclosed in the Meninges. The peripheral nervous system ( PNS) resides or extends outside the Central nervous system (CNS which consists of the Brain and Spinal cord. Vomiting (also called throwing up, emesis) is the forceful expulsion of the contents of one's Stomach through the Mouth and sometimes the In Gastroenterology, irritable bowel syndrome ( IBS) is a Functional bowel disorder characterized by mild to severe Abdominal pain, discomfort Metoclopramide ( INN) (ˌmɛtəˈkloʊprəmaɪd or /ˌmɛtəˈklɒprəmaɪd is a potent Dopamine receptor antagonist used for its Antiemetic and Prokinetic Renzapride is a full Serotonin 5-HT4 receptor agonist partial Serotonin 5-HT3 and 5-HT2b receptor antagonist Alosetron (initial Brand name Lotronex originator GSK) is a 5-HT3 antagonist used for the management of severe diarrhoea-predominant An anti-emetic is a drug that is effective against Vomiting and Nausea. Ondansetron ( INN) (ɒnˈdænsɛtrɒn or Zofran is a Serotonin 5-HT3 receptor antagonist used mainly as an Antiemetic to Tropisetron ( INN) is a Serotonin 5-HT3 receptor antagonist used mainly as an Antiemetic to treat Nausea and Vomiting Granisetron is a Serotonin 5-HT3 receptor antagonist used as an Antiemetic to treat Nausea and Vomiting following Mirtazapine is an Antidepressant introduced by Organon International in 1994 used for the treatment of moderate to severe depression. An antidepressant is a Psychiatric medication used for alleviating major depression or Dysthymia ('milder' depression Memantine is the first in a novel class of Alzheimer's disease medications acting on the Glutamatergic system by blocking NMDA glutamate receptors Alzheimer's disease ( AD) also called Alzheimer disease or simply Alzheimer's, is the most common form of Dementia. [2] However, with the discovery that the 5-HT3 receptor plays a prominent role in chemotherapy- and radiotherapy-induced vomiting, and the concomitant development of selective 5-HT3 receptor antagonists to suppress these side effects aroused intense interest from the pharmaceutical industry[14][15] and therefore the identification of 5-HT3 receptors in cell lines and native tissues quickly followed. Chemotherapy, in its most general sense refers to treatment of disease by chemicals that kill cells specifically those of micro-organisms or Cancer. Radiation therapy (or radiotherapy) is the medical use of Ionizing radiation as part of Cancer treatment to control Malignant Vomiting (also called throwing up, emesis) is the forceful expulsion of the contents of one's Stomach through the Mouth and sometimes the The 5-HT3 antagonists are a class of Medications which act as Receptor antagonists at the 5-hydroxytryptamine-3 receptor (5-HT3 receptor [2]

References

  1. ^ Maricq AV, Peterson AS, Brake AJ, Myers RM, Julius D (1991). "Primary structure and functional expression of the 5HT3 receptor, a serotonin-gated ion channel". Science 254 (5030): 432–7. doi:10.1126/science.1718042. A digital object identifier ( DOI) is a permanent identifier given to an Electronic document. PMID 1718042.  
  2. ^ a b c d Yakel, JL (2000), Endo, M; Kurachi, Y & Mishina, M, eds. , The 5-HT3 receptor channel: function, activation and regulation in Pharmacology of Ionic Channel Function: Activators and Inhibitors (Handbook of Experimental Pharmacology), vol. 147, Berlin: Springer-Verlag, pp. Springer Science+Business Media or Springer (ˈʃpʁɪŋɐ is a worldwide Publishing company based in Germany, which publishes textbooks academic 541–560, ISBN 3540661271 
  3. ^ Davies PA, Pistis M, Hanna MC, Peters JA, Lambert JJ, Hales TG, Kirkness EF (1999). "The 5-HT3B subunit is a major determinant of serotonin-receptor function". Nature 397 (6717): 359–63. doi:10.1038/16941. A digital object identifier ( DOI) is a permanent identifier given to an Electronic document. PMID 9950429.  
  4. ^ Dubin AE, Huvar R, D'Andrea MR, Pyati J, Zhu JY, Joy KC, Wilson SJ, Galindo JE, Glass CA, Luo L, Jackson MR, Lovenberg TW, Erlander MG (1999). "The pharmacological and functional characteristics of the serotonin 5-HT3A receptor are specifically modified by a 5-HT3B receptor subunit". J Biol Chem 274 (43): 30799–810. PMID 10521471.  
  5. ^ Monk SA, Desai K, Brady CA, Williams JM, Lin L, Princivalle A, Hope AG, Barnes NM (2001). "Generation of a selective 5-HT3B subunit-recognising polyclonal antibody; identification of immunoreactive cells in rat hippocampus". Neuropharmacology 41 (8): 1013–6. doi:10.1016/S0028-3908(01)00153-8. A digital object identifier ( DOI) is a permanent identifier given to an Electronic document. PMID 11747906.  
  6. ^ Niesler B, Walstab J, Combrink S, Moeller D, Kapeller J, Rietdorf J, Boenisch H, Goethert M, Rappold G, Bruess M (2007). "Characterization of the Novel Human Serotonin Receptor Subunits 5-HT3C, 5- HT3D and 5-HT3E". Mol Pharmacol 71 (Mar 28): Epub ahead of print. doi:10.1124/mol.106.032144. A digital object identifier ( DOI) is a permanent identifier given to an Electronic document. PMID 17392525.  
  7. ^ Férézou I, Cauli B, Hill EL, Rossier J, Hamel E, Lambolez B (2002). "5-HT3 receptors mediate serotonergic fast synaptic excitation of neocortical vasoactive intestinal peptide/cholecystokinin interneurons". J Neurosci 22 (17): 7389–97. PMID 12196560.  
  8. ^ Sugita S, Shen KZ, North RA (1992). "5-hydroxytryptamine is a fast excitatory transmitter at 5-HT3 receptors in rat amygdala". Neuron 8 (1): 199–203. doi:10.1016/0896-6273(92)90121-S. A digital object identifier ( DOI) is a permanent identifier given to an Electronic document. PMID 1346089.  
  9. ^ Roerig B, Nelson DA, Katz LC (1992). "Fast synaptic signaling by nicotinic acetylcholine and serotonin 5-HT3 receptors in developing visual cortex". J Neurosci 17 (21): 199–203. PMID 9334409.  
  10. ^ Rondé P, Nichols RA (1998). "High calcium permeability of serotonin 5-HT3 receptors on presynaptic nerve terminals from rat striatum". J Neurochem 70 (3): 1094–103. doi:10.1046/j.1471-4159.1998.70031094.x. A digital object identifier ( DOI) is a permanent identifier given to an Electronic document. PMID 9489730.  
  11. ^ Rondé P, Nichols RA (1997). "5-HT3 receptors induce rises in cytosolic and nuclear calcium in NG108-15 cells via calcium-induced calcium release". Cell Calcium 22 (5): 357–65. PMID 9448942.  
  12. ^ van Hooft JA, Vijverberg HP (2000). "5-HT3 receptors and neurotransmitter release in the CNS: a nerve ending story?". Trends Neurosci 23 (12): 605–10. doi:10.1016/S0166-2236(00)01662-3. A digital object identifier ( DOI) is a permanent identifier given to an Electronic document. PMID 11137150.  
  13. ^ a b c d e Rang, H. P. (2003). Pharmacology. Edinburgh: Churchill Livingstone. ISBN 0-443-07145-4.   Page 187
  14. ^ Thompson AJ, Lummis SC (2006). "5-HT3 receptors". Curr Pharm Des 12 (28): 3615–30. PMID 17073663.  
  15. ^ Thompson AJ, Lummis SC (2007). "The 5-HT3 receptor as a therapeutic target". Expert Opin Ther Targets 11 (4): 527–40. doi:10.1517/14728222.11.4.527. A digital object identifier ( DOI) is a permanent identifier given to an Electronic document. PMID 17373882.  

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