HTR3A

Summary

Gene Symbol: HTR3A
Description: 5-hydroxytryptamine receptor 3A
Alias: 5-HT-3, 5-HT3A, 5-HT3R, 5HT3R, HTR3, 5-hydroxytryptamine receptor 3A, 5-HT3-A, 5-hydroxytryptamine (serotonin) receptor 3A, ionotropic, 5-hydroxytryptamine receptor 3, 5HT3 serotonin receptor, serotonin receptor 3A, serotonin-gated ion channel receptor
Species: human
Products:     HTR3A

Top Publications

  1. Hales T, Dunlop J, Deeb T, Carland J, Kelley S, Lambert J, et al. Common determinants of single channel conductance within the large cytoplasmic loop of 5-hydroxytryptamine type 3 and alpha4beta2 nicotinic acetylcholine receptors. J Biol Chem. 2006;281:8062-71 pubmed
    ..This locus may be a common determinant of ion conduction throughout the Cys loop receptor family...
  2. Belelli D, Balcarek J, Hope A, Peters J, Lambert J, Blackburn T. Cloning and functional expression of a human 5-hydroxytryptamine type 3AS receptor subunit. Mol Pharmacol. 1995;48:1054-62 pubmed
  3. Iidaka T, Ozaki N, Matsumoto A, Nogawa J, Kinoshita Y, Suzuki T, et al. A variant C178T in the regulatory region of the serotonin receptor gene HTR3A modulates neural activation in the human amygdala. J Neurosci. 2005;25:6460-6 pubmed
    ..for the single nucleotide polymorphism C178T in the regulatory region of the serotonin receptor type 3 gene (HTR3A)...
  4. Cheng A, McDonald N, Connolly C. Cell surface expression of 5-hydroxytryptamine type 3 receptors is promoted by RIC-3. J Biol Chem. 2005;280:22502-7 pubmed
  5. Ducci F, ENOCH M, Yuan Q, Shen P, White K, Hodgkinson C, et al. HTR3B is associated with alcoholism with antisocial behavior and alpha EEG power--an intermediate phenotype for alcoholism and co-morbid behaviors. Alcohol. 2009;43:73-84 pubmed publisher
    ..We tested whether genetic variation within the HTR3A and HTR3B genes influences vulnerability to AUD with comorbid ASPD (AUD+ASPD) and moderates alpha power...
  6. Paulsen I, Martin I, Dunn S. Isomerization of the proline in the M2-M3 linker is not required for activation of the human 5-HT3A receptor. J Neurochem. 2009;110:870-8 pubmed publisher
    ..These results demonstrate an important role for P303 in 5-HT(3)A receptor function but indicate that trans-cis isomerization at this proline is unlikely to be a general mechanism underlying the gating process. ..
  7. Kilpatrick L, Labus J, Coveleskie K, Hammer C, Rappold G, Tillisch K, et al. The HTR3A polymorphism c. -42C>T is associated with amygdala responsiveness in patients with irritable bowel syndrome. Gastroenterology. 2011;140:1943-51 pubmed publisher
    ..A single nucleotide polymorphism in HTR3A, c...
  8. Niesler B, Walstab J, Combrink S, Möller D, Kapeller J, Rietdorf J, et al. Characterization of the novel human serotonin receptor subunits 5-HT3C,5-HT3D, and 5-HT3E. Mol Pharmacol. 2007;72:8-17 pubmed
    ..These data show for the first time that the novel 5-HT(3) subunits are able to form heteromeric 5-HT(3) receptors, which exhibit quantitatively different functional properties compared with homomeric 5-HT(3A) receptors. ..
  9. Zhang R, Wen X, Militante J, Hester B, Rhubottom H, Sun H, et al. The role of loop F residues in determining differential d-tubocurarine potencies in mouse and human 5-hydroxytryptamine 3A receptors. Biochemistry. 2007;46:1194-204 pubmed
    ..8 +/- 6.38 nM) as that of the human receptor containing all six loop F mouse substitutions. These results demonstrate that two loop F residues make a significant contribution in determining curare potency at the 5-HT3A receptor...

More Information

Publications94

  1. Deeb T, Carland J, Cooper M, Livesey M, Lambert J, Peters J, et al. Dynamic modification of a mutant cytoplasmic cysteine residue modulates the conductance of the human 5-HT3A receptor. J Biol Chem. 2007;282:6172-82 pubmed
  2. Yamada K, Hattori E, Iwayama Y, Ohnishi T, Ohba H, Toyota T, et al. Distinguishable haplotype blocks in the HTR3A and HTR3B region in the Japanese reveal evidence of association of HTR3B with female major depression. Biol Psychiatry. 2006;60:192-201 pubmed
    Genetic variations in the serotonin receptor 3A (HTR3A) and 3B (HTR3B) genes, positioned in tandem on chromosome 11q23.2, have been shown to be associated with psychiatric disorders in samples of European ancestry...
  3. Walstab J, Hammer C, Lasitschka F, Möller D, Connolly C, Rappold G, et al. RIC-3 exclusively enhances the surface expression of human homomeric 5-hydroxytryptamine type 3A (5-HT3A) receptors despite direct interactions with 5-HT3A, -C, -D, and -E subunits. J Biol Chem. 2010;285:26956-65 pubmed publisher
    ..These data implicate a possible role of RIC-3 in determining 5-HT(3) receptor composition in vivo. ..
  4. Boyd G, Low P, Dunlop J, Robertson L, Vardy A, Lambert J, et al. Assembly and cell surface expression of homomeric and heteromeric 5-HT3 receptors: the role of oligomerization and chaperone proteins. Mol Cell Neurosci. 2002;21:38-50 pubmed
    ..In support of the existence of homomeric 5-HT3 receptors in vivo, recombinantly expressed 5-HT3A receptors were capable of clustered cell surface expression in cortical neurons. ..
  5. Niesler B, Flohr T, Nöthen M, Fischer C, Rietschel M, Franzek E, et al. Association between the 5' UTR variant C178T of the serotonin receptor gene HTR3A and bipolar affective disorder. Pharmacogenetics. 2001;11:471-5 pubmed
    ..was to identify nucleotide variants in a specific portion of the 5' region of the serotonin receptor gene (HTR3A) containing upstream open reading frames (uORFs) and to investigate their effect on bipolar disease...
  6. Krzywkowski K, Davies P, Irving A, Brauner Osborne H, Jensen A. Characterization of the effects of four HTR3B polymorphisms on human 5-HT3AB receptor expression and signalling. Pharmacogenet Genomics. 2008;18:1027-40 pubmed publisher
    ..In contrast, three other 5-HT3B variants, S156R, V183I and A223T, do not appear to alter 5-HT3AB receptor expression or signalling. ..
  7. Krzywkowski K, Davies P, Feinberg Zadek P, Brauner Osborne H, Jensen A. High-frequency HTR3B variant associated with major depression dramatically augments the signaling of the human 5-HT3AB receptor. Proc Natl Acad Sci U S A. 2008;105:722-7 pubmed publisher
    ..Thus, the impact of the high-frequency variant 5-HT3B(Y129S) on 5-HT3AB receptor signaling calls for a search for additional phenotypes, and the variant may thus aid in establishing the role of the 5-HT3AB receptor in pathophysiology. ..
  8. Hammer C, Kapeller J, Endele M, Fischer C, Hebebrand J, Hinney A, et al. Functional variants of the serotonin receptor type 3A and B gene are associated with eating disorders. Pharmacogenet Genomics. 2009;19:790-9 pubmed publisher
    ..response) have triggered our interest in investigating the putative role of variants in the 5-HT3 receptor genes, HTR3A and HTR3B, in the susceptibility to anorexia nervosa (AN) and bulimia nervosa (BN)...
  9. Kapeller J, Houghton L, Monnikes H, Walstab J, Möller D, Bonisch H, et al. First evidence for an association of a functional variant in the microRNA-510 target site of the serotonin receptor-type 3E gene with diarrhea predominant irritable bowel syndrome. Hum Mol Genet. 2008;17:2967-77 pubmed publisher
    ..complex conditions, we investigated the untranslated regions (UTRs) of the serotonin receptor type 3 subunit genes HTR3A and HTR3E...
  10. van Lelyveld N, Linde J, Schipper M, Samsom M. Candidate genotypes associated with functional dyspepsia. Neurogastroenterol Motil. 2008;20:767-73 pubmed publisher
    ..Polymorphisms in genes encoding the serotonin receptor type three A subunit (HTR3A), the serotonin transporter (SERT) and the G-protein beta3 subunit (GNB3) were analysed...
  11. Ilegems E, Pick H, Deluz C, Kellenberger S, Vogel H. Noninvasive imaging of 5-HT3 receptor trafficking in live cells: from biosynthesis to endocytosis. J Biol Chem. 2004;279:53346-52 pubmed
  12. Sugai T, Suzuki Y, Sawamura K, Fukui N, Inoue Y, Someya T. The effect of 5-hydroxytryptamine 3A and 3B receptor genes on nausea induced by paroxetine. Pharmacogenomics J. 2006;6:351-6 pubmed
    We investigated the effect of 5-hydroxytryptamine 3A and 3B receptor (HTR3A and HTR3B) gene polymorphisms on nausea induced by paroxetine in Japanese psychiatric patients...
  13. Gatt J, Williams L, Schofield P, Dobson Stone C, Paul R, Grieve S, et al. Impact of the HTR3A gene with early life trauma on emotional brain networks and depressed mood. Depress Anxiety. 2010;27:752-9 pubmed publisher
    ..The role of serotonin 3A receptor gene (HTR3A -42C>T polymorphism) and its interaction with early life stress (ELS) was investigated in view of the receptor'..
  14. Melke J, Westberg L, Nilsson S, Landen M, Soderstrom H, Baghaei F, et al. A polymorphism in the serotonin receptor 3A (HTR3A) gene and its association with harm avoidance in women. Arch Gen Psychiatry. 2003;60:1017-23 pubmed
    ..Serotonin receptor type 3 is a ligand-gated channel encoded by 2 different subunit genes, HTR3A and HTR3B...
  15. Kelley S, Dunlop J, Kirkness E, Lambert J, Peters J. A cytoplasmic region determines single-channel conductance in 5-HT3 receptors. Nature. 2003;424:321-4 pubmed
    ..Our findings solve the conundrum of the anomalously low conductance of homomeric 5-HT3A receptors and indicate an important function for the HA-stretch in Cys-loop transmitter-gated ion channels. ..
  16. Baptista Hon D, Deeb T, Lambert J, Peters J, Hales T. The minimum M3-M4 loop length of neurotransmitter-activated pentameric receptors is critical for the structural integrity of cytoplasmic portals. J Biol Chem. 2013;288:21558-68 pubmed publisher
  17. Niesler B, Weiss B, Fischer C, Nöthen M, Propping P, Bondy B, et al. Serotonin receptor gene HTR3A variants in schizophrenic and bipolar affective patients. Pharmacogenetics. 2001;11:21-7 pubmed
    ..In this study, we assessed sequence variations of the HTR3A gene...
  18. Davies P, Pistis M, Hanna M, Peters J, Lambert J, Hales T, et al. The 5-HT3B subunit is a major determinant of serotonin-receptor function. Nature. 1999;397:359-63 pubmed
    ..In addition to providing a new target for therapeutic agents, the 5-HT3B subunit will be a valuable resource for defining the molecular mechanisms of ion-channel function. ..
  19. Miyake A, Mochizuki S, Takemoto Y, Akuzawa S. Molecular cloning of human 5-hydroxytryptamine3 receptor: heterogeneity in distribution and function among species. Mol Pharmacol. 1995;48:407-16 pubmed
    ..Our data revealed that the 5-HT3R molecule has interspecies differences in both tissue distribution and functional profile. ..
  20. Udina M, Navines R, Egmond E, Oriolo G, Langohr K, Gimenez D, et al. Glucocorticoid Receptors, Brain-Derived Neurotrophic Factor, Serotonin and Dopamine Neurotransmission are Associated with Interferon-Induced Depression. Int J Neuropsychopharmacol. 2016;19: pubmed publisher
    ..These findings may help to improve the management of patients on antiviral treatment and broaden our understanding of the pathogenesis of mood disorders. ..
  21. Sarrouilhe D, Dejean C. [Autism spectrum disorders and bisphenol A: Is serotonin the lacking link in the chain?]. Encephale. 2017;43:402-404 pubmed publisher
    ..In France, BPA was banned in baby bottles in 2010 and in any food or beverage packaging since January 2015. Therefore, there is an urgent need to find safe alternatives in the use of BPA in the manufacture of industrial products. ..
  22. Vizziano Cantonnet D, Lasalle A, Di Landro S, Klopp C, Genthon C. De novo transcriptome analysis to search for sex-differentiation genes in the Siberian sturgeon. Gen Comp Endocrinol. 2018;268:96-109 pubmed publisher
    ..These newly-reported genes are involved in stem-cell niche building and regulation as well as sex-specific nerve development. ..
  23. Hong S, Lee J, Lee J, Lee H, Kim H, Lee S, et al. The traditional drug Gongjin-Dan ameliorates chronic fatigue in a forced-stress mouse exercise model. J Ethnopharmacol. 2015;168:268-78 pubmed publisher
    ..The underlying mechanisms involve attenuation of oxidative and inflammatory reactions in muscle and regulation of the stress response through the hypothalmo-pituitary-adrenal axis. ..
  24. Aminzadeh A. Protective effect of tropisetron on high glucose induced apoptosis and oxidative stress in PC12 cells: roles of JNK, P38 MAPKs, and mitochondria pathway. Metab Brain Dis. 2017;32:819-826 pubmed publisher
    ..The phosphorylation of these kinases was inhibited by tropisetron. It may be concluded that tropisetron treatment protects PC12 cells against HG-induced apoptosis by preventing JNK, P38 activation and mitochondrial pathway. ..
  25. El Oussini H, Bayer H, Scekic Zahirovic J, Vercruysse P, Sinniger J, Dirrig Grosch S, et al. Serotonin 2B receptor slows disease progression and prevents degeneration of spinal cord mononuclear phagocytes in amyotrophic lateral sclerosis. Acta Neuropathol. 2016;131:465-80 pubmed publisher
    ..Thus, the 5-HT2B receptor limits degeneration of spinal cord mononuclear phagocytes, most likely microglia, and slows disease progression in ALS. Targeting this receptor might be therapeutically useful. ..
  26. Gressier F, Porcelli S, Calati R, Serretti A. Pharmacogenetics of clozapine response and induced weight gain: A comprehensive review and meta-analysis. Eur Neuropsychopharmacol. 2016;26:163-185 pubmed publisher
    ..SNPs in 6 genes to perform meta-analyses: DRD2 rs1799732, DRD3 rs6280, HTR2A rs6313, rs6311, rs6314, HTR2C rs6318, HTR3A rs1062613, TNFa rs1800629...
  27. Mizuta N, Akiyoshi J, Sato A, Hanada H, Tanaka Y, Tsuru J, et al. Serotonin receptor 3A (HTR3A) gene is associated with personality traits, but not panic disorder. Psychiatr Genet. 2008;18:44 pubmed publisher
  28. Su Y, Chiu Y, Lin S, Chen C, Sun W. Serotonin Receptor 2B Mediates Mechanical Hyperalgesia by Regulating Transient Receptor Potential Vanilloid 1. J Mol Neurosci. 2016;59:113-25 pubmed publisher
    ..Thus, 5-HT2B mediates 5-HT-induced mechanical hyperalgesia by regulating TRPV1 function. ..
  29. Larson E, Vandenbeuch A, Voigt A, Meyerhof W, Kinnamon S, Finger T. The Role of 5-HT3 Receptors in Signaling from Taste Buds to Nerves. J Neurosci. 2015;35:15984-95 pubmed publisher
    ..Our results suggest that 5-HT released from type III cells activates gustatory nerve fibers via 5-HT3 receptors, accounting for a significant proportion of the neural taste response. ..
  30. Barrenschee M, Zorenkov D, Böttner M, Lange C, Cossais F, Scharf A, et al. Distinct pattern of enteric phospho-alpha-synuclein aggregates and gene expression profiles in patients with Parkinson's disease. Acta Neuropathol Commun. 2017;5:1 pubmed publisher
    ..Increased expression of dopamine receptor D1, VIP and serotonin receptor 3A was observed in PD patients, while serotonin receptor 4 and muscarinic receptor 3 (M3R) were downregulated...
  31. Alix K, Khatri S, Mosier P, Casterlow S, Yan D, Nyce H, et al. Superagonist, Full Agonist, Partial Agonist, and Antagonist Actions of Arylguanidines at 5-Hydroxytryptamine-3 (5-HT3) Subunit A Receptors. ACS Chem Neurosci. 2016;7:1565-1574 pubmed
  32. Zurawski Z, Rodriguez S, Hyde K, Alford S, Hamm H. Gβγ Binds to the Extreme C Terminus of SNAP25 to Mediate the Action of Gi/o-Coupled G Protein-Coupled Receptors. Mol Pharmacol. 2016;89:75-83 pubmed publisher
    ..Syt1 calcium-dependent binding to SNAP25Δ3 was reduced by a small extent compared with the wild type. We conclude that the extreme C terminus of SNAP25 is a critical region for the Gβγ-SNARE interaction. ..
  33. Gutierrez B, Arranz M, Huezo Diaz P, Dempster D, Matthiasson P, Travis M, et al. Novel mutations in 5-HT3A and 5-HT3B receptor genes not associated with clozapine response. Schizophr Res. 2002;58:93-7 pubmed
    ..Two different isoforms of 5-HT3 receptor subunit genes (HTR3A and HTR3B) have been identified. They have been assigned to chromosome 11q23.1-q23...
  34. Scrogin K, Johnson A, Brooks V. Methysergide delays the decompensatory responses to severe hemorrhage by activating 5-HT(1A) receptors. Am J Physiol Regul Integr Comp Physiol. 2000;279:R1776-86 pubmed
    ..These data indicate that methysergide stimulates 5-HT(1A) receptors to delay the decompensatory responses to hemorrhage...
  35. Chhibber A, Zhao L. ER? and ApoE isoforms interact to regulate BDNF-5-HT2A signaling and synaptic function in the female brain. Alzheimers Res Ther. 2017;9:79 pubmed publisher
    ..Enhancing ER? activity could provide a greater therapeutic benefit to non-ApoE4 carriers than to ApoE4 carriers in interventions for these brain disorders. ..
  36. Krzywkowski K, Jensen A, Connolly C, Brauner Osborne H. Naturally occurring variations in the human 5-HT3A gene profoundly impact 5-HT3 receptor function and expression. Pharmacogenet Genomics. 2007;17:255-66 pubmed
    ..These severe single nucleotide polymorphism effects hold promise for identification of new 5-HT3A gene-disease causalities. ..
  37. Falola M, Limdi N, Shelton R. Clinical and Genetic Predictors of Delayed Remission After Multiple Levels of Antidepressant Treatment: Toward Early Identification of Depressed Individuals for Advanced Care Options. J Clin Psychiatry. 2017;78:e1291-e1298 pubmed publisher
    ..The results offer clinical tools for clinicians to identify depressed individuals who are likely to have delayed remission with multiple antidepressant treatments and therefore might be candidates for advanced care options. ..
  38. Wu D, Othman N, Sharp D, Mahendra A, Deeb T, Hales T. A conserved cysteine residue in the third transmembrane domain is essential for homomeric 5-HT3 receptor function. J Physiol. 2010;588:603-16 pubmed publisher
    ..Thus, 5-HT(3)A residue 312 and equivalent polar residues in the M3 of other Cys-loop subunits are essential determinants of homopentameric gating. ..
  39. Lambe E, Fillman S, Webster M, Shannon Weickert C. Serotonin receptor expression in human prefrontal cortex: balancing excitation and inhibition across postnatal development. PLoS ONE. 2011;6:e22799 pubmed publisher
    ..Examining and understanding the healthy balance is critical to appreciate how abnormal expression of an individual HTR may create a window of vulnerability for the emergence of psychiatric illness. ..
  40. García González D, Khodosevich K, Watanabe Y, Rollenhagen A, Lübke J, Monyer H. Serotonergic Projections Govern Postnatal Neuroblast Migration. Neuron. 2017;94:534-549.e9 pubmed publisher
    ..Furthermore, we show that the underlying mechanism involves serotonin receptor 3A (5HT3A)-mediated calcium influx...
  41. Distler O, Cozzio A. Systemic sclerosis and localized scleroderma--current concepts and novel targets for therapy. Semin Immunopathol. 2016;38:87-95 pubmed publisher
    ..Finally, we discuss whether the novel targeted therapies currently tested in SSc could be used for localized scleroderma. ..
  42. Darmon M, Al Awabdh S, Emerit M, Masson J. Insights into Serotonin Receptor Trafficking: Cell Membrane Targeting and Internalization. Prog Mol Biol Transl Sci. 2015;132:97-126 pubmed publisher
    ..In this review, we describe the trafficking of 5-HTRs including their internalization, desensitization, or addressing to the plasma membrane depending on specific mechanisms which are peculiar for each class of serotonin receptor. ..
  43. Ko C, Liu Y. Disruptions of sensorimotor gating, cytokines, glycemia, monoamines, and genes in both sexes of rats reared in social isolation can be ameliorated by oral chronic quetiapine administration. Brain Behav Immun. 2016;51:119-30 pubmed publisher
    ..inhibition (PPI)] and the expression of monoamines (dopamine and serotonin) and related genes (Htr1a, Htr2a, Htr3a, Drd1a, and Gabbr2)...
  44. Ritze Y, Hengelhaupt C, Bárdos G, Ernst B, Thurnheer M, D Haese J, et al. Altered intestinal neuroendocrine gene expression in humans with obesity. Obesity (Silver Spring). 2015;23:2278-85 pubmed publisher
    ..1 receptor (GLP1R), serotonin transporter (SERT), tryptophan hydroxylase 1 (TPH1), and serotonin receptor 3A (5HT3A R) was determined with qRT-PCR...
  45. Wierucka Rybak M, Wolak M, Juszczak M, Drobnik J, Bojanowska E. The inhibitory effect of combination treatment with leptin and cannabinoid CB1 receptor agonist on food intake and body weight gain is mediated by serotonin 1B and 2C receptors. J Physiol Pharmacol. 2016;67:457-63 pubmed
    ..These results suggest that serotonin mediates the leptin- and AM 251-dependent regulation of feeding behavior in rats via the 5-HT1B and 5-HT2C receptors. ..
  46. Weitekamp C, Nguyen J, Hofmann H. Neuromolecular Regulation of Aggression Differs by Social Role during Joint Territory Defense. Integr Comp Biol. 2017;57:631-639 pubmed publisher
    ..Our results highlight the critical effect of social context on both behavior and its neuromolecular basis. ..
  47. Zolotarev Y, Kovalev G, Kost N, Voevodina M, Sokolov O, Dadayan A, et al. Anxiolytic activity of the neuroprotective peptide HLDF-6 and its effects on brain neurotransmitter systems in BALB/c and C57BL/6 mice. J Psychopharmacol. 2016;30:922-35 pubmed publisher
    ..The psychotropic activity of HLDF-6-amide is promising for its introduction to medical practice as a highly effective anxiolytic medicine for mental and neurological diseases. ..
  48. Zanos P, Thompson S, Duman R, Zarate C, Gould T. Convergent Mechanisms Underlying Rapid Antidepressant Action. CNS Drugs. 2018;32:197-227 pubmed publisher
    ..These ongoing studies suggest that the future acute treatment of depression will typically occur within hours, rather than months, of treatment initiation. ..
  49. McLaughlin P, Jagielo Miller J, Plyler E, Schutte K, Vemuri V, Makriyannis A. Differential effects of cannabinoid CB1 inverse agonists and antagonists on impulsivity in male Sprague Dawley rats: identification of a possibly clinically relevant vulnerability involving the serotonin 5HT1A receptor. Psychopharmacology (Berl). 2017;234:1029-1043 pubmed publisher
    ..Furthermore, neutral CB1 antagonists do not produce this effect and therefore may have greater safety. ..
  50. Shen E, Jiang Y, Javidfar B, Kassim B, Loh Y, Ma Q, et al. Neuronal Deletion of Kmt2a/Mll1 Histone Methyltransferase in Ventral Striatum is Associated with Defective Spike-Timing-Dependent Striatal Synaptic Plasticity, Altered Response to Dopaminergic Drugs, and Increased Anxiety. Neuropsychopharmacology. 2016;41:3103-3113 pubmed publisher
    ..Therefore, Kmt2a regulates synaptic plasticity in striatal neurons and provides an epigenetic drug target for anxiety and dopamine-mediated behaviors. ..
  51. Cao X, Chen Y, Zhang Y, Qiu Y, Yu M, Xu X, et al. Synthesis and biological evaluation of new 6-hydroxypyridazinone benzisoxazoles: Potential multi-receptor-targeting atypical antipsychotics. Eur J Med Chem. 2016;124:713-728 pubmed publisher
    ..In contrast to risperidone, compound 46 exhibited a high cataleptic threshold; this may be useful in the development of a novel class of drugs treating schizophrenia. ..
  52. Zhong J, Liu Z, Zhou X, Xu J. Synergic Anti-Pruritus Mechanisms of Action for the Radix Sophorae Flavescentis and Fructus Cnidii Herbal Pair. Molecules. 2017;22: pubmed publisher
    ..are inflammation-related proteins (MAPK14, PTGS2, PTGS2, and F2) and pruritus-related proteins (HRH1, TRPA1, HTR3A, and HTR6)...
  53. Ji X, Takahashi N, Saito S, Ishihara R, Maeno N, Inada T, et al. Relationship between three serotonin receptor subtypes (HTR3A, HTR2A and HTR4) and treatment-resistant schizophrenia in the Japanese population. Neurosci Lett. 2008;435:95-8 pubmed publisher
    ..study, single marker and haplotype analyses between several mutations of serotonin receptor subtypes (HTR2A, HTR3A and HTR4) and TRS (TRS=101, NON-TRS=239) were performed to determine a possible relationship with the development ..
  54. Stratford J, Larson E, Yang R, Salcedo E, Finger T. 5-HT3A -driven green fluorescent protein delineates gustatory fibers innervating sour-responsive taste cells: A labeled line for sour taste?. J Comp Neurol. 2017;525:2358-2375 pubmed publisher
  55. Shin H, Lee J, Kim K, Shin H, Choi J, Lee C, et al. Modulation of hippocampal neuronal activity by So-ochim-tang-gamibang in mice subjected to chronic restraint stress. BMC Complement Altern Med. 2017;17:456 pubmed publisher
    ..Our data suggest that SOCG treatment may increase synaptic responsiveness to serotonergic neuronal inputs by upregulating 5-HT1AR in the hippocampal neurons. ..
  56. Barann M, Linden I, Witten S, Urban B. Molecular actions of propofol on human 5-HT3A receptors: enhancement as well as inhibition by closely related phenol derivatives. Anesth Analg. 2008;106:846-57, table of contents pubmed publisher
    ..Propofol was less potent than expected from its hydrophobic properties. Underlying mechanisms appear to involve the phenolic hydroxyl group, hydrophobic interactions, and steric restrictions. ..
  57. Guan T, Li T, Cai W, Huang D, Ouyang P, Wang Y, et al. HTR3A and HTR3E gene polymorphisms and diarrhea predominant irritable bowel syndrome risk: evidence from a meta-analysis. Oncotarget. 2017;8:100459-100468 pubmed publisher
    Several studies have reported an association between serotonin receptor type 3 (5-HT3) subunit genes HTR3A (rs1062613) and HTR3E (rs62625044) and diarrhea predominant irritable bowel syndrome (IBS-D)...
  58. Mujakovic S, Ter Linde J, de Wit N, Van Marrewijk C, Fransen G, Onland Moret N, et al. Serotonin receptor 3A polymorphism c.-42C > T is associated with severe dyspepsia. BMC Med Genet. 2011;12:140 pubmed publisher
    ..Interestingly, a functional polymorphism in HTR3A, encoding the 5-HT3 receptor A subunit, has been reported to be associated with depression and anxiety related ..
  59. Enoch M, Gorodetsky E, Hodgkinson C, Roy A, Goldman D. Functional genetic variants that increase synaptic serotonin and 5-HT3 receptor sensitivity predict alcohol and drug dependence. Mol Psychiatry. 2011;16:1139-46 pubmed publisher
    ..single-nucleotide polymorphisms (SNPs) across HTR3B (including the functional rs1176744 Tyr129Ser) and HTR3A, genes encoding 5-HT3 receptors...
  60. Louca Jounger S, Christidis N, Hedenberg Magnusson B, List T, Svensson P, Schalling M, et al. Influence of Polymorphisms in the HTR3A and HTR3B Genes on Experimental Pain and the Effect of the 5-HT3 Antagonist Granisetron. PLoS ONE. 2016;11:e0168703 pubmed publisher
    ..Sixty healthy participants were genotyped regarding HTR3A (rs1062613) and HTR3B (rs1176744). First, pain was induced by bilateral hypertonic saline injections (HS, 5.5%, 0...
  61. Frank B, Niesler B, Bondy B, Späth M, Pongratz D, Ackenheil M, et al. Mutational analysis of serotonin receptor genes: HTR3A and HTR3B in fibromyalgia patients. Clin Rheumatol. 2004;23:338-44 pubmed
    ..In our study, both serotonin receptor subunit genes, HTR3A and HTR3B, have been investigated for sequence variations in FMS patients in order to reveal a possible ..
  62. Mastrangelo L, Cassidy A, Mulholland F, Wang W, Bao Y. Serotonin receptors, novel targets of sulforaphane identified by proteomic analysis in Caco-2 cells. Cancer Res. 2008;68:5487-91 pubmed publisher
    ..Thus, the effect of sulforaphane may help to elucidate signaling pathways serotonin-mediated in colon cancer and lead to development of potential novel therapeutic agents. ..
  63. Wittmann M, Peters I, Schaaf T, Wartenberg H, Wirz S, Nadstawek J, et al. The effects of morphine on human 5-HT3A receptors. Anesth Analg. 2006;103:747-52 pubmed
    ..The effects of morphine and naloxone were not additive. The potency of morphine and the competitivity of the blocking effect points to a specific mechanism at a receptor site rather than an unspecific membrane effect. ..
  64. Korytina G, Akhmadishina L, Kochetova O, Aznabaeva Y, Zagidullin S, Victorova T. [Polymorphic Variants of Glutamate Receptor (GRIK5, GRIN2B) and Serotonin Receptor (HTR2A) Genes Are Associated with Chronic Obstructive Pulmonary Disease]. Mol Biol (Mosk). 2017;51:603-614 pubmed publisher
    ..0011 and P = 0.037). Our results may provide insight into potential molecular mechanisms that involve the glutamate (GRIK5, GRIN2B) and serotonin (HTR2A) receptor genes in the pathogenesis of COPD. ..
  65. Hassaine G, Deluz C, Grasso L, Wyss R, Hovius R, Stahlberg H, et al. Expression, Biochemistry, and Stabilization with Camel Antibodies of Membrane Proteins: Case Study of the Mouse 5-HT3 Receptor. Methods Mol Biol. 2017;1635:139-168 pubmed publisher
    ..These protocols were used to solve the structure of the mouse 5-HT3 serotonin receptor but are of broad applicability for crystallization or cryo-electron microscopy projects. ..
  66. Olaya J, Heusner C, Matsumoto M, Sinclair D, Kondo M, Karl T, et al. Overexpression of Neuregulin 1 Type III Confers Hippocampal mRNA Alterations and Schizophrenia-Like Behaviors in Mice. Schizophr Bull. 2017;: pubmed publisher
  67. Hagbom M, Novak D, Ekstrom M, Khalid Y, Andersson M, Lindh M, et al. Ondansetron treatment reduces rotavirus symptoms-A randomized double-blinded placebo-controlled trial. PLoS ONE. 2017;12:e0186824 pubmed publisher
  68. Dinklo T, Lesage A, Grantham C. Desensitization characteristics of the human alpha7nAChR/5HT3A chimera receptor. J Mol Neurosci. 2006;30:109-10 pubmed
    ..Here, we describe a fully human chimera receptor (h-alpha7/5HT3A), which is characterized by desensitization, and recovery kinetics that deviate from the human WT alpha7. ..
  69. Murata Y, Kobayashi D, Imuta N, Haraguchi K, Ieiri I, Nishimura R, et al. Effects of the serotonin 1A, 2A, 2C, 3A, and 3B and serotonin transporter gene polymorphisms on the occurrence of paroxetine discontinuation syndrome. J Clin Psychopharmacol. 2010;30:11-7 pubmed publisher
  70. Jonsson E, Bah J, Melke J, Abou Jamra R, Schumacher J, Westberg L, et al. Monoamine related functional gene variants and relationships to monoamine metabolite concentrations in CSF of healthy volunteers. BMC Psychiatry. 2004;4:4 pubmed
    ..possible relationships between DNA polymorphisms in the serotonin 2C receptor (HTR2C), the serotonin 3A receptor (HTR3A), the dopamine D4 receptor (DRD4), and the dopamine beta-hydroxylase (DBH) genes and CSF concentrations of 5-..
  71. Pote W, Musarira S, Chuma D, Gadaga L, Mwandiringana E, Tagwireyi D. Effects of a hydroethanolic extract of Boophone disticha bulb on anxiety-related behaviour in naive BALB/c mice. J Ethnopharmacol. 2018;214:218-224 pubmed publisher
    ..The extract of B. disticha exerted good anxiolytic-like activity in both the ST and OF at medium dose (25mg/kg), while the low dose (10mg/kg) showed prominent anxiolytic-like activity in the EPM. ..
  72. Maksay G, Bikadi Z, Simonyi M. Binding interactions of antagonists with 5-hydroxytryptamine3A receptor models. J Recept Signal Transduct Res. 2003;23:255-70 pubmed
    ..Ligand binding interferes with crucial intra- and interface interactions along the binding cleft. ..
  73. Diamantopoulou A, Kalpachidou T, Aspiotis G, Gampierakis I, Stylianopoulou F, Stamatakis A. An early experience of mild adversity involving temporary denial of maternal contact affects the serotonergic system of adult male rats and leads to a depressive-like phenotype and inability to adapt to a chronic social stress. Physiol Behav. 2018;184:46-54 pubmed publisher
    ..They also suggest that even mild adversity, if it involves intervention in mother-offspring interactions, can be sufficient to compromise adaptability. ..
  74. van Lelyveld N, Ter Linde J, Schipper M, Samsom M. Regional differences in expression of TPH-1, SERT, 5-HT(3) and 5-HT(4) receptors in the human stomach and duodenum. Neurogastroenterol Motil. 2007;19:342-8 pubmed
  75. Marazziti D, Betti L, Giannaccini G, Rossi A, Masala I, Baroni S, et al. Distribution of [3H]GR65630 binding in human brain postmortem. Neurochem Res. 2001;26:187-90 pubmed
    ..These observations extend previous findings on the distribution of 5-HT3 receptors and confirm interspecies variations that might explain the heterogeneous properties of 5-HT3 receptors in different animals. ..
  76. Uetz P, Abdelatty F, Villarroel A, Rappold G, Weiss B, Koenen M. Organisation of the murine 5-HT3 receptor gene and assignment to human chromosome 11. FEBS Lett. 1994;339:302-6 pubmed
    ..The 5-HT3R gene, whose structure is closely related to neuronal and muscle AChR alpha genes, as demonstrated by four common splice junctions, was localised on human chromosome 11. ..
  77. Anderson B, Schnetz Boutaud N, Bartlett J, Wotawa A, Wright H, Abramson R, et al. Examination of association of genes in the serotonin system to autism. Neurogenetics. 2009;10:209-16 pubmed publisher
    ..0002; p = 0.02 after correcting for multiple comparisons) was found at rs1150220 (HTR3A) located on chromosome 11 ( approximately 113 Mb)...
  78. Laursen S, Leontiadis G, Stanley A, Hallas J, Schaffalitzky De Muckadell O. The use of selective serotonin receptor inhibitors (SSRIs) is not associated with increased risk of endoscopy-refractory bleeding, rebleeding or mortality in peptic ulcer bleeding. Aliment Pharmacol Ther. 2017;46:355-363 pubmed publisher
    ..Further data are needed to clarify whether treatment with SSRIs is associated with poor outcomes, which would support temporary discontinuation of treatment...
  79. Lennertz L, Wagner M, Frommann I, Schulze Rauschenbach S, Schuhmacher A, Kuhn K, et al. A coding variant of the novel serotonin receptor subunit 5-HT3E influences sustained attention in schizophrenia patients. Eur Neuropsychopharmacol. 2010;20:414-20 pubmed publisher
    ..This study provides additional evidence for a role of the serotonergic system and the 5-HT3 receptor in schizophrenia. ..
  80. Souza R, De Luca V, Manchia M, Kennedy J. Are serotonin 3A and 3B receptor genes associated with suicidal behavior in schizophrenia subjects?. Neurosci Lett. 2011;489:137-41 pubmed publisher
    ..We evaluated whether genetic variants in the serotonin receptors HTR3A (rs897692, rs1150226, rs1176724, rs2276302, rs3737457, rs897687 and rs1176713) and HTR3B (rs3758987, rs10502180, ..
  81. Joy Lin Y, Hsu C, Hsieh H, Tseng C, Sun H. Sequence variants of the HTR3A gene contribute to the genetic prediction of postoperative nausea in Taiwan. J Hum Genet. 2014;59:655-60 pubmed publisher
    ..Current clinical and basic research suggests that the 5-hydroxytryptamine type 3A receptor (HTR3A) may be important in the occurrence of PON...
  82. Morton R, Baptista Hon D, Hales T, Lovinger D. Agonist- and antagonist-induced up-regulation of surface 5-HT3 A receptors. Br J Pharmacol. 2015;172:4066-77 pubmed publisher
    ..However, this will require further investigation in vivo. ..
  83. Nikiforuk A, Hołuj M, Kos T, Popik P. The effects of a 5-HT5A receptor antagonist in a ketamine-based rat model of cognitive dysfunction and the negative symptoms of schizophrenia. Neuropharmacology. 2016;105:351-360 pubmed publisher
    ..The utility of this receptor as a target for improvement of cognitive and social dysfunctions warrants further studies. ..
  84. Santello M, Bisco A, Nevian N, Lacivita E, Leopoldo M, Nevian T. The brain-penetrant 5-HT7 receptor agonist LP-211 reduces the sensory and affective components of neuropathic pain. Neurobiol Dis. 2017;106:214-221 pubmed publisher
    ..Thus systemic treatment with a 5-HT7R agonist leads to modulation of the ACC, which dampens sensory and affective aspects of chronic pain. ..
  85. Etxabe A, Lara Castillo M, Cornet Masana J, Banús Mulet A, Nomdedeu M, Torrente M, et al. Inhibition of serotonin receptor type 1 in acute myeloid leukemia impairs leukemia stem cell functionality: a promising novel therapeutic target. Leukemia. 2017;31:2288-2302 pubmed publisher
    ..Our results highlight the importance of HTR1 in leukemogenesis and LSC survival and identify this receptor family as a new target for therapy in AML with prognostic value. ..