5-HT3 receptor

[1][2][3] This ion channel is cation-selective and mediates neuronal depolarization and excitation within the central and peripheral nervous systems.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.The 5-HT3C, 5-HT3D and 5-HT3E genes tend to show peripherally restricted pattern of expression, with high levels in the gut.The 5-HT3 receptor is expressed throughout the central and peripheral nervous systems and mediates a variety of physiological functions.[14] On a cellular level, it has been shown that postsynaptic 5-HT3 receptors mediate fast excitatory synaptic transmission in rat neocortical interneurons, amygdala, and hippocampus, and in ferret visual cortex.

Figure 1. The subunits are assembled as a pentamer (right) and each subunit has four transmembrane domains (left).

Figure 2. Structure of the mouse 5HT3 receptor gene , showing its 9 exons (E1-E9), corresponding to the exons shown in the cDNA below. The 5' ends of exons 2, 6, and 9 have alternative splice sites. Figure drawn to scale. Modified after Uetz et al. 1994. ^{[

12

]}

Figure 3. The cDNA sequence of the mouse 5HT3 receptor . The cDNA encodes a 122 nucleotide 5' UTR and a ~510 nucleotide 3' UTR. Boxes indicate exons and the numbers below the exons indicate their length. For instance, the first exon encodes 22 amino acids plus one nucleotide belonging to a split codon with another 2 nucleotides encoded by the next exon. M1-4 indicate the transmembrane helices and C-C indicates the Cysteine loop. Modified after Uetz et al. 1994 ^{[

12

]}

Cys-loop superfamilyligand-gated ion channels5-HT receptorsserotoninG protein-coupled receptorscationcentralperipheralnervous systemssodiumpotassiumcalciumneurotransmitteranionsnicotinic acetylcholine receptor5-HT receptorG-protein-coupled5-HT3Aion channelextracellulartransmembraneagonistscompetitive antagonistscell membranechromosomes 11gene duplicationspathophysiologicalintronsα7-acetylcholine receptorduodenumstomachchemotherapeuticpolymorphism5-HTR3B receptorbiomarkerperipheral nervous systemsamygdalavisual cortexbrain stemnociceptiveemesisCereulide2-methyl-5-HTAlpha-MethyltryptamineBufoteninChlorophenylbiguanideEthanolIbogainePhenylbiguanideQuipazineRS-56812SR-57227VareniclineYM-31636CGS-12066A5-HT3 antagonistAntiemeticsAS-8112GranisetronOndansetronTropisetronGastroprokineticsAlosetronBatanoprideMetoclopramideRenzaprideZacopridemosaprideAntidepressantsBupropionMianserinMirtazapineVortioxetineAntipsychoticsClozapineOlanzapineQuetiapineAntimalarialsQuinineChloroquineMefloquineCannabidiol (CBD)Delta-9-TetrahydrocannabinolLamotrigineepilepsybipolar disorderMemantineAlzheimer's diseaseMentholThujoneIndoleAnaestheticsChloroformHalothaneIsofluranechemotherapyradiotherapyvomiting5-HT3 receptor antagonists5-HT1 receptor5-HT2 receptor5-HT4 receptor5-HT5 receptor5-HT6 receptor5-HT7 receptorBibcodeSpringer-VerlagMedical Subject Headingscell surface receptorCys-loop receptors5-HT/serotoninGABAA-ρGlycineNicotinic acetylcholine(α3)2(β4)3(α4)2(β2)3(α7)5(α1)2(β4)3 - Ganglion type(α1)2β1δε - Muscle typeZinc-activatedIonotropicglutamatesKainatePurinergic receptorsSerotonin receptormodulators5-HT1A8-OH-DPATAdatanserinAmphetamineetoperidonehydroxynefazodonenefazodonetrazodonetriazoledionevilazodoneAtypical antipsychoticsaripiprazoleasenapinebrexpiprazolecariprazinelurasidoneziprasidoneAzapironesbuspironeeptapironegepironeperospironetandospironeBay R 1531BefiradolBMY-14802CannabidiolDimemebfeDopamineEbalzotanEltoprazineEnciprazineErgolinesbromocriptinecabergolinedihydroergotamineergotaminelisuridemethylergometrine (methylergonovine)methysergidepergolideF-11,461F-15063F-15,599FlesinoxanFlibanserinFlumexadolHypidoneLesopitronLY-293284MKC-242NaluzotanOsemozotanOxaflozanePardoprunoxPiclozotanRauwolscineRepinotanRoxindoleRU-24,969S-14,506S-14671S-15535SarizotanSerotonin (5-HT)SunepitronTryptamines5-MeO-DMTindorenateN-Me-5-HTpsilocinpsilocybinTGBA01AD